PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 11248431-2 2001 Intrastriatal administration of phosphoramidon (PRN, 5 microM), a dual inhibitor of ECE and neutral endopeptidase (NEP), significantly increased infarct volume to hypoxia with a significant attenuation of CBF(LDF). phosphoramidon 32-46 endothelin converting enzyme 1 Rattus norvegicus 84-87 11248431-2 2001 Intrastriatal administration of phosphoramidon (PRN, 5 microM), a dual inhibitor of ECE and neutral endopeptidase (NEP), significantly increased infarct volume to hypoxia with a significant attenuation of CBF(LDF). phosphoramidon 32-46 membrane metallo-endopeptidase Rattus norvegicus 92-113 11248431-2 2001 Intrastriatal administration of phosphoramidon (PRN, 5 microM), a dual inhibitor of ECE and neutral endopeptidase (NEP), significantly increased infarct volume to hypoxia with a significant attenuation of CBF(LDF). phosphoramidon 32-46 membrane metallo-endopeptidase Rattus norvegicus 115-118 11248431-2 2001 Intrastriatal administration of phosphoramidon (PRN, 5 microM), a dual inhibitor of ECE and neutral endopeptidase (NEP), significantly increased infarct volume to hypoxia with a significant attenuation of CBF(LDF). phosphoramidon 32-46 CCAAT/enhancer binding protein zeta Rattus norvegicus 205-213 11223883-7 2001 NEP family members are potential therapeutic targets, for example in cardiovascular and inflammatory disorders, and potent and selective inhibitors such as phosphoramidon have contributed to understanding enzyme function. phosphoramidon 156-170 membrane metalloendopeptidase Homo sapiens 0-3 11223883-8 2001 Inhibitor design should be facilitated by the recent three-dimensional structural solution of the NEP-phosphoramidon complex. phosphoramidon 102-116 membrane metalloendopeptidase Homo sapiens 98-101 11099107-6 2000 PGE2 at 10(-5) M reduced the expression of ET-1 at the mRNA and protein levels but did not exert any significant modification at lower concentrations from 10(-10) to 10(6) M. Phosphoramidon, an endothelin converting enzyme (ECE) inhibitor, drastically decreased the amount of ET-1 accumulating in the culture medium in basal conditions or after UVB irradiation. phosphoramidon 175-189 endothelin converting enzyme 1 Homo sapiens 224-227 11385696-2 2001 In pig intravesical ureteral strips pretreated with phosphoramidon (10(-5) mol/L) to block the endopeptidase activities, isometric force recordings showed that SP, NKA, and the NK2 receptor selective agonist [beta-Ala(8)]-NKA (4-10), all three induced contractions, with the following potency order: NKA > [beta-Ala(8) ]-NKA (4-10) > SP. phosphoramidon 52-66 tachykinin precursor 1 Homo sapiens 164-167 11385696-2 2001 In pig intravesical ureteral strips pretreated with phosphoramidon (10(-5) mol/L) to block the endopeptidase activities, isometric force recordings showed that SP, NKA, and the NK2 receptor selective agonist [beta-Ala(8)]-NKA (4-10), all three induced contractions, with the following potency order: NKA > [beta-Ala(8) ]-NKA (4-10) > SP. phosphoramidon 52-66 tachykinin receptor 2 Homo sapiens 177-189 11385696-2 2001 In pig intravesical ureteral strips pretreated with phosphoramidon (10(-5) mol/L) to block the endopeptidase activities, isometric force recordings showed that SP, NKA, and the NK2 receptor selective agonist [beta-Ala(8)]-NKA (4-10), all three induced contractions, with the following potency order: NKA > [beta-Ala(8) ]-NKA (4-10) > SP. phosphoramidon 52-66 tachykinin precursor 1 Homo sapiens 222-225 11385696-2 2001 In pig intravesical ureteral strips pretreated with phosphoramidon (10(-5) mol/L) to block the endopeptidase activities, isometric force recordings showed that SP, NKA, and the NK2 receptor selective agonist [beta-Ala(8)]-NKA (4-10), all three induced contractions, with the following potency order: NKA > [beta-Ala(8) ]-NKA (4-10) > SP. phosphoramidon 52-66 tachykinin precursor 1 Homo sapiens 222-225 11385696-2 2001 In pig intravesical ureteral strips pretreated with phosphoramidon (10(-5) mol/L) to block the endopeptidase activities, isometric force recordings showed that SP, NKA, and the NK2 receptor selective agonist [beta-Ala(8)]-NKA (4-10), all three induced contractions, with the following potency order: NKA > [beta-Ala(8) ]-NKA (4-10) > SP. phosphoramidon 52-66 tachykinin precursor 1 Homo sapiens 222-225 11092533-6 2000 The NEP enzyme activity in these cell lines correlated with cell-surface protein levels and was abolished by the NEP inhibitor phosphoramidon. phosphoramidon 127-141 membrane metalloendopeptidase Homo sapiens 4-7 11145756-6 2000 Phosphoramidon and a specific ECE-1 inhibitor, FR901533, inhibited ECE-1 activity by over 90%. phosphoramidon 0-14 endothelin converting enzyme 1 Homo sapiens 67-72 11137456-5 2000 The endopeptidase PE, with a molecular weight of 45 kDa, was inhibited 100% by EDTA and pOHMB and resistant to PMSF, thyorphan, E64 and phosphoramidon, when we used the mentioned substrates. phosphoramidon 136-150 prolyl endopeptidase Homo sapiens 18-20 11078325-1 2000 Phosphoramidon has been shown to inhibit endothelin-converting enzyme-1 (ECE-1) in a remarkably pH-dependent manner (Ahn et al. phosphoramidon 0-14 endothelin converting enzyme 1 Homo sapiens 41-71 11078325-1 2000 Phosphoramidon has been shown to inhibit endothelin-converting enzyme-1 (ECE-1) in a remarkably pH-dependent manner (Ahn et al. phosphoramidon 0-14 endothelin converting enzyme 1 Homo sapiens 73-78 11092533-6 2000 The NEP enzyme activity in these cell lines correlated with cell-surface protein levels and was abolished by the NEP inhibitor phosphoramidon. phosphoramidon 127-141 membrane metalloendopeptidase Homo sapiens 113-116 11145282-6 2000 Pretreatment with phosphoramidon produced dose-dependent reduction in the extent of mucosal damage caused by indomethacin, accompanied by a significant recovery in the expression of cNOS, and a marked decline in ECE-1, epithelial cell apoptosis and the mucosal level of ET-1. phosphoramidon 18-32 nitric oxide synthase 3 Rattus norvegicus 182-186 11145282-2 2000 In this study using phosphoramidon, a potent inhibitor of endothelin-converting enzyme-1 (ECE-1), we investigated the influence of ET-1 on the expression of constitutive (cNOS) and inducible nitric oxide synthase (NOS-2) during gastric mucosal injury caused by indomethacin. phosphoramidon 20-34 endothelin converting enzyme 1 Rattus norvegicus 58-88 11145282-6 2000 Pretreatment with phosphoramidon produced dose-dependent reduction in the extent of mucosal damage caused by indomethacin, accompanied by a significant recovery in the expression of cNOS, and a marked decline in ECE-1, epithelial cell apoptosis and the mucosal level of ET-1. phosphoramidon 18-32 endothelin converting enzyme 1 Rattus norvegicus 212-217 11145282-2 2000 In this study using phosphoramidon, a potent inhibitor of endothelin-converting enzyme-1 (ECE-1), we investigated the influence of ET-1 on the expression of constitutive (cNOS) and inducible nitric oxide synthase (NOS-2) during gastric mucosal injury caused by indomethacin. phosphoramidon 20-34 endothelin converting enzyme 1 Rattus norvegicus 90-95 11145282-6 2000 Pretreatment with phosphoramidon produced dose-dependent reduction in the extent of mucosal damage caused by indomethacin, accompanied by a significant recovery in the expression of cNOS, and a marked decline in ECE-1, epithelial cell apoptosis and the mucosal level of ET-1. phosphoramidon 18-32 endothelin 1 Rattus norvegicus 270-274 11011035-6 2000 Exogenous endothelin-1 (1-100 nM) did not affect the catecholamine output responses, but it inhibited the responses under treatment with phosphoramidon and FR139317. phosphoramidon 137-151 endothelin 1 Rattus norvegicus 10-22 10951272-8 2000 Moreover, in the presence of phosphoramidon, a stable inhibitor of neprilysin, we observed an increased efficiency of alpha-melanocyte-stimulating hormone and adrenocorticotropic hormone to stimulate both tyrosinase activity and microphthalmia expression. phosphoramidon 29-43 membrane metalloendopeptidase Homo sapiens 67-77 11005759-10 2000 Inhibition of the cell-surface protease neutral endopeptidase (NEP) by phosphoramidon potentiated the effect of exogenous SP; therefore endogenous NEP attenuates SP-induced plasma extravasation. phosphoramidon 71-85 membrane metallo-endopeptidase Rattus norvegicus 40-61 11005759-10 2000 Inhibition of the cell-surface protease neutral endopeptidase (NEP) by phosphoramidon potentiated the effect of exogenous SP; therefore endogenous NEP attenuates SP-induced plasma extravasation. phosphoramidon 71-85 membrane metallo-endopeptidase Rattus norvegicus 63-66 11121595-5 2000 The endothelin-converting enzyme (ECE) inhibitor, phosphoramidon, and endothelin type-A (ETA) receptor antagonist BQ-123 reduced expression of CD44 in VSMC. phosphoramidon 50-64 CD44 antigen Mus musculus 143-147 11121595-6 2000 ET-1 reversed the reduction of CD44 expression by phosphoramidon. phosphoramidon 50-64 endothelin 1 Mus musculus 0-4 11121595-6 2000 ET-1 reversed the reduction of CD44 expression by phosphoramidon. phosphoramidon 50-64 CD44 antigen Mus musculus 31-35 11121595-10 2000 ET-1 reversed the suppression of oHA-induced proliferation by phosphoramidon. phosphoramidon 62-76 endothelin 1 Mus musculus 0-4 11016327-9 2000 CONCLUSIONS: In the present study phosphoramidon potentiated the effect of BK in the absence of nitric oxide and prostaglandins in porcine-isolated coronary artery. phosphoramidon 34-48 kininogen 1 Homo sapiens 75-77 10951272-8 2000 Moreover, in the presence of phosphoramidon, a stable inhibitor of neprilysin, we observed an increased efficiency of alpha-melanocyte-stimulating hormone and adrenocorticotropic hormone to stimulate both tyrosinase activity and microphthalmia expression. phosphoramidon 29-43 tyrosinase Homo sapiens 205-215 10894105-11 2000 Neurokinin A contractility in the presence of phosphoramidon indicated that the enhanced contractility following cytokine exposure was not due to a reduction in endogenous neutral endopeptidase activity. phosphoramidon 46-60 tachykinin precursor 1 Homo sapiens 0-12 10720586-9 2000 Finally, systemically administered big ET-1, but not big ET-2, induced a phosphoramidon-sensitive increase in plasma IR-ET. phosphoramidon 73-87 endothelin-1 Oryctolagus cuniculus 39-43 10799294-3 2000 The mucosal activity of ECE-1, characterized by sensitivity to phosphoramidon, was associated with microsomal fraction and showed an elevated (3.1-fold) level in the alcohol diet group. phosphoramidon 63-77 endothelin converting enzyme 1 Rattus norvegicus 24-29 10803579-6 2000 The addition of the NEP enzyme inhibitor phosphoramidon to PC3 and LNCaP-OM1 or the NEP competitive inhibitor CGS 24592 to LNCaP-OM1 blocked the increase in NEP enzyme activity and reversed the DHT-induced growth inhibition. phosphoramidon 41-55 proprotein convertase subtilisin/kexin type 1 Homo sapiens 59-62 10749671-7 2000 The recombinant enzyme exhibited neprilysin-like peptidase activity and was efficiently inhibited by phosphoramidon and thiorphan, two inhibitors of neprilysin. phosphoramidon 101-115 membrane metallo-endopeptidase-like 1 Mus musculus 33-58 10749671-7 2000 The recombinant enzyme exhibited neprilysin-like peptidase activity and was efficiently inhibited by phosphoramidon and thiorphan, two inhibitors of neprilysin. phosphoramidon 101-115 membrane metallo endopeptidase Mus musculus 33-43 10750028-3 2000 Synthesis of ET-2 by ACHN cells was inhibited by phosphoramidon (IC(50( congruent with11 microM). phosphoramidon 49-63 endothelin 2 Homo sapiens 13-17 10749759-10 2000 In addition, L1 cells showed greater ECE-1 activity than L2 cells, and in both, the activity was sensitive to the metalloprotease inhibitor phosphoramidon. phosphoramidon 140-154 endothelin-converting enzyme 1 Ovis aries 37-42 10669592-0 2000 Structure of human neutral endopeptidase (Neprilysin) complexed with phosphoramidon. phosphoramidon 69-83 membrane metalloendopeptidase Homo sapiens 42-52 10669592-4 2000 Here we describe the crystal structure of the extracellular domain (residues 52-749) of human NEP complexed with the generic metalloproteinase inhibitor phosphoramidon at 2.1 A resolution. phosphoramidon 153-167 membrane metalloendopeptidase Homo sapiens 94-97 10704724-5 2000 With the putative ECE inhibitor phosphoramidon (10(-3) M) in the bath a small rightwards shift of the CEC for big ET-1 was observed in control segments and a more marked one in de-endothelialized segments. phosphoramidon 32-46 endothelin converting enzyme 1 Rattus norvegicus 18-21 10672972-5 2000 In other experiments, nitrous oxide antinociception was significantly enhanced by 30-min pretreatment with phosphoramidon, an inhibitor of endopeptidase 24.11, which has been implicated in DYN degradation, but not bestatin or captopril, which inhibit aminopeptidase and angiotensin-converting enzyme, respectively. phosphoramidon 107-121 angiotensin I converting enzyme (peptidyl-dipeptidase A) 1 Mus musculus 270-299 10694217-6 2000 Phosphoramidon (10 microM) also produced an inhibition of the response to big ET-1 that was equivalent to that produced by CGS 26393 (10 microM). phosphoramidon 0-14 endothelin 1 Homo sapiens 78-82 10704724-5 2000 With the putative ECE inhibitor phosphoramidon (10(-3) M) in the bath a small rightwards shift of the CEC for big ET-1 was observed in control segments and a more marked one in de-endothelialized segments. phosphoramidon 32-46 endothelin 1 Rattus norvegicus 114-118 10640916-8 1999 Pretreatment with phosphoramidon, an NEP inhibitor, also enhanced SP- and ET-1-induced bronchoconstriction. phosphoramidon 18-32 endothelin-1 Cavia porcellus 74-78 10542292-8 1999 This activity of SEP was inhibited by phosphoramidon and the neutral endopeptidase 24.11 specific inhibitor thiorphan, but it was only partially inhibited by the endothelin-converting enzyme specific inhibitor FR901533. phosphoramidon 38-52 membrane metallo-endopeptidase-like 1 Mus musculus 17-20 10455291-4 1999 Increases in [Ca2+]i caused by ET-1(1-31), big ET-1 and ET-2(1-31) were completely inhibited by 10(-4)M phosphoramidon, a dual neutral endopeptidase (NEP)/endothelin-converting enzyme (ECE) inhibitor, and 10(-5)M thiorphan, a NEP inhibitor. phosphoramidon 104-118 endothelin 1 Homo sapiens 31-35 10571076-7 1999 The purified enzyme was strongly inhibited by phosphoramidon, and converted big endothelin-1 to endothelin-1. phosphoramidon 46-60 endothelin 1 Homo sapiens 80-92 10571076-7 1999 The purified enzyme was strongly inhibited by phosphoramidon, and converted big endothelin-1 to endothelin-1. phosphoramidon 46-60 endothelin 1 Homo sapiens 96-108 10455291-4 1999 Increases in [Ca2+]i caused by ET-1(1-31), big ET-1 and ET-2(1-31) were completely inhibited by 10(-4)M phosphoramidon, a dual neutral endopeptidase (NEP)/endothelin-converting enzyme (ECE) inhibitor, and 10(-5)M thiorphan, a NEP inhibitor. phosphoramidon 104-118 endothelin 1 Homo sapiens 47-51 10455291-4 1999 Increases in [Ca2+]i caused by ET-1(1-31), big ET-1 and ET-2(1-31) were completely inhibited by 10(-4)M phosphoramidon, a dual neutral endopeptidase (NEP)/endothelin-converting enzyme (ECE) inhibitor, and 10(-5)M thiorphan, a NEP inhibitor. phosphoramidon 104-118 endothelin 2 Homo sapiens 56-60 10455291-4 1999 Increases in [Ca2+]i caused by ET-1(1-31), big ET-1 and ET-2(1-31) were completely inhibited by 10(-4)M phosphoramidon, a dual neutral endopeptidase (NEP)/endothelin-converting enzyme (ECE) inhibitor, and 10(-5)M thiorphan, a NEP inhibitor. phosphoramidon 104-118 membrane metalloendopeptidase Homo sapiens 150-153 10455291-4 1999 Increases in [Ca2+]i caused by ET-1(1-31), big ET-1 and ET-2(1-31) were completely inhibited by 10(-4)M phosphoramidon, a dual neutral endopeptidase (NEP)/endothelin-converting enzyme (ECE) inhibitor, and 10(-5)M thiorphan, a NEP inhibitor. phosphoramidon 104-118 endothelin converting enzyme 1 Homo sapiens 185-188 10455291-4 1999 Increases in [Ca2+]i caused by ET-1(1-31), big ET-1 and ET-2(1-31) were completely inhibited by 10(-4)M phosphoramidon, a dual neutral endopeptidase (NEP)/endothelin-converting enzyme (ECE) inhibitor, and 10(-5)M thiorphan, a NEP inhibitor. phosphoramidon 104-118 membrane metalloendopeptidase Homo sapiens 226-229 10222335-4 1999 ECE-1 and ECE-2 can be differentiated by pH dependence for optimal activity and by sensitivity to phosphoramidon, which shows selectivity for ECE-2 over ECE-1 and PD159790, a novel ECE-1 selective inhibitor. phosphoramidon 98-112 endothelin converting enzyme 1 Homo sapiens 0-5 10215677-9 1999 The peptidase inhibitor phosphoramidon increased in a dose-related manner the plasma steady-state level of hBNP 1.7 +/- 0.4-fold during continuous i.v. phosphoramidon 24-38 natriuretic peptide B Homo sapiens 107-111 10220569-5 1999 This cytokine-stimulated release of ET-1 was inhibited by a series of dual endothelin-converting enzyme (ECE)/neutral endopeptidase inhibitors, phosphoramidon, CGS 26303, and CGS 26393, with an accompanying increase in big ET-1 release but with no effect on expression of mRNA for prepro-ET-1. phosphoramidon 144-158 endothelin 1 Homo sapiens 36-40 10217651-7 1999 Phosphoramidon-sensitive ECE activity and immunodetectable amounts of ECE protein in left ventricular membrane preparations did not differ between NF and DCM hearts. phosphoramidon 0-14 endothelin converting enzyme 1 Homo sapiens 25-28 10352425-4 1999 In the rat proximal tubule, phosphoramidon and thiorphan inhibited NEP activity, with IC50 values of 26.6 +/- 6.0 and 6.9 +/- 1.6 nmol/l, respectively. phosphoramidon 28-42 membrane metallo-endopeptidase Rattus norvegicus 67-70 10401760-2 1999 We, therefore, tested whether inhibition of ET-1-converting enzyme by phosphoramidon (PA) would attenuate rejection in a rat model of chronic cardiac allograft rejection (Lewis [LEW] to F344). phosphoramidon 70-84 endothelin 1 Rattus norvegicus 44-48 10401760-2 1999 We, therefore, tested whether inhibition of ET-1-converting enzyme by phosphoramidon (PA) would attenuate rejection in a rat model of chronic cardiac allograft rejection (Lewis [LEW] to F344). phosphoramidon 86-88 endothelin 1 Rattus norvegicus 44-48 10401760-4 1999 Plasma ET-1 levels in Fisher 344 (F344) recipients were 0.8+/-0.1 pg/ml in water-treated rats and 0.2+/-0.2 pg/ml (P<0.01) in PA-treated rats, demonstrating that the PA treatment protocol effectively lowered ET-1 biosynthesis. phosphoramidon 129-131 endothelin 1 Rattus norvegicus 7-11 10401760-4 1999 Plasma ET-1 levels in Fisher 344 (F344) recipients were 0.8+/-0.1 pg/ml in water-treated rats and 0.2+/-0.2 pg/ml (P<0.01) in PA-treated rats, demonstrating that the PA treatment protocol effectively lowered ET-1 biosynthesis. phosphoramidon 169-171 endothelin 1 Rattus norvegicus 7-11 10401760-6 1999 Inhibition of ET-1 secretion by PA improved allograft survival to 28.8+/-3.3 days (P<0.01, n=8). phosphoramidon 32-34 endothelin 1 Rattus norvegicus 14-18 10352019-5 1999 Northern blot analysis showed that ECE-1 (and not ECE-2) is specifically expressed in Sertoli cells; competitive enzyme immunoassay of ET production showed that Sertoli cell monolayers are capable of cleaving big ET-1, an activity inhibited by the ECE inhibitor phosphoramidon. phosphoramidon 262-276 endothelin converting enzyme 1 Homo sapiens 35-40 10352019-5 1999 Northern blot analysis showed that ECE-1 (and not ECE-2) is specifically expressed in Sertoli cells; competitive enzyme immunoassay of ET production showed that Sertoli cell monolayers are capable of cleaving big ET-1, an activity inhibited by the ECE inhibitor phosphoramidon. phosphoramidon 262-276 endothelin converting enzyme 1 Homo sapiens 35-38 10228105-7 1999 Inhalation of peptidase inhibitors (phosphoramidon plus captopril) potentiated the effect of both hIL-17 and rIL-1beta. phosphoramidon 36-50 interleukin 17A Homo sapiens 98-104 10228105-7 1999 Inhalation of peptidase inhibitors (phosphoramidon plus captopril) potentiated the effect of both hIL-17 and rIL-1beta. phosphoramidon 36-50 interleukin 1 beta Rattus norvegicus 109-118 10228105-8 1999 Inhalation of a neutral endopeptidase inhibitor (phosphoramidon) alone also increased the neutrophil count for hIL-17, whereas an angiotensin-converting enzyme inhibitor (captopril) alone did not. phosphoramidon 49-63 interleukin 17A Homo sapiens 111-117 10222335-4 1999 ECE-1 and ECE-2 can be differentiated by pH dependence for optimal activity and by sensitivity to phosphoramidon, which shows selectivity for ECE-2 over ECE-1 and PD159790, a novel ECE-1 selective inhibitor. phosphoramidon 98-112 endothelin converting enzyme 2 Homo sapiens 10-15 10222335-4 1999 ECE-1 and ECE-2 can be differentiated by pH dependence for optimal activity and by sensitivity to phosphoramidon, which shows selectivity for ECE-2 over ECE-1 and PD159790, a novel ECE-1 selective inhibitor. phosphoramidon 98-112 endothelin converting enzyme 2 Homo sapiens 142-147 10222335-4 1999 ECE-1 and ECE-2 can be differentiated by pH dependence for optimal activity and by sensitivity to phosphoramidon, which shows selectivity for ECE-2 over ECE-1 and PD159790, a novel ECE-1 selective inhibitor. phosphoramidon 98-112 endothelin converting enzyme 1 Homo sapiens 153-158 10222335-4 1999 ECE-1 and ECE-2 can be differentiated by pH dependence for optimal activity and by sensitivity to phosphoramidon, which shows selectivity for ECE-2 over ECE-1 and PD159790, a novel ECE-1 selective inhibitor. phosphoramidon 98-112 endothelin converting enzyme 1 Homo sapiens 153-158 10222335-6 1999 At pH 6.9, conversion of big ET-1 was inhibited markedly by 30 micromol/L PD159790 and by 100 micromol/L phosphoramidon but not by 0.1 micromol/L phosphoramidon. phosphoramidon 105-119 endothelin 1 Homo sapiens 29-33 10222335-7 1999 In contrast, ECE activity was unaffected by 30 micromol/L PD159790 but was inhibited markedly by 0.1 and 100 micromol/L phosphoramidon at pH 5. phosphoramidon 120-134 endothelin converting enzyme 1 Homo sapiens 13-16 10334507-3 1999 The cGMP formation stimulated by ANP in LLC-PK1 cells was significantly decreased by pre-treatment of the peptide with rat renal brush-border membranes, and the inactivation of ANP was inhibited by neutral endopeptidase inhibitors, phosphoramidon and S-thiorphan. phosphoramidon 232-246 natriuretic peptides A Sus scrofa 33-36 10334507-3 1999 The cGMP formation stimulated by ANP in LLC-PK1 cells was significantly decreased by pre-treatment of the peptide with rat renal brush-border membranes, and the inactivation of ANP was inhibited by neutral endopeptidase inhibitors, phosphoramidon and S-thiorphan. phosphoramidon 232-246 natriuretic peptide A Rattus norvegicus 177-180 10334507-5 1999 In addition, phosphoramidon potentiated the natriuresis with a low dose (7.5 pmol min(-1) kg(-1)) of ANP but not of BNP in rats. phosphoramidon 13-27 natriuretic peptide A Rattus norvegicus 101-104 10190051-2 1999 ET-1-immunoreactivity (ET-IR) was detected in the epithelial and smooth muscle layers of tracheal sections from normal guinea pigs and it was enhanced slightly by phosphoramidon (1 microM) treatment. phosphoramidon 163-177 endothelin-1 Cavia porcellus 0-4 9878818-9 1999 Furthermore, morphine, in a dose-dependent manner, increased the hemolymph levels of alpha-MSH and ACTH (1-39) in a naloxone and phosphoramidon antagonizable manner, indicating a neutral endopeptidase (24.11; NEP) mediated cleavage. phosphoramidon 129-143 proopiomelanocortin Homo sapiens 99-103 9888460-5 1999 In vitro stimulation of T47D cell growth by bombesin (BN) was enhanced to 138% of control levels (bombesin alone) by the addition of the selective endopeptidase EC 3.4.24.11 inhibitor phosphoramidon (0.1 ng ml(-1)). phosphoramidon 184-198 gastrin releasing peptide Homo sapiens 44-52 9888460-5 1999 In vitro stimulation of T47D cell growth by bombesin (BN) was enhanced to 138% of control levels (bombesin alone) by the addition of the selective endopeptidase EC 3.4.24.11 inhibitor phosphoramidon (0.1 ng ml(-1)). phosphoramidon 184-198 gastrin releasing peptide Homo sapiens 54-56 9676729-2 1998 First, by amplifying endothelin B receptor numbers through the use of phosphoramidon and intact cell-binding techniques, we demonstrated the presence of these receptors in human umbilical vein endothelial cells (100% endothelin B receptors), human aortic smooth-muscle cells (22% endothelin B, 78% endothelin A receptors), and human bronchial smooth-muscle cells (55% endothelin B, 45% endothelin A receptors) by using [125I]-endothelin-1 radioligand binding. phosphoramidon 70-84 endothelin receptor type B Homo sapiens 21-42 10341317-13 1999 Phosphoramidon and 1,10-phenanthroline dose-dependently inhibited shedding of the IL-4R, even in nonactivated T cells. phosphoramidon 0-14 interleukin 4 receptor Homo sapiens 82-87 9888460-5 1999 In vitro stimulation of T47D cell growth by bombesin (BN) was enhanced to 138% of control levels (bombesin alone) by the addition of the selective endopeptidase EC 3.4.24.11 inhibitor phosphoramidon (0.1 ng ml(-1)). phosphoramidon 184-198 gastrin releasing peptide Homo sapiens 98-106 10070497-7 1998 Naloxone (mu-opioid receptor antagonist) (4.82 +/- 1.02 nmol/mg protein) and phosphoramidon (NEP inhibitor) (4.66 +/- 1.00 nmol/mg protein) inhibited morphine-activated NEP, whereas glibenclamide (ATP-sensitive potassium channel antagonist) and chelerythrine (protein kinase C inhibitor) had no effects. phosphoramidon 77-91 membrane metallo-endopeptidase Rattus norvegicus 93-96 10070497-7 1998 Naloxone (mu-opioid receptor antagonist) (4.82 +/- 1.02 nmol/mg protein) and phosphoramidon (NEP inhibitor) (4.66 +/- 1.00 nmol/mg protein) inhibited morphine-activated NEP, whereas glibenclamide (ATP-sensitive potassium channel antagonist) and chelerythrine (protein kinase C inhibitor) had no effects. phosphoramidon 77-91 membrane metallo-endopeptidase Rattus norvegicus 169-172 9537830-6 1998 The half-life of TNF-alpha induced membrane-associated ICAM-1 on rat astrocytes is approximately 5 h. The proteolytic cleavage process for the conversion of membrane-associated ICAM-1 to sICAM-1 was sensitive to Batimastat (BB94) and phosphoramidon, two inhibitors of metalloproteases, whereas inhibitors of serine-, cysteine-, aspartic-, and chymotrypsin-like proteases had no effect on this process. phosphoramidon 234-248 tumor necrosis factor Rattus norvegicus 17-26 9484239-3 1998 The release of the amyloid precursor protein from both SH-SY5Y and IMR-32 neuronal cells by alpha-secretase was blocked by batimastat and other related synthetic hydroxamic acid-based zinc metalloprotease inhibitors, but not by the structurally unrelated zinc metalloprotease inhibitors enalaprilat and phosphoramidon. phosphoramidon 303-317 amyloid beta precursor protein Homo sapiens 19-44 9515580-6 1998 However phosphoramidon (100 microM), an inhibitor of ECE and NEP, almost abolished specific binding, indicating that both NEP and ECE cleave big ET-1 in the kidney. phosphoramidon 8-22 endothelin converting enzyme 1 Homo sapiens 53-56 9515580-6 1998 However phosphoramidon (100 microM), an inhibitor of ECE and NEP, almost abolished specific binding, indicating that both NEP and ECE cleave big ET-1 in the kidney. phosphoramidon 8-22 membrane metalloendopeptidase Homo sapiens 61-64 9515580-6 1998 However phosphoramidon (100 microM), an inhibitor of ECE and NEP, almost abolished specific binding, indicating that both NEP and ECE cleave big ET-1 in the kidney. phosphoramidon 8-22 membrane metalloendopeptidase Homo sapiens 122-125 9515580-6 1998 However phosphoramidon (100 microM), an inhibitor of ECE and NEP, almost abolished specific binding, indicating that both NEP and ECE cleave big ET-1 in the kidney. phosphoramidon 8-22 endothelin converting enzyme 1 Homo sapiens 130-133 9515580-6 1998 However phosphoramidon (100 microM), an inhibitor of ECE and NEP, almost abolished specific binding, indicating that both NEP and ECE cleave big ET-1 in the kidney. phosphoramidon 8-22 endothelin 1 Homo sapiens 145-149 10374426-12 1998 L-NMA and phosphoramidon obviously reduced the plasma levels of NO and ET-1 to below their respective baseline levels, and showed transient effect of increase on blood pressure. phosphoramidon 10-24 endothelin-1 Oryctolagus cuniculus 71-75 9537830-6 1998 The half-life of TNF-alpha induced membrane-associated ICAM-1 on rat astrocytes is approximately 5 h. The proteolytic cleavage process for the conversion of membrane-associated ICAM-1 to sICAM-1 was sensitive to Batimastat (BB94) and phosphoramidon, two inhibitors of metalloproteases, whereas inhibitors of serine-, cysteine-, aspartic-, and chymotrypsin-like proteases had no effect on this process. phosphoramidon 234-248 intercellular adhesion molecule 1 Rattus norvegicus 55-61 9537830-6 1998 The half-life of TNF-alpha induced membrane-associated ICAM-1 on rat astrocytes is approximately 5 h. The proteolytic cleavage process for the conversion of membrane-associated ICAM-1 to sICAM-1 was sensitive to Batimastat (BB94) and phosphoramidon, two inhibitors of metalloproteases, whereas inhibitors of serine-, cysteine-, aspartic-, and chymotrypsin-like proteases had no effect on this process. phosphoramidon 234-248 intercellular adhesion molecule 1 Rattus norvegicus 177-183 9595400-8 1998 Furthermore, phosphoramidon attenuated human big ET-1-induced contractions only in the umbilical artery and not in the vein. phosphoramidon 13-27 endothelin 1 Homo sapiens 49-53 9543242-4 1998 Phosphoramidon enhanced the contractile response to neurokinin A and substance P, but not to neuropeptide gamma, [Sar9, Met(O2)11]substance P or senktide. phosphoramidon 0-14 tachykinin precursor 1 Homo sapiens 52-64 9543242-4 1998 Phosphoramidon enhanced the contractile response to neurokinin A and substance P, but not to neuropeptide gamma, [Sar9, Met(O2)11]substance P or senktide. phosphoramidon 0-14 tachykinin precursor 1 Homo sapiens 69-80 9533826-7 1998 Pre-treatment with phosphoramidon (1 micron) an ECE-inhibitor, followed by TNF-alpha stimulation, decreased ir-ET-1 levels. phosphoramidon 19-33 endothelin converting enzyme 1 Homo sapiens 48-51 9533826-7 1998 Pre-treatment with phosphoramidon (1 micron) an ECE-inhibitor, followed by TNF-alpha stimulation, decreased ir-ET-1 levels. phosphoramidon 19-33 tumor necrosis factor Homo sapiens 75-84 9533826-7 1998 Pre-treatment with phosphoramidon (1 micron) an ECE-inhibitor, followed by TNF-alpha stimulation, decreased ir-ET-1 levels. phosphoramidon 19-33 endothelin 1 Homo sapiens 111-115 9473154-4 1998 RESULTS: The artery membranes hydrolysed bigET-1 to ET-1 through a partly phosphoramidon-sensitive pathway. phosphoramidon 74-88 endothelin 1 Homo sapiens 44-48 9473154-6 1998 Phosphoramidon decreased pEC50% for bigET-1-evoked contractions (p < 0.05; n = 8), without affecting the response to ET-1. phosphoramidon 0-14 endothelin 1 Homo sapiens 39-43 9595528-5 1998 Membrane ECE activity was phosphoramidon-sensitive, in contrast to the cytosolic activity capable of producing ET-1 from big ET-1. phosphoramidon 26-40 endothelin converting enzyme 1 Homo sapiens 9-12 9595383-7 1998 In contrast, conversion of big ET-3 (10 nM) under the same conditions was not detected in either intact or permeabilized cells after 2 h. Big ET-3 and big ET-1 were converted by a phosphoramidon-sensitive/thiorphan-insensitive enzyme on the surface of confluent cultures of human umbilical vein smooth-muscle cells, with concentrations of the corresponding mature peptides increasing by 99.5 +/- 14.5 pM and 222.2 +/- 11.6 pM, respectively. phosphoramidon 180-194 endothelin 3 Homo sapiens 31-35 9595383-7 1998 In contrast, conversion of big ET-3 (10 nM) under the same conditions was not detected in either intact or permeabilized cells after 2 h. Big ET-3 and big ET-1 were converted by a phosphoramidon-sensitive/thiorphan-insensitive enzyme on the surface of confluent cultures of human umbilical vein smooth-muscle cells, with concentrations of the corresponding mature peptides increasing by 99.5 +/- 14.5 pM and 222.2 +/- 11.6 pM, respectively. phosphoramidon 180-194 endothelin 3 Homo sapiens 142-146 9595383-7 1998 In contrast, conversion of big ET-3 (10 nM) under the same conditions was not detected in either intact or permeabilized cells after 2 h. Big ET-3 and big ET-1 were converted by a phosphoramidon-sensitive/thiorphan-insensitive enzyme on the surface of confluent cultures of human umbilical vein smooth-muscle cells, with concentrations of the corresponding mature peptides increasing by 99.5 +/- 14.5 pM and 222.2 +/- 11.6 pM, respectively. phosphoramidon 180-194 endothelin 1 Homo sapiens 155-159 9595388-6 1998 Phosphoramidon inhibited the wild-type ECE-1 with an IC50 of 1.5 microM, but it was about sixfold weaker for the C412S mutant. phosphoramidon 0-14 endothelin converting enzyme 1 Rattus norvegicus 39-44 9595400-9 1998 Such observations, in terms of substrate selectivity and phosphoramidon sensitivity, suggest the presence of distinct ECE activities in human vein and arteries. phosphoramidon 57-71 endothelin converting enzyme 1 Homo sapiens 118-121 9595402-5 1998 In the presence of phosphoramidon (10(-4) M in segments with an intact endothelium or 5 x 10(-4) M in de-endothelialized segments), there was only a small shift to the right of the concentration-effect curve for big ET-1. phosphoramidon 19-33 endothelin 1 Rattus norvegicus 216-220 9493857-6 1998 Phosphoramidon inhibited the metabolism of NT by LNCaP cells. phosphoramidon 0-14 neurotensin Homo sapiens 43-45 9472729-2 1998 Although both phosphoramidon and thiorphan are metalloprotease inhibitors, the ECE activity is inhibited by phosphoramidon but not by thiorphan, a specific inhibitor of NEP. phosphoramidon 14-28 endothelin converting enzyme 1 Rattus norvegicus 79-82 9472729-2 1998 Although both phosphoramidon and thiorphan are metalloprotease inhibitors, the ECE activity is inhibited by phosphoramidon but not by thiorphan, a specific inhibitor of NEP. phosphoramidon 108-122 endothelin converting enzyme 1 Rattus norvegicus 79-82 9472729-4 1998 Phosphoramidon significantly decreased ET-1 levels, causing a concomitant big ET-1 increase and dose-dependently attenuated indomethacin-induced gastric mucosal damage. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 39-43 9472729-4 1998 Phosphoramidon significantly decreased ET-1 levels, causing a concomitant big ET-1 increase and dose-dependently attenuated indomethacin-induced gastric mucosal damage. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 78-82 9533650-4 1998 Peptidase inhibition by captopril and phosphoramidon increased the relaxant effect and duration of action for original VIP but not for the VIP analog. phosphoramidon 38-52 VIP peptides Cavia porcellus 119-122 9401784-7 1997 Kininases were identified by ramiprilat, phosphoramidon, diprotin A and 2-mercaptoethanol or apstatin as specific inhibitors of ACE, neutral endopeptidase 24.11 (NEP), dipeptidylaminopeptidase IV and aminopeptidase P (APP), respectively. phosphoramidon 41-55 angiotensin I converting enzyme Rattus norvegicus 128-131 9537817-7 1997 Transforming growth factor-beta1 (TGF-beta1) (40 pM) also significantly enhanced the pressor responses to norepinephrine (10(-6) M) and this enhancement was significantly inhibited by phosphoramidon. phosphoramidon 184-198 transforming growth factor, beta 1 Rattus norvegicus 0-32 9537817-7 1997 Transforming growth factor-beta1 (TGF-beta1) (40 pM) also significantly enhanced the pressor responses to norepinephrine (10(-6) M) and this enhancement was significantly inhibited by phosphoramidon. phosphoramidon 184-198 transforming growth factor, beta 1 Rattus norvegicus 34-43 9426079-0 1997 Neutral endopeptidase inhibition with inhaled phosphoramidon: no effect on bronchial responsiveness to adenosine 5"-monophosphate (AMP) in asthma. phosphoramidon 46-60 membrane metalloendopeptidase Homo sapiens 0-21 9426079-3 1997 We have, therefore, investigated the change in bronchial reactivity to adenosine 5"-monophosphate (AMP), after treatment with inhaled phosphoramidon, a potent neutral endopeptidase (NEP) inhibitor, in a double-blind, placebo-controlled, randomized study of 12 asthmatic subjects. phosphoramidon 134-148 membrane metalloendopeptidase Homo sapiens 182-185 9375329-6 1997 Constriction was not affected by removing extracellular Ca2+ but was abolished after treatment with ryanodine to deplete intracellular Ca2+ stores, with the endothelin-1 synthesis inhibitor phosphoramidon, with the endothelin A-receptor antagonist BQ-123, with the protein kinase C inhibitor staurosporine, or with glutaraldehyde to reduce endothelial cell deformability. phosphoramidon 190-204 endothelin 1 Homo sapiens 157-169 9422810-18 1997 Big ET-1 was also unaffected by thiorphan but antagonized in a concentration-dependent manner by phosphoramidon (10(-5) M and 10(-4) M). phosphoramidon 97-111 endothelin 1 Homo sapiens 4-8 9422810-23 1997 To conclude we have demonstrated the presence of a phosphoramidon-sensitive ECE on the smooth muscle layer of the human umbilical vein which can convert big ET-1, big ET-2(1-37), big ET-2(1-38) and big ET-3 to their mature biologically active forms. phosphoramidon 51-65 endothelin converting enzyme 1 Homo sapiens 76-79 9422810-23 1997 To conclude we have demonstrated the presence of a phosphoramidon-sensitive ECE on the smooth muscle layer of the human umbilical vein which can convert big ET-1, big ET-2(1-37), big ET-2(1-38) and big ET-3 to their mature biologically active forms. phosphoramidon 51-65 endothelin 1 Homo sapiens 157-161 9422810-23 1997 To conclude we have demonstrated the presence of a phosphoramidon-sensitive ECE on the smooth muscle layer of the human umbilical vein which can convert big ET-1, big ET-2(1-37), big ET-2(1-38) and big ET-3 to their mature biologically active forms. phosphoramidon 51-65 endothelin 2 Homo sapiens 167-171 9422810-23 1997 To conclude we have demonstrated the presence of a phosphoramidon-sensitive ECE on the smooth muscle layer of the human umbilical vein which can convert big ET-1, big ET-2(1-37), big ET-2(1-38) and big ET-3 to their mature biologically active forms. phosphoramidon 51-65 endothelin 2 Homo sapiens 183-187 9422810-23 1997 To conclude we have demonstrated the presence of a phosphoramidon-sensitive ECE on the smooth muscle layer of the human umbilical vein which can convert big ET-1, big ET-2(1-37), big ET-2(1-38) and big ET-3 to their mature biologically active forms. phosphoramidon 51-65 endothelin 3 Homo sapiens 202-206 9401774-17 1997 However, when angiotensin-converting enzyme and neutral endopeptidase were inhibited by perindoprilat (10 microM) and phosphoramidon (1 microM), respectively, bradykinin (1 microM) significantly inhibited the S-I efflux in epithelium-intact preparations as well as in epithelium-denuded preparations. phosphoramidon 118-132 angiotensin I converting enzyme Rattus norvegicus 14-43 9401784-7 1997 Kininases were identified by ramiprilat, phosphoramidon, diprotin A and 2-mercaptoethanol or apstatin as specific inhibitors of ACE, neutral endopeptidase 24.11 (NEP), dipeptidylaminopeptidase IV and aminopeptidase P (APP), respectively. phosphoramidon 41-55 membrane metallo-endopeptidase Rattus norvegicus 133-160 9357856-8 1997 ANP, BNP, and CNP (10(-9) to 10(-5) M) + phosphoramidon (10(-6) M) caused a concentration-dependent elevation in cGMP with an order of potency ANP > BNP > CNP. phosphoramidon 41-55 2',3'-cyclic nucleotide 3' phosphodiesterase Homo sapiens 14-17 9357856-8 1997 ANP, BNP, and CNP (10(-9) to 10(-5) M) + phosphoramidon (10(-6) M) caused a concentration-dependent elevation in cGMP with an order of potency ANP > BNP > CNP. phosphoramidon 41-55 natriuretic peptide B Homo sapiens 152-155 9357856-8 1997 ANP, BNP, and CNP (10(-9) to 10(-5) M) + phosphoramidon (10(-6) M) caused a concentration-dependent elevation in cGMP with an order of potency ANP > BNP > CNP. phosphoramidon 41-55 2',3'-cyclic nucleotide 3' phosphodiesterase Homo sapiens 161-164 9085052-4 1997 Big-endothelin-1, but not endothelin-1 actions were inhibited by phosphoramidon. phosphoramidon 65-79 endothelin 1 Rattus norvegicus 4-16 9196090-6 1997 We found that among ETs, only ET-1 was steadily released under basal conditions over 24 h. The basal production was attenuated by both phosphoramidon and CGS 26 303, dual NEP and ECE inhibitors. phosphoramidon 135-149 endothelin 1 Homo sapiens 30-34 9196090-10 1997 These data suggest that ET-1 is simultaneously produced and degraded by guinea-pig tracheal epithelial cells via phosphoramidon-sensitive ECE and NEP pathways, respectively. phosphoramidon 113-127 endothelin 1 Homo sapiens 24-28 9196090-10 1997 These data suggest that ET-1 is simultaneously produced and degraded by guinea-pig tracheal epithelial cells via phosphoramidon-sensitive ECE and NEP pathways, respectively. phosphoramidon 113-127 membrane metalloendopeptidase Homo sapiens 146-149 9085052-8 1997 These results indicate that the pharmacological responses to big-endothelin-1 in aortic endothelial cells are due to the extracellular phosphoramidon-sensitive conversion to endothelin-1. phosphoramidon 135-149 endothelin 1 Rattus norvegicus 65-77 9085052-8 1997 These results indicate that the pharmacological responses to big-endothelin-1 in aortic endothelial cells are due to the extracellular phosphoramidon-sensitive conversion to endothelin-1. phosphoramidon 135-149 endothelin 1 Rattus norvegicus 174-186 9227507-11 1997 Removal of endogenous ET-1 with either phosphoramidon or BQ-123 significantly augments cytokine-stimulated NO. phosphoramidon 39-53 endothelin 1 Rattus norvegicus 22-26 9227507-13 1997 To further test the effect of ET-1 on iNOS, we treated cells with phosphoramidon to inhibit endogenous ET-1 synthesis and then administered ET-1 (10(-9) to 10(-7) M). phosphoramidon 66-80 endothelin 1 Rattus norvegicus 103-107 9227507-13 1997 To further test the effect of ET-1 on iNOS, we treated cells with phosphoramidon to inhibit endogenous ET-1 synthesis and then administered ET-1 (10(-9) to 10(-7) M). phosphoramidon 66-80 endothelin 1 Rattus norvegicus 103-107 9094756-5 1997 Through a partly phosphoramidon-sensitive enzymatic activity, endothelin-1 (ET-1) was formed independently of bigET1-31. phosphoramidon 17-31 endothelin 1 Homo sapiens 62-74 9108624-3 1997 Inhibition of NEP by phosphoramidon (10 mg/kg, i.v.) phosphoramidon 21-35 membrane metallo-endopeptidase Rattus norvegicus 14-17 9051300-2 1997 An obligatory step in the biosynthesis of endothelin-1 (ET-1) is the conversion of its inactive precursor, big ET-1, into the mature form by the action of specific, phosphoramidon-sensitive, endothelin converting enzyme(s) (ECE). phosphoramidon 165-179 endothelin 1 Rattus norvegicus 42-54 9051300-2 1997 An obligatory step in the biosynthesis of endothelin-1 (ET-1) is the conversion of its inactive precursor, big ET-1, into the mature form by the action of specific, phosphoramidon-sensitive, endothelin converting enzyme(s) (ECE). phosphoramidon 165-179 endothelin 1 Rattus norvegicus 56-60 9051300-2 1997 An obligatory step in the biosynthesis of endothelin-1 (ET-1) is the conversion of its inactive precursor, big ET-1, into the mature form by the action of specific, phosphoramidon-sensitive, endothelin converting enzyme(s) (ECE). phosphoramidon 165-179 endothelin 1 Rattus norvegicus 111-115 9051300-2 1997 An obligatory step in the biosynthesis of endothelin-1 (ET-1) is the conversion of its inactive precursor, big ET-1, into the mature form by the action of specific, phosphoramidon-sensitive, endothelin converting enzyme(s) (ECE). phosphoramidon 165-179 endothelin converting enzyme 1 Rattus norvegicus 191-222 9051300-2 1997 An obligatory step in the biosynthesis of endothelin-1 (ET-1) is the conversion of its inactive precursor, big ET-1, into the mature form by the action of specific, phosphoramidon-sensitive, endothelin converting enzyme(s) (ECE). phosphoramidon 165-179 endothelin converting enzyme 1 Rattus norvegicus 224-227 9051300-6 1997 In renal cortical slices incubated with big ET-1, pretreatment with phosphoramidon (an ECE inhibitor) reduced tissue immunoreactive ET-1 to a level similar to that of cortical tissue not exposed to big ET-1. phosphoramidon 68-82 endothelin 1 Rattus norvegicus 44-48 9051300-6 1997 In renal cortical slices incubated with big ET-1, pretreatment with phosphoramidon (an ECE inhibitor) reduced tissue immunoreactive ET-1 to a level similar to that of cortical tissue not exposed to big ET-1. phosphoramidon 68-82 endothelin converting enzyme 1 Rattus norvegicus 87-90 9051300-6 1997 In renal cortical slices incubated with big ET-1, pretreatment with phosphoramidon (an ECE inhibitor) reduced tissue immunoreactive ET-1 to a level similar to that of cortical tissue not exposed to big ET-1. phosphoramidon 68-82 endothelin 1 Rattus norvegicus 132-136 9051300-6 1997 In renal cortical slices incubated with big ET-1, pretreatment with phosphoramidon (an ECE inhibitor) reduced tissue immunoreactive ET-1 to a level similar to that of cortical tissue not exposed to big ET-1. phosphoramidon 68-82 endothelin 1 Rattus norvegicus 132-136 9051300-7 1997 This confirms the presence and effectiveness of ECE inhibition by phosphoramidon. phosphoramidon 66-80 endothelin converting enzyme 1 Rattus norvegicus 48-51 9110381-3 1997 Treatment of Clara cells with 1 mM phosphoramidon strongly suppressed (80%) the conversion of big-ET-1 to ET-1 during 1, 2 and 6 h incubation periods. phosphoramidon 35-49 endothelin 1 Homo sapiens 98-102 9110381-3 1997 Treatment of Clara cells with 1 mM phosphoramidon strongly suppressed (80%) the conversion of big-ET-1 to ET-1 during 1, 2 and 6 h incubation periods. phosphoramidon 35-49 endothelin 1 Homo sapiens 106-110 9110381-6 1997 Phosphoramidon and thiorphan (1 mM) reduced the amount of ir-ET generated from exogenous human big-ET-2 (10(-8) M) by 69 and 56%, respectively. phosphoramidon 0-14 endothelin 2 Homo sapiens 99-103 9094756-5 1997 Through a partly phosphoramidon-sensitive enzymatic activity, endothelin-1 (ET-1) was formed independently of bigET1-31. phosphoramidon 17-31 endothelin 1 Homo sapiens 76-80 9117086-16 1997 Degradation of [3H]-BK was not influenced by ramiprilat, but was inhibited by 85% in the presence of phosphoramidon. phosphoramidon 101-115 kininogen 1 Bos taurus 20-22 9015192-5 1997 Finally, we found that thymopentin and to a lesser extent phosphoramidon, a specific endopeptidase 24.11 inhibitor, induced up-regulation of CD4 and CD8 molecules at the thymocyte cell surface. phosphoramidon 58-72 CD4 molecule Homo sapiens 141-144 9015192-5 1997 Finally, we found that thymopentin and to a lesser extent phosphoramidon, a specific endopeptidase 24.11 inhibitor, induced up-regulation of CD4 and CD8 molecules at the thymocyte cell surface. phosphoramidon 58-72 CD8a molecule Homo sapiens 149-152 9117086-17 1997 Phosporamidon markedly inhibited the generation of [1-7]- and [1-5]-BK and nearly abolished the formation of [1-3]- and [2-3]-BK. phosphoramidon 0-13 kininogen 1 Bos taurus 68-70 9117086-17 1997 Phosporamidon markedly inhibited the generation of [1-7]- and [1-5]-BK and nearly abolished the formation of [1-3]- and [2-3]-BK. phosphoramidon 0-13 kininogen 1 Bos taurus 126-128 9296343-7 1997 These results indicate that phosphoramidon-sensitive endothelin converting enzyme activity is highly present in stomach and phosphoramidon, by inhibiting the conversion of big endothelin-1 to endothelin-1 attenuated the gastric mucosal damage in this model. phosphoramidon 28-42 endothelin 1 Rattus norvegicus 176-188 9296343-7 1997 These results indicate that phosphoramidon-sensitive endothelin converting enzyme activity is highly present in stomach and phosphoramidon, by inhibiting the conversion of big endothelin-1 to endothelin-1 attenuated the gastric mucosal damage in this model. phosphoramidon 28-42 endothelin 1 Rattus norvegicus 192-204 9296343-7 1997 These results indicate that phosphoramidon-sensitive endothelin converting enzyme activity is highly present in stomach and phosphoramidon, by inhibiting the conversion of big endothelin-1 to endothelin-1 attenuated the gastric mucosal damage in this model. phosphoramidon 124-138 endothelin 1 Rattus norvegicus 176-188 9296343-7 1997 These results indicate that phosphoramidon-sensitive endothelin converting enzyme activity is highly present in stomach and phosphoramidon, by inhibiting the conversion of big endothelin-1 to endothelin-1 attenuated the gastric mucosal damage in this model. phosphoramidon 124-138 endothelin 1 Rattus norvegicus 192-204 9126883-6 1997 Pre-incubation of tissue with a metalloprotease ECE inhibitor phosphoramidon (10 microM) strongly inhibited the response to big ET-1, but not to ET-1. phosphoramidon 62-76 endothelin converting enzyme 1 Rattus norvegicus 48-51 9396049-3 1997 This increased NEP-like activity is blocked by phosphoramidon, a potent inhibitor of mammalian NEP. phosphoramidon 47-61 membrane metalloendopeptidase Homo sapiens 15-18 9396049-3 1997 This increased NEP-like activity is blocked by phosphoramidon, a potent inhibitor of mammalian NEP. phosphoramidon 47-61 membrane metalloendopeptidase Homo sapiens 95-98 9018495-8 1996 In addition, unlike the transient vasodilator response to ductus arteriosus compression in control studies, ET-1 blockade with BQ-123 or phosphoramidon prolonged the increase in flow caused by ductus arteriosus compression. phosphoramidon 137-151 EDN1 Ovis aries 108-112 8901663-5 1996 In CHF patients (n = 10), phosphoramidon (a combined ECE and neutral endopeptidase inhibitor) and BQ-123 (an ETA receptor antagonist) increased FBF by 52 +/- 10% (P = .0006) and 31 +/- 6% (P = .002), respectively, and thiorphan (a selective neutral endopeptidase inhibitor) reduced FBF by 15 +/- 5% (P = .0007). phosphoramidon 26-40 endothelin converting enzyme 1 Homo sapiens 53-56 8841832-13 1996 SR 140333, SR 48968, and SR 142801 blocked the enhancement by phosphoramidon of the response to SP, NKA, and NKB, respectively. phosphoramidon 62-76 tachykinin 1 Mus musculus 96-98 8815887-8 1996 Using a metabolically stable analog of SP, SP (5-11), or an endopeptidase inhibitor, phosphoramidon, we were able to demonstrate that CGRP enhances the SP effect by inhibiting an SP endopeptidase. phosphoramidon 85-99 calcitonin related polypeptide alpha Homo sapiens 134-138 8818353-16 1996 Pretreatment with NEP inhibitors, SCH 39370 or phosphoramidon, slowed the loss of cFP-AAY-pAB from the plasma, but did not prevent inhibition of ACE. phosphoramidon 47-61 neprilysin Oryctolagus cuniculus 18-21 8994440-6 1997 The size of the neointima was effectively reduced by phosphoramidon, an inhibitor of neutral metalloproteases, including ECE-1. phosphoramidon 53-67 endothelin converting enzyme 1 Homo sapiens 121-126 8912717-8 1996 The increase was preceded by an increase in uPA-R- and uPA-specific mRNA, which was not observed when the proteinase inhibitor phosphoramidon was added together with dispase. phosphoramidon 127-141 plasminogen activator, urokinase Homo sapiens 44-47 8912717-8 1996 The increase was preceded by an increase in uPA-R- and uPA-specific mRNA, which was not observed when the proteinase inhibitor phosphoramidon was added together with dispase. phosphoramidon 127-141 plasminogen activator, urokinase Homo sapiens 55-58 8933767-8 1996 Decreasing ET-1 levels by inhibiting endothelin-converting enzyme with phosphoramidon normalized retinal blood flow in diabetic rats. phosphoramidon 71-85 endothelin 1 Rattus norvegicus 11-15 8938666-3 1996 The metalloprotease inhibitor phosphoramidon (30 mumol/l) almost abolished the contractile response to big ET-1, whereas the ET-1-induced contraction was unaffected. phosphoramidon 30-44 endothelin-1 Oryctolagus cuniculus 107-111 8938666-9 1996 These results suggest that externally applied big ET-1 is converted to ET-1 by a phosphoramidon-sensitive "endothelin converting enzyme" present in the vascular smooth muscle cells. phosphoramidon 81-95 endothelin-1 Oryctolagus cuniculus 50-54 8938666-9 1996 These results suggest that externally applied big ET-1 is converted to ET-1 by a phosphoramidon-sensitive "endothelin converting enzyme" present in the vascular smooth muscle cells. phosphoramidon 81-95 endothelin-1 Oryctolagus cuniculus 71-75 8938667-3 1996 This latter effect was increased in rat paws by captopril, an inhibitor of angiotensin-converting enzyme (ACE), administered locally in combination with diprotin A, an inhibitor of an dipeptidyl(amino)peptidase IV (DAP IV) or phosphoramidon, an inhibitor of neutral endopeptidase (NEP). phosphoramidon 226-240 angiotensin I converting enzyme Rattus norvegicus 106-109 8916270-1 1996 The mechanism(s) of degradation of the potent vasoconstrictor endothelin-1 (ET-1) by rat vascular smooth muscle A-10 cells, which possess the ETA receptor subtype, was investigated by incubating [125I]ET-1 (0.1 nM) with cells for 0-4 h at 37 degrees C in the presence and absence of lysosomal enzyme inhibitors, NH4Cl and chloroquine, and a neutral endopeptidase inhibitor, phosphoramidon. phosphoramidon 374-388 endothelin 1 Rattus norvegicus 62-74 8916270-1 1996 The mechanism(s) of degradation of the potent vasoconstrictor endothelin-1 (ET-1) by rat vascular smooth muscle A-10 cells, which possess the ETA receptor subtype, was investigated by incubating [125I]ET-1 (0.1 nM) with cells for 0-4 h at 37 degrees C in the presence and absence of lysosomal enzyme inhibitors, NH4Cl and chloroquine, and a neutral endopeptidase inhibitor, phosphoramidon. phosphoramidon 374-388 endothelin 1 Rattus norvegicus 76-80 9232670-3 1996 Inhibition of NEP with phosphoramidon caused cough, which was inhibited by systemic capsaicin treatment and by aerosols of a specific NK1 receptor antagonist FK 888. phosphoramidon 23-37 membrane metalloendopeptidase Homo sapiens 14-17 9232670-3 1996 Inhibition of NEP with phosphoramidon caused cough, which was inhibited by systemic capsaicin treatment and by aerosols of a specific NK1 receptor antagonist FK 888. phosphoramidon 23-37 tachykinin receptor 1 Homo sapiens 134-146 9232670-5 1996 The number of coughs induced by histamine aerosols was inhibited by systemic capsaicin treatment and enhanced by pretreatment with a NEP inhibitor phosphoramidon. phosphoramidon 147-161 membrane metalloendopeptidase Homo sapiens 133-136 8841832-13 1996 SR 140333, SR 48968, and SR 142801 blocked the enhancement by phosphoramidon of the response to SP, NKA, and NKB, respectively. phosphoramidon 62-76 tachykinin 1 Mus musculus 100-103 8687431-4 1996 EDTA, phosphoramidon and thiorphan inhibit the proteolysis of PAMP by NEP. phosphoramidon 6-20 adrenomedullin Homo sapiens 62-66 8889700-4 1996 Degradation of bradykinin was strongly inhibited by phosphoramidon and thiorphan, which are specific inhibitors of neutral metalloendopeptidase-24.11. phosphoramidon 52-66 thimet oligopeptidase 1 Rattus norvegicus 123-143 8687431-4 1996 EDTA, phosphoramidon and thiorphan inhibit the proteolysis of PAMP by NEP. phosphoramidon 6-20 membrane metalloendopeptidase Homo sapiens 70-73 8670289-5 1996 Endothelin converting enzyme is characteristically inhibited by phosphoramidon and other metalloproteinase inhibitors including EDTA, o-phenanthroline, and diethylpyrocarbonate, but not by inhibitors of other classes of proteases or thiorphan. phosphoramidon 64-78 endothelin 1 Homo sapiens 0-10 8670289-6 1996 The inhibition by phosphoramidon is competitive with big porcine endothelin-1 suggestive of a common binding site for substrate and inhibitor. phosphoramidon 18-32 endothelin 1 Homo sapiens 65-77 8828809-2 1996 The specific ECE activity was demonstrated by a phosphoramidon dose-dependent decrease in ET-1 level with a concomitant increase in big ET-1 level. phosphoramidon 48-62 endothelin converting enzyme 1 Homo sapiens 13-16 8828809-3 1996 By using a specific neutral endopeptidase 24.11 (NEP 24.11) inhibitor, thiorphan, it was also shown that the phosphoramidon-sensitive ET-1 degrading activity in this cell line is due to the NEP 24.11 activity. phosphoramidon 109-123 membrane metalloendopeptidase Homo sapiens 20-47 8828809-3 1996 By using a specific neutral endopeptidase 24.11 (NEP 24.11) inhibitor, thiorphan, it was also shown that the phosphoramidon-sensitive ET-1 degrading activity in this cell line is due to the NEP 24.11 activity. phosphoramidon 109-123 membrane metalloendopeptidase Homo sapiens 49-58 8828809-3 1996 By using a specific neutral endopeptidase 24.11 (NEP 24.11) inhibitor, thiorphan, it was also shown that the phosphoramidon-sensitive ET-1 degrading activity in this cell line is due to the NEP 24.11 activity. phosphoramidon 109-123 membrane metalloendopeptidase Homo sapiens 190-199 8793593-7 1996 Furthermore, use of the specific neutral endopeptidase inhibitor, phosphoramidon, significantly increased the efficacy of alpha-MSH in inhibiting CPB-induced immunocyte activation. phosphoramidon 66-80 proopiomelanocortin Homo sapiens 122-131 8636398-4 1996 Coincubation with UK73967 or phosphoramidon, inhibitors of NEP, potentiated all of the effects of ANP and BNP on the neutrophil functions, and the NEP inhibitors protected degradation of ANP and BNP by the neutrophils. phosphoramidon 29-43 membrane metalloendopeptidase Homo sapiens 59-62 8636398-4 1996 Coincubation with UK73967 or phosphoramidon, inhibitors of NEP, potentiated all of the effects of ANP and BNP on the neutrophil functions, and the NEP inhibitors protected degradation of ANP and BNP by the neutrophils. phosphoramidon 29-43 natriuretic peptide A Homo sapiens 98-101 8636398-4 1996 Coincubation with UK73967 or phosphoramidon, inhibitors of NEP, potentiated all of the effects of ANP and BNP on the neutrophil functions, and the NEP inhibitors protected degradation of ANP and BNP by the neutrophils. phosphoramidon 29-43 natriuretic peptide B Homo sapiens 106-109 8636398-4 1996 Coincubation with UK73967 or phosphoramidon, inhibitors of NEP, potentiated all of the effects of ANP and BNP on the neutrophil functions, and the NEP inhibitors protected degradation of ANP and BNP by the neutrophils. phosphoramidon 29-43 natriuretic peptide A Homo sapiens 187-190 8636398-4 1996 Coincubation with UK73967 or phosphoramidon, inhibitors of NEP, potentiated all of the effects of ANP and BNP on the neutrophil functions, and the NEP inhibitors protected degradation of ANP and BNP by the neutrophils. phosphoramidon 29-43 natriuretic peptide B Homo sapiens 195-198 8796300-5 1996 Addition of phosphoramidon and thiorphan, which are specific inhibitors of neutral metalloendopeptidase 3.4.24.11 (NEP), strongly inhibited the degradation of bradykinin. phosphoramidon 12-26 membrane metallo-endopeptidase Rattus norvegicus 115-118 8600940-0 1996 Guinea pig Clara cells secrete endothelin 1 through a phosphoramidon-sensitive pathway. phosphoramidon 54-68 endothelin-1 Cavia porcellus 31-43 7490515-9 1995 Phosphoramidon (4 mg/kg, iv) pretreatment attenuated the increase in MAP and TPR induced by proET-1. phosphoramidon 0-14 translocated promoter region, nuclear basket protein Rattus norvegicus 77-80 8834339-11 1996 Inhibition of SP destruction by phosphoramidon (10(-6) M) also eliminated the transient rise in CBF. phosphoramidon 32-46 tachykinin precursor 1 Homo sapiens 14-16 8992314-3 1996 The endopeptidase resembled mammalian neprilysin (NEP, endopeptidase 24.11) in that the enzyme activity was inhibited by phosphoramidon and thiorphan and that it cleaved AF1 on the amino side of phenylalanine. phosphoramidon 121-135 membrane metalloendopeptidase Homo sapiens 38-48 8992314-3 1996 The endopeptidase resembled mammalian neprilysin (NEP, endopeptidase 24.11) in that the enzyme activity was inhibited by phosphoramidon and thiorphan and that it cleaved AF1 on the amino side of phenylalanine. phosphoramidon 121-135 membrane metalloendopeptidase Homo sapiens 50-53 7490515-14 1995 In phosphoramidon-treated rats, DCLHb increased MAP (99%), HR (25%), cardiac output (37%), and TPR (60%). phosphoramidon 3-17 translocated promoter region, nuclear basket protein Rattus norvegicus 95-98 7490515-17 1995 It is concluded that proET-1 increases blood flow to various organs and that phosphoramidon, an ECE inhibitor, could block the proET-1-induced increases in regional blood flow. phosphoramidon 77-91 endothelin converting enzyme 1 Rattus norvegicus 96-99 7561524-1 1995 Neutrophil responses to alpha-N-formyl-L-Met-L-Leu-L-Phe (fMLF) are modulated by inhibitors of surface membrane neutral endopeptidase (NEP), such as phosphoramidon (PPAD). phosphoramidon 149-163 membrane metalloendopeptidase Homo sapiens 135-138 7595577-6 1995 Phosphoramidon, an inhibitor of neutral endopeptidase 24.11, decreased Met-enkephalin degradation in caudate-putamen (14%) but had no effect on that in frontal cortex. phosphoramidon 0-14 membrane metallo-endopeptidase Rattus norvegicus 32-59 8559593-3 1995 Phosphoramidon, thiorphan and SQ 28603, potent inhibitors of mammalian neprilysin (neutral endopeptidase, endopeptidase 24.11), inhibited the endopeptidase activity towards AKH-I with IC50 values of 0.13 microM, 22 microM and 6.3 microM, respectively. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 71-81 8587664-4 1995 In approximately half of the preparations, the peptidase inhibitors, phosphoramidon (1 microM) and bestatin (100 microM), caused a marked and well-maintained contraction (approximately 20% of neurokinin A maximum), which may indicate a role for endogenous tachykinins in the regulation of tone in this preparation. phosphoramidon 69-83 tachykinin precursor 1 Homo sapiens 192-204 7561524-1 1995 Neutrophil responses to alpha-N-formyl-L-Met-L-Leu-L-Phe (fMLF) are modulated by inhibitors of surface membrane neutral endopeptidase (NEP), such as phosphoramidon (PPAD). phosphoramidon 165-169 membrane metalloendopeptidase Homo sapiens 135-138 8523455-10 1995 In the presence of the ET-1 converting enzyme inhibitor, phosphoramidon (1.7 mumol/l), ischaemia-induced increases of ET-1 secretion were attenuated, and this was accompanied by a time-dependent rise in coronary perfusion pressure up to 60% (P < 0.05). phosphoramidon 57-71 endothelin 1 Rattus norvegicus 23-27 8548322-6 1995 Besides, phosphoramidon per se markedly stimulated the expression of ET-1 mRNA. phosphoramidon 9-23 endothelin 1 Rattus norvegicus 69-73 8528566-14 1995 However, IR CTF was still detected, suggesting that either some conversion by phosphoramidon-insensitive enzyme(s) was occurring, and/or that CTF was being protected from further degradation by phosphoramidon.5. phosphoramidon 194-208 nuclear factor I C Homo sapiens 142-145 8523455-10 1995 In the presence of the ET-1 converting enzyme inhibitor, phosphoramidon (1.7 mumol/l), ischaemia-induced increases of ET-1 secretion were attenuated, and this was accompanied by a time-dependent rise in coronary perfusion pressure up to 60% (P < 0.05). phosphoramidon 57-71 endothelin 1 Rattus norvegicus 118-122 8538872-6 1995 Phosphoramidon (5 x 10(-6) M) potentiated the relaxant responses of epithelium-intact GPT to both PACAP and VIP but did not affect the responses of epithelium-denuded GPT. phosphoramidon 0-14 VIP peptides Cavia porcellus 108-111 7473528-5 1995 Vasoconstriction to big endothelin-1 was abolished by co-infusion of phosphoramidon, whereas vasoconstriction to endothelin-1 was unaffected. phosphoramidon 69-83 endothelin 1 Homo sapiens 24-36 7592194-5 1995 Both phosphoramidon (NEP inhibitor) and captopril (ACE inhibitor) potentiated the increase in airway blood flow produced by SP in pathogen-free rats. phosphoramidon 5-19 membrane metallo-endopeptidase Rattus norvegicus 21-24 8528566-0 1995 Phosphoramidon inhibition of the in vivo conversion of big endothelin-1 to endothelin-1 in the human forearm. phosphoramidon 0-14 endothelin 1 Homo sapiens 59-71 8528566-0 1995 Phosphoramidon inhibition of the in vivo conversion of big endothelin-1 to endothelin-1 in the human forearm. phosphoramidon 0-14 endothelin 1 Homo sapiens 75-87 8528566-2 1995 The vasoconstrictor peptide, endothelin-1 (ET-1) and a biologically inactive C-terminal fragment (CTF) are generated from an intermediate big ET-1 by a putative ET converting enzyme, sensitive to phosphoramidon. phosphoramidon 196-210 endothelin 1 Homo sapiens 29-41 8528566-2 1995 The vasoconstrictor peptide, endothelin-1 (ET-1) and a biologically inactive C-terminal fragment (CTF) are generated from an intermediate big ET-1 by a putative ET converting enzyme, sensitive to phosphoramidon. phosphoramidon 196-210 endothelin 1 Homo sapiens 43-47 8528566-2 1995 The vasoconstrictor peptide, endothelin-1 (ET-1) and a biologically inactive C-terminal fragment (CTF) are generated from an intermediate big ET-1 by a putative ET converting enzyme, sensitive to phosphoramidon. phosphoramidon 196-210 nuclear factor I C Homo sapiens 77-96 8528566-2 1995 The vasoconstrictor peptide, endothelin-1 (ET-1) and a biologically inactive C-terminal fragment (CTF) are generated from an intermediate big ET-1 by a putative ET converting enzyme, sensitive to phosphoramidon. phosphoramidon 196-210 nuclear factor I C Homo sapiens 98-101 8528566-2 1995 The vasoconstrictor peptide, endothelin-1 (ET-1) and a biologically inactive C-terminal fragment (CTF) are generated from an intermediate big ET-1 by a putative ET converting enzyme, sensitive to phosphoramidon. phosphoramidon 196-210 endothelin 1 Homo sapiens 142-146 8528566-13 1995 When phosphoramidon was co-infused with big ET-1, both the rise in IR ET and associated vasoconstriction were abolished. phosphoramidon 5-19 endothelin 1 Homo sapiens 44-48 7797512-7 1995 ECE-2 resembles ECE-1 in that it is inhibited in vitro by phosphoramidon and FR901533 but not by thiorphan or captopril, and it converts big ET-1 more efficiently than big ET-2 or big ET-3. phosphoramidon 58-72 EEF1A lysine methyltransferase 4 Cricetulus griseus 0-5 7797512-7 1995 ECE-2 resembles ECE-1 in that it is inhibited in vitro by phosphoramidon and FR901533 but not by thiorphan or captopril, and it converts big ET-1 more efficiently than big ET-2 or big ET-3. phosphoramidon 58-72 endothelin-converting enzyme 1 Cricetulus griseus 16-21 7797512-9 1995 (i) The sensitivity of ECE-2 to phosphoramidon is 250-fold higher as compared with ECE-1, while FR901533 inhibits both enzymes at similar concentrations. phosphoramidon 32-46 EEF1A lysine methyltransferase 4 Cricetulus griseus 23-28 7597662-0 1995 Effect of an inhaled neutral endopeptidase inhibitor, phosphoramidon, on baseline airway calibre and bronchial responsiveness to bradykinin in asthma. phosphoramidon 54-68 membrane metalloendopeptidase Homo sapiens 21-42 7599928-0 1995 Differential effects of phosphoramidon on contractile responses to angiotensin II in rat blood vessels. phosphoramidon 24-38 angiotensinogen Rattus norvegicus 67-81 7599928-6 1995 Phosphoramidon blocked the responses to AII in a concentration-dependent manner, whereas even very high concentrations of phosphoramidon (100 microM) failed to affect the tension responses evoked by ET-1 and AVP in all three preparations. phosphoramidon 0-14 angiotensinogen Rattus norvegicus 40-43 7599928-7 1995 Low concentrations of phosphoramidon (10 microM) produced significant increases in EC50 values for AII in tail artery (P < 0.01) and mesenteric artery (P < 0.05) but not in aorta. phosphoramidon 22-36 angiotensinogen Rattus norvegicus 99-102 7599928-9 1995 Phosphoramidon-evoked rightward shifts in the C-R curves to AII were much higher than those to big ET-1 in both mesenteric artery and tail artery. phosphoramidon 0-14 angiotensinogen Rattus norvegicus 60-63 7599928-14 1995 It is concluded that the vasoconstrictor responses to AII in mesenteric artery and tail artery may be mediated by the release of endothelins from the endothelium by increased formation from big ET, an effect that is blocked by phosphoramidon. phosphoramidon 227-241 angiotensinogen Rattus norvegicus 54-57 7599928-14 1995 It is concluded that the vasoconstrictor responses to AII in mesenteric artery and tail artery may be mediated by the release of endothelins from the endothelium by increased formation from big ET, an effect that is blocked by phosphoramidon. phosphoramidon 227-241 endothelin 1 Rattus norvegicus 129-140 7606343-23 1995 In conclusion, urodilatin, like ANP reversed and protected against, subsequent methacholine-induced bronchoconstriction; an action enhanced by the presence of phosphoramidon (3.68 x 1O-5 M).Associated with these actions of urodilatin was a rise in cyclic GMP levels as well as the opening of ATP-sensitive K+ and small conductance Ca2+-activated K+ channels. phosphoramidon 159-173 natriuretic peptide A Bos taurus 32-35 7891111-5 1995 The residual activity observed in the presence of the selective endopeptidase-24.11 inhibitor phosphoramidon was blocked by Pro-Ile or N-[1-(RS)-carboxy-3-phenylpropyl]-Ala-Ala-Phe-p-aminobenzoate, inhibitors of endopeptidase-24.16 and endopeptidase-24.15, respectively. phosphoramidon 94-108 neurolysin Homo sapiens 212-231 7891111-5 1995 The residual activity observed in the presence of the selective endopeptidase-24.11 inhibitor phosphoramidon was blocked by Pro-Ile or N-[1-(RS)-carboxy-3-phenylpropyl]-Ala-Ala-Phe-p-aminobenzoate, inhibitors of endopeptidase-24.16 and endopeptidase-24.15, respectively. phosphoramidon 94-108 thimet oligopeptidase 1 Homo sapiens 236-255 7706315-5 1995 Phosphoramidon inhibited the hydrolysis of AZB-125I-ANP. phosphoramidon 0-14 natriuretic peptide A Bos taurus 52-55 7781681-10 1995 Preincubation with phosphoramidon (100 microM) reduced responses to big-endothelin-1, but not endothelin-1. phosphoramidon 19-33 endothelin 1 Mus musculus 72-84 7550091-0 1995 Effects of phosphoramidon on endothelin-1 and big endothelin-1 production in human aortic endothelial cells. phosphoramidon 11-25 endothelin 1 Homo sapiens 50-62 7597662-8 1995 RESULTS: Phosphoramidon administration caused a transient fall in FEV1 from baseline, FEV1 values decreasing 6.3% and 5.3% on the bradykinin and histamine study days, respectively. phosphoramidon 9-23 kininogen 1 Homo sapiens 130-140 7597662-9 1995 When compared with placebo, phosphoramidon elicited a small enhancement of the airways response to bradykinin, the geometric mean PC20 value (range) decreasing from 0.281 (0.015-5.575) to 0.136 (0.006-2.061) mg/ml. phosphoramidon 28-42 kininogen 1 Homo sapiens 99-109 7597662-11 1995 CONCLUSIONS: The small increase in bronchial reactivity to bradykinin after phosphoramidon exposure suggests that endogenous airway NEP may play a modulatory role in the airways response to inflammatory peptides in human asthma. phosphoramidon 76-90 kininogen 1 Homo sapiens 59-69 7597662-11 1995 CONCLUSIONS: The small increase in bronchial reactivity to bradykinin after phosphoramidon exposure suggests that endogenous airway NEP may play a modulatory role in the airways response to inflammatory peptides in human asthma. phosphoramidon 76-90 membrane metalloendopeptidase Homo sapiens 132-135 7550091-1 1995 Using cultured human aortic endothelial cells, we examined the effects of phosphoramidon, an endothelin converting enzyme (ECE) inhibitor, on the release of endogenous endothelin-1 (ET-1) and big endothelin-1 (big ET-1), and on the generation of ET-1 from exogenously applied big ET-1. phosphoramidon 74-88 endothelin 1 Homo sapiens 168-180 7550091-1 1995 Using cultured human aortic endothelial cells, we examined the effects of phosphoramidon, an endothelin converting enzyme (ECE) inhibitor, on the release of endogenous endothelin-1 (ET-1) and big endothelin-1 (big ET-1), and on the generation of ET-1 from exogenously applied big ET-1. phosphoramidon 74-88 endothelin 1 Homo sapiens 182-186 7550091-1 1995 Using cultured human aortic endothelial cells, we examined the effects of phosphoramidon, an endothelin converting enzyme (ECE) inhibitor, on the release of endogenous endothelin-1 (ET-1) and big endothelin-1 (big ET-1), and on the generation of ET-1 from exogenously applied big ET-1. phosphoramidon 74-88 endothelin 1 Homo sapiens 196-208 7550091-2 1995 Phosphoramidon, at concentrations of 10(-6) to 2 x 10(-4) M, caused a biphasic alteration of the ET-1 release, i.e., at lower concentrations of the drug, there were slight but unexpected increases of the release, whereas higher concentrations led to a decrease which is due to the drug-induced inhibition of ECE. phosphoramidon 0-14 endothelin 1 Homo sapiens 97-101 7550091-2 1995 Phosphoramidon, at concentrations of 10(-6) to 2 x 10(-4) M, caused a biphasic alteration of the ET-1 release, i.e., at lower concentrations of the drug, there were slight but unexpected increases of the release, whereas higher concentrations led to a decrease which is due to the drug-induced inhibition of ECE. phosphoramidon 0-14 endothelin converting enzyme 1 Homo sapiens 308-311 7550091-4 1995 Phosphoramidon enhanced the big ET-1 release from the cells in a concentration-dependent manner. phosphoramidon 0-14 endothelin 1 Homo sapiens 32-36 7550091-5 1995 When high concentrations of phosphoramidon were added, there was a dramatic increase in the release of big ET-1, which cannot be explained only by the drug-induced inhibition of ECE. phosphoramidon 28-42 endothelin 1 Homo sapiens 107-111 7550091-5 1995 When high concentrations of phosphoramidon were added, there was a dramatic increase in the release of big ET-1, which cannot be explained only by the drug-induced inhibition of ECE. phosphoramidon 28-42 endothelin converting enzyme 1 Homo sapiens 178-181 7550091-7 1995 The amount of ET-1 generated from exogenously applied big ET-1 was markedly decreased by phosphoramidon in a concentration-dependent manner. phosphoramidon 89-103 endothelin 1 Homo sapiens 14-18 7550091-7 1995 The amount of ET-1 generated from exogenously applied big ET-1 was markedly decreased by phosphoramidon in a concentration-dependent manner. phosphoramidon 89-103 endothelin 1 Homo sapiens 58-62 7550091-8 1995 In a similar fashion, phosphoramidon markedly inhibited ECE activity of the membrane fraction of cultured cells. phosphoramidon 22-36 endothelin converting enzyme 1 Homo sapiens 56-59 7550091-9 1995 Thus, ET-1 generation from exogenously applied big ET-1 reflects the functional phosphoramidon-sensitive ECE activities in human aortic endothelial cells. phosphoramidon 80-94 endothelin 1 Homo sapiens 6-10 7550091-9 1995 Thus, ET-1 generation from exogenously applied big ET-1 reflects the functional phosphoramidon-sensitive ECE activities in human aortic endothelial cells. phosphoramidon 80-94 endothelin 1 Homo sapiens 51-55 7550091-9 1995 Thus, ET-1 generation from exogenously applied big ET-1 reflects the functional phosphoramidon-sensitive ECE activities in human aortic endothelial cells. phosphoramidon 80-94 endothelin converting enzyme 1 Homo sapiens 105-108 7752584-5 1995 The response of urinary NEP to known inhibitors such as phosphoramidon and thiorphan, and its dependence on pH and salt concentration was studied. phosphoramidon 56-70 membrane metallo-endopeptidase Rattus norvegicus 24-27 7620708-16 1995 Addition of phosphoramidon (10 microM), an inhibitor of a range of metalloendopeptidases, including neutral endopeptidase (E.C.3.4.24.11), markedly reduced the potency of cFP in these systems. phosphoramidon 12-26 complement factor properdin Rattus norvegicus 171-174 7620708-19 1995 Given that cFP is a poor inhibitor of ACE in the presence of phosphoramidon in vitro, it is likely that cFP is cleaved by a phosphoramidon-sensitive metallopeptidase in vivo to liberate N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala, a potent ACE inhibitor. phosphoramidon 61-75 complement factor properdin Rattus norvegicus 104-107 7620708-19 1995 Given that cFP is a poor inhibitor of ACE in the presence of phosphoramidon in vitro, it is likely that cFP is cleaved by a phosphoramidon-sensitive metallopeptidase in vivo to liberate N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala, a potent ACE inhibitor. phosphoramidon 61-75 endothelin converting enzyme-like 1 Rattus norvegicus 149-165 7880721-4 1995 Both basal ET-1 production and exogenously added big ET-1 to ET-1 conversion were greatly reduced in all three cell lines in response to the metalloproteinase inhibitor phosphoramidon but were insensitive to other classes of protease inhibitors. phosphoramidon 169-183 endothelin 1 Homo sapiens 11-15 7880721-4 1995 Both basal ET-1 production and exogenously added big ET-1 to ET-1 conversion were greatly reduced in all three cell lines in response to the metalloproteinase inhibitor phosphoramidon but were insensitive to other classes of protease inhibitors. phosphoramidon 169-183 endothelin 1 Homo sapiens 53-65 7775337-5 1995 Phosphoramidon (0.1 and 1 mM; 90 breaths), an NEP inhibitor, induced a dose-dependent increase in lung resistance to bradykinin without further enhancing BHR induced by IL-1 beta. phosphoramidon 0-14 membrane metallo-endopeptidase Rattus norvegicus 46-49 7775337-5 1995 Phosphoramidon (0.1 and 1 mM; 90 breaths), an NEP inhibitor, induced a dose-dependent increase in lung resistance to bradykinin without further enhancing BHR induced by IL-1 beta. phosphoramidon 0-14 kininogen 1 Homo sapiens 117-127 7857289-1 1995 Subcellular fractionation of the phosphoramidon sensitive membrane-bound endothelin converting enzyme (ECE-1) activity from homogenates of bovine aortic endothelial cells and the human endothelial cell line EA.hy 926, combined with studies of intact cells, shows ECE-1 to be localised primarily to the plasma membrane with the topology of an ectoenzyme. phosphoramidon 33-47 endothelin converting enzyme 1 Bos taurus 103-108 7864859-2 1995 Metalloendoprotease inhibitors (phosphoramidon and DL-thiorphan), but not captopril, inhibited the contractions elicited by human big ET-1 and big ET-2 but DL-thiorphan was less active, suggesting that a non-selective enzymatic process is involved in conversion of big ET-1 and big ET-2 in addition to a phosphoramidon-sensitive ECE. phosphoramidon 32-46 endothelin converting enzyme 1 Homo sapiens 329-332 7774663-5 1995 When big-endothelin-1 was added to the incubation medium of intact live astrocytes, it was converted into mature endothelin-1 in a time-dependent manner and the conversion was inhibited by phosphoramidon. phosphoramidon 189-203 endothelin 1 Rattus norvegicus 9-21 7774663-5 1995 When big-endothelin-1 was added to the incubation medium of intact live astrocytes, it was converted into mature endothelin-1 in a time-dependent manner and the conversion was inhibited by phosphoramidon. phosphoramidon 189-203 endothelin 1 Rattus norvegicus 113-125 7761621-4 1995 Phosphoramidon and SCH 39370, both inhibitors of neutral endopeptidase 24.11 (NEP), markedly inhibited degradation of 125I-ET-I in lung extract and clearly less in kidney extract. phosphoramidon 0-14 membrane metallo-endopeptidase Rattus norvegicus 49-76 7761621-4 1995 Phosphoramidon and SCH 39370, both inhibitors of neutral endopeptidase 24.11 (NEP), markedly inhibited degradation of 125I-ET-I in lung extract and clearly less in kidney extract. phosphoramidon 0-14 membrane metallo-endopeptidase Rattus norvegicus 78-81 7532371-9 1995 Phosphoramidon (5 x 10(-6)-10(-5) M), an NEP inhibitor, enhanced fibroblast proliferation in a dose-dependent manner. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 41-44 7857289-1 1995 Subcellular fractionation of the phosphoramidon sensitive membrane-bound endothelin converting enzyme (ECE-1) activity from homogenates of bovine aortic endothelial cells and the human endothelial cell line EA.hy 926, combined with studies of intact cells, shows ECE-1 to be localised primarily to the plasma membrane with the topology of an ectoenzyme. phosphoramidon 33-47 endothelin converting enzyme 1 Homo sapiens 263-268 7857289-3 1995 The metallopeptidase ECE-1 obtained displayed a neutral pH optimum, a molecular weight of 250 kDa on gel filtration chromatography and was inhibited by phosphoramidon with an IC50 of 0.8 microM. phosphoramidon 152-166 endothelin converting enzyme 1 Homo sapiens 21-26 7857324-5 1995 In addition, the effect of phosphoramidon (10 mg.kg-1) on the pressor response to big ET-1 and its disappearance rate from the circulation were examined. phosphoramidon 27-41 endothelin 1 Rattus norvegicus 86-90 7735698-15 1995 Our results suggest the presence of a phosphoramidon-sensitive endothelin-converting enzyme (ECE) which is responsible for the conversion of big-endothelin-1 and big-endothelin-2 to their active moieties, endothelin-1 and 2. phosphoramidon 38-52 endothelin-1 Cavia porcellus 145-157 7735698-15 1995 Our results suggest the presence of a phosphoramidon-sensitive endothelin-converting enzyme (ECE) which is responsible for the conversion of big-endothelin-1 and big-endothelin-2 to their active moieties, endothelin-1 and 2. phosphoramidon 38-52 endothelin-2 Cavia porcellus 166-178 7735698-15 1995 Our results suggest the presence of a phosphoramidon-sensitive endothelin-converting enzyme (ECE) which is responsible for the conversion of big-endothelin-1 and big-endothelin-2 to their active moieties, endothelin-1 and 2. phosphoramidon 38-52 endothelin-1 Cavia porcellus 205-223 7857324-7 1995 Phosphoramidon reduced the pressor response to big ET-1 by 93%, but did not alter its rate of clearance from the circulation. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 51-55 7541210-3 1995 After pretreatment of the nasal mucosa with PA, the effects of VIP, SP and CGRP on the LDF signal, NAR and mucus production were potentiated, whereas local pretreatment with captopril did not modify these functional effects. phosphoramidon 44-46 vasoactive intestinal peptide Homo sapiens 63-66 7714833-13 1995 Big ET-1 contraction, unlike ET-1 contraction, was curtailed by the inhibitor of the ET-1-converting enzyme, phosphoramidon (50 microM). phosphoramidon 109-123 EDN1 Ovis aries 4-8 7541210-3 1995 After pretreatment of the nasal mucosa with PA, the effects of VIP, SP and CGRP on the LDF signal, NAR and mucus production were potentiated, whereas local pretreatment with captopril did not modify these functional effects. phosphoramidon 44-46 tachykinin precursor 1 Homo sapiens 68-70 7541210-3 1995 After pretreatment of the nasal mucosa with PA, the effects of VIP, SP and CGRP on the LDF signal, NAR and mucus production were potentiated, whereas local pretreatment with captopril did not modify these functional effects. phosphoramidon 44-46 calcitonin related polypeptide alpha Homo sapiens 75-79 8835628-0 1995 Degradation of bradykinin in human urine by carboxypeptidase Y-like exopeptidase and neutral endopeptidase and their inhibition by ebelactone B and phosphoramidon. phosphoramidon 148-162 kininogen 1 Homo sapiens 15-25 8835628-3 1995 The combination of phosphoramidon and ebelactone B completely (by 95%) inhibited bradykinin degradation in human urine. phosphoramidon 19-33 kininogen 1 Homo sapiens 81-91 8587408-7 1995 These data confirm that exogenous big ET-1 is locally converted to ET-1 and CTF in the human forearm, at least in part by a phosphoramidon-sensitive ECE. phosphoramidon 124-138 endothelin 1 Homo sapiens 38-42 8587357-3 1995 Brachial artery infusion of local doses of big ET-1 caused a slow-onset, dose-dependent forearm vasoconstriction that was abolished by co-infusion of the ECE inhibitor phosphoramidon. phosphoramidon 168-182 endothelin 1 Homo sapiens 47-51 8587357-3 1995 Brachial artery infusion of local doses of big ET-1 caused a slow-onset, dose-dependent forearm vasoconstriction that was abolished by co-infusion of the ECE inhibitor phosphoramidon. phosphoramidon 168-182 endothelin converting enzyme 1 Homo sapiens 154-157 8587418-2 1995 Phosphoramidon-sensitive ECE activity was not enriched on immunomagnetically separated angiotensin-converting enzyme (ACE)-bearing luminal endothelial membranes from pig lung, whereas ACE showed a sevenfold enrichment. phosphoramidon 0-14 endothelin converting enzyme 1 Rattus norvegicus 25-28 8587439-8 1995 In the presence of the ET-1-converting enzyme inhibitor phosphoramidon (1.7 mumol/L), ischemia-induced increases of ET-1 concentrations were attenuated in parallel with a time-dependent rise in coronary perfusion pressure. phosphoramidon 56-70 endothelin 1 Rattus norvegicus 23-27 8587439-8 1995 In the presence of the ET-1-converting enzyme inhibitor phosphoramidon (1.7 mumol/L), ischemia-induced increases of ET-1 concentrations were attenuated in parallel with a time-dependent rise in coronary perfusion pressure. phosphoramidon 56-70 endothelin 1 Rattus norvegicus 116-120 7791520-4 1995 These include: (i) one sharp activity optimum at neutral pH; (ii) characteristics typical of a metalloprotease; (iii) IC50 value for phosphoramidon of 1.8 microM (2.7 microM for HUVEC); (iv) no inhibition by captopril and thiorphan, inhibitors of angiotensin converting enzyme and neutral endopeptidase 24.11. phosphoramidon 133-147 angiotensin I converting enzyme Homo sapiens 247-276 7791520-4 1995 These include: (i) one sharp activity optimum at neutral pH; (ii) characteristics typical of a metalloprotease; (iii) IC50 value for phosphoramidon of 1.8 microM (2.7 microM for HUVEC); (iv) no inhibition by captopril and thiorphan, inhibitors of angiotensin converting enzyme and neutral endopeptidase 24.11. phosphoramidon 133-147 membrane metalloendopeptidase Homo sapiens 281-308 8587388-2 1995 Phosphoramidon dose-dependently decreased ET-1-LI production but reciprocally increased [125I]ET-1 binding capacity. phosphoramidon 0-14 endothelin 1 Bos taurus 42-46 8587388-2 1995 Phosphoramidon dose-dependently decreased ET-1-LI production but reciprocally increased [125I]ET-1 binding capacity. phosphoramidon 0-14 endothelin 1 Bos taurus 94-98 8587388-3 1995 ET-1 and ET-3 equipotently inhibited the binding of [125I]ET-1 only in the presence of phosphoramidon. phosphoramidon 87-101 endothelin 1 Bos taurus 0-4 8587388-3 1995 ET-1 and ET-3 equipotently inhibited the binding of [125I]ET-1 only in the presence of phosphoramidon. phosphoramidon 87-101 endothelin 1 Bos taurus 58-62 8587388-4 1995 Northern blot analysis revealed that ETB receptor mRNA expression was more evident in phosphoramidon-treated cells than in nontreated cells. phosphoramidon 86-100 endothelin receptor type B Bos taurus 37-40 8587388-5 1995 In the presence of phosphoramidon, ET-1 and ET-3 equipotently stimulated inositol 1,4,5-trisphosphate formation and [3H]-thymidine incorporation into cultured ECs. phosphoramidon 19-33 endothelin 1 Bos taurus 35-39 8587469-3 1995 In both models, phosphoramidon selectively inhibited the pressor responses to big ET-1 without influencing those to ET-1, angiotensins (AT-I and AT-II) or norepinephrine. phosphoramidon 16-30 endothelin 1 Rattus norvegicus 82-86 8587469-5 1995 It selectively inhibited the pressor responses to big ET-1 with ID50 values of 160 micrograms/kg/min (phosphoramidon: 120 micrograms/kg/min) in the spinal rat and 6 microM (phosphoramidon: 5 microM) in the perfused rat kidney. phosphoramidon 102-116 endothelin 1 Rattus norvegicus 54-58 8587469-5 1995 It selectively inhibited the pressor responses to big ET-1 with ID50 values of 160 micrograms/kg/min (phosphoramidon: 120 micrograms/kg/min) in the spinal rat and 6 microM (phosphoramidon: 5 microM) in the perfused rat kidney. phosphoramidon 173-187 endothelin 1 Rattus norvegicus 54-58 8587470-0 1995 Differential structure-activity relationships of phosphoramidon analogues for inhibition of three metalloproteases: endothelin-converting enzyme, neutral endopeptidase, and angiotensin-converting enzyme. phosphoramidon 49-63 angiotensin I converting enzyme Homo sapiens 173-202 8587470-1 1995 The structure-activity relationships of phosphoramidon analogues for inhibition of endothelin-converting enzyme (ECE), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE) were compared. phosphoramidon 40-54 endothelin converting enzyme 1 Homo sapiens 113-116 8587470-1 1995 The structure-activity relationships of phosphoramidon analogues for inhibition of endothelin-converting enzyme (ECE), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE) were compared. phosphoramidon 40-54 membrane metalloendopeptidase Homo sapiens 119-146 8587470-2 1995 Phosphoramidon inhibited ECE, NEP, and ACE activities with IC50 values of 3.5, 0.034, and 78 microM, respectively. phosphoramidon 0-14 endothelin converting enzyme 1 Homo sapiens 25-28 8587470-2 1995 Phosphoramidon inhibited ECE, NEP, and ACE activities with IC50 values of 3.5, 0.034, and 78 microM, respectively. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 30-33 8587470-2 1995 Phosphoramidon inhibited ECE, NEP, and ACE activities with IC50 values of 3.5, 0.034, and 78 microM, respectively. phosphoramidon 0-14 angiotensin I converting enzyme Homo sapiens 39-42 8587470-3 1995 Removal of the rhamnose moiety of phosphoramidon (dipeptide 3) reduced the potency for ECE (IC50 = 70 microM), whereas the potencies for NEP (0.003 microM) and ACE (0.20 microM) were increased. phosphoramidon 34-48 endothelin converting enzyme 1 Homo sapiens 87-90 8587470-6 1995 These results suggest that a hydrophobic group in the P1 position of phosphoramidon analogues increases the potency for ECE significantly, whereas compounds containing a free phosphonic acid are optimal for inhibition of NEP and ACE. phosphoramidon 69-83 endothelin converting enzyme 1 Homo sapiens 120-123 7674808-4 1995 When cells were pretreated with 100 microM phosphoramidon, the stimulation by big ET-1, but not ET-1 was abolished. phosphoramidon 43-57 endothelin 1 Bos taurus 82-86 7674808-4 1995 When cells were pretreated with 100 microM phosphoramidon, the stimulation by big ET-1, but not ET-1 was abolished. phosphoramidon 43-57 endothelin 1 Bos taurus 96-100 7674808-5 1995 In separate experiments, when cells were incubated with exogenous big ET-1, a time-dependent phosphoramidon-sensitive conversion to ET-1 was detected by radioimmunoassay. phosphoramidon 93-107 endothelin 1 Bos taurus 70-74 7674808-5 1995 In separate experiments, when cells were incubated with exogenous big ET-1, a time-dependent phosphoramidon-sensitive conversion to ET-1 was detected by radioimmunoassay. phosphoramidon 93-107 endothelin 1 Bos taurus 132-136 7674808-6 1995 These results are consistent with the presence of a phosphoramidon-sensitive endothelin converting enzyme on the surface of bovine pulmonary artery smooth muscle cells, which may play a role in regulating signalling by circulating big ET-1. phosphoramidon 52-66 endothelin 1 Bos taurus 235-239 7705468-2 1994 Endothelin-3-evoked contractions were markedly enhanced by phosphoramidon (3.67 x 10(-5) M), unaffected by atropine (10(-5) M), and attenuated by indomethacin (10(-6) M) or nifedipine (10(-5) M). phosphoramidon 59-73 endothelin 3 Homo sapiens 0-12 8587408-7 1995 These data confirm that exogenous big ET-1 is locally converted to ET-1 and CTF in the human forearm, at least in part by a phosphoramidon-sensitive ECE. phosphoramidon 124-138 endothelin 1 Homo sapiens 67-79 8587408-7 1995 These data confirm that exogenous big ET-1 is locally converted to ET-1 and CTF in the human forearm, at least in part by a phosphoramidon-sensitive ECE. phosphoramidon 124-138 endothelin converting enzyme 1 Homo sapiens 149-152 7896062-3 1994 Addition of phosphoramidon to the medium caused a potentiation in the vasoconstrictor response to endothelin-1 and greatly, but not completely, inhibited vasoconstriction induced by pre-pro-endothelin-1. phosphoramidon 12-26 endothelin-1 Oryctolagus cuniculus 98-110 7896062-3 1994 Addition of phosphoramidon to the medium caused a potentiation in the vasoconstrictor response to endothelin-1 and greatly, but not completely, inhibited vasoconstriction induced by pre-pro-endothelin-1. phosphoramidon 12-26 endothelin-1 Oryctolagus cuniculus 190-202 7921430-9 1994 The NEP inhibitor phosphoramidon tended to increase the sensitivity to BK (NS) and did not change the direction of the response. phosphoramidon 18-32 membrane metalloendopeptidase Homo sapiens 4-7 7896062-13 1994 From these results it was concluded that phosphoramidon-sensitive endothelin-converting enzyme, probably localized in microvasculature of the kidney, can convert pre-pro-endothelin-1 to endothelin-1 which is responsible for the vasoconstrictor effect of pre-pro-endothelin-1 in addition to its possible direct vasoconstrictor effect on kidney vasculature. phosphoramidon 41-55 endothelin-1 Oryctolagus cuniculus 170-182 7896062-13 1994 From these results it was concluded that phosphoramidon-sensitive endothelin-converting enzyme, probably localized in microvasculature of the kidney, can convert pre-pro-endothelin-1 to endothelin-1 which is responsible for the vasoconstrictor effect of pre-pro-endothelin-1 in addition to its possible direct vasoconstrictor effect on kidney vasculature. phosphoramidon 41-55 endothelin-1 Oryctolagus cuniculus 186-198 7896062-13 1994 From these results it was concluded that phosphoramidon-sensitive endothelin-converting enzyme, probably localized in microvasculature of the kidney, can convert pre-pro-endothelin-1 to endothelin-1 which is responsible for the vasoconstrictor effect of pre-pro-endothelin-1 in addition to its possible direct vasoconstrictor effect on kidney vasculature. phosphoramidon 41-55 endothelin-1 Oryctolagus cuniculus 186-198 7916401-3 1994 Brachial artery infusion of local doses of proendothelin-1, the precursor to endothelin-1, caused a slow-onset dose-dependent forearm vasoconstriction which was abolished by co-infusion of phosphoramidon. phosphoramidon 189-203 endothelin 1 Homo sapiens 46-58 7923622-4 1994 Therefore, we examined the effect of an NEP inhibitor, phosphoramidon, on myocardial perfusion in rats after (1) stimulating sensory nerves with capsaicin and (2) inducing myocardial hypoperfusion with isoproterenol, with or without pretreatment with selective antagonists of the substance P (NK1) and bradykinin (B2) receptors. phosphoramidon 55-69 membrane metallo-endopeptidase Rattus norvegicus 40-43 7965744-8 1994 Phosphoramidon (50 microM) inhibited (60%) both AII-induced irET release and cell proliferation. phosphoramidon 0-14 angiotensinogen Rattus norvegicus 48-51 7812611-10 1994 Both phosphoramidon and SQ-28,603, potent inhibitors of NEP, completely protected both peptides from metabolism by rNEP. phosphoramidon 5-19 membrane metalloendopeptidase Homo sapiens 56-59 7535520-5 1994 In contrast, phosphoramidon potentiated BK-induced responses only at low concentrations of BK. phosphoramidon 13-27 kininogen 1 Canis lupus familiaris 40-42 7535520-5 1994 In contrast, phosphoramidon potentiated BK-induced responses only at low concentrations of BK. phosphoramidon 13-27 kininogen 1 Canis lupus familiaris 91-93 7529108-2 1994 Phosphoramidon, a potent inhibitor of endopeptidase-24.11 (E-24.11) and thermolysin, has been shown to reduce the hypertensive effect of exogenous big endothelin-1 (big ET-1) in rats. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 151-163 7529108-2 1994 Phosphoramidon, a potent inhibitor of endopeptidase-24.11 (E-24.11) and thermolysin, has been shown to reduce the hypertensive effect of exogenous big endothelin-1 (big ET-1) in rats. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 169-173 7812611-10 1994 Both phosphoramidon and SQ-28,603, potent inhibitors of NEP, completely protected both peptides from metabolism by rNEP. phosphoramidon 5-19 membrane metallo-endopeptidase Rattus norvegicus 115-119 7847182-0 1994 Differential effects of phosphoramidon and captopril on NK1 receptor-mediated plasma extravasation in the rat trachea. phosphoramidon 24-38 tachykinin receptor 1 Rattus norvegicus 56-68 7847182-7 1994 Nevertheless, the responses to substance P and neurokinin A were clearly potentiated in rats given phosphoramidon, indicating that NEP effectively degrades tachykinins in vivo. phosphoramidon 99-113 membrane metallo-endopeptidase Rattus norvegicus 131-134 7924171-0 1994 Effects of phosphoramidon and pepstatin A on the secretion of endothelin-1 and big endothelin-1 by human umbilical vein endothelial cells: measurement by two-site enzyme-linked immunosorbent assays. phosphoramidon 11-25 endothelin 1 Homo sapiens 62-74 7924171-0 1994 Effects of phosphoramidon and pepstatin A on the secretion of endothelin-1 and big endothelin-1 by human umbilical vein endothelial cells: measurement by two-site enzyme-linked immunosorbent assays. phosphoramidon 11-25 endothelin 1 Homo sapiens 83-95 7924171-9 1994 The secretion of both peptides was time-dependent over 12 h. The metalloprotease inhibitor phosphoramidon (1 x 10(-4) mol/l) significantly reduced the amount of endothelin-1 secreted into the medium (P < 0.05), with a concomitant increase in the secreted levels of big endothelin-1 (P < 0.01). phosphoramidon 91-105 endothelin 1 Homo sapiens 161-173 7924171-9 1994 The secretion of both peptides was time-dependent over 12 h. The metalloprotease inhibitor phosphoramidon (1 x 10(-4) mol/l) significantly reduced the amount of endothelin-1 secreted into the medium (P < 0.05), with a concomitant increase in the secreted levels of big endothelin-1 (P < 0.01). phosphoramidon 91-105 endothelin 1 Homo sapiens 272-284 7949376-6 1994 Both intact cells and membrane preparations used as the enzyme source predict similar IC50 values for phosphoramidon inhibition of ECE (ca 1 microM). phosphoramidon 102-116 endothelin converting enzyme 1 Homo sapiens 131-134 8039848-0 1994 Phosphoramidon-sensitive conversion of big endothelin-1 and degradation of endothelin-1 in rat kidney. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 43-55 8039848-0 1994 Phosphoramidon-sensitive conversion of big endothelin-1 and degradation of endothelin-1 in rat kidney. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 75-87 8039848-4 1994 Phosphoramidon (10(-4) mol/L), a metalloproteinase inhibitor, significantly suppressed the big ET-1-induced pressor action and the accumulation of immunoreactive endothelin in renal tissues. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 95-99 8039848-5 1994 On the other hand, phosphoramidon slightly but significantly sustained the ET-1-induced pressor effect. phosphoramidon 19-33 endothelin 1 Rattus norvegicus 75-79 8039848-7 1994 When ET-1 was exogenously added to the perfusate, phosphoramidon or kelatorphan significantly increased the immunoreactive endothelin levels in renal tissues after perfusion, without affecting the disappearance rate of immunoreactive endothelin from the perfusate. phosphoramidon 50-64 endothelin 1 Rattus norvegicus 5-9 8039848-8 1994 Therefore, the phosphoramidon-sensitive ET-1-converting enzyme in the kidney seems to contribute to the functional local conversion of big ET-1 to ET-1, and neutral endopeptidase 24.11 may be responsible for the proteolytic degradation of ET-1 in the kidney. phosphoramidon 15-29 endothelin 1 Rattus norvegicus 40-44 8039848-8 1994 Therefore, the phosphoramidon-sensitive ET-1-converting enzyme in the kidney seems to contribute to the functional local conversion of big ET-1 to ET-1, and neutral endopeptidase 24.11 may be responsible for the proteolytic degradation of ET-1 in the kidney. phosphoramidon 15-29 endothelin 1 Rattus norvegicus 139-151 8039848-8 1994 Therefore, the phosphoramidon-sensitive ET-1-converting enzyme in the kidney seems to contribute to the functional local conversion of big ET-1 to ET-1, and neutral endopeptidase 24.11 may be responsible for the proteolytic degradation of ET-1 in the kidney. phosphoramidon 15-29 endothelin 1 Rattus norvegicus 139-143 7938704-0 1994 Evidence for phosphoramidon-sensitive cleavage of big endothelin-1 involved in endothelin-stimulated hepatic glucose production. phosphoramidon 13-27 endothelin 1 Rattus norvegicus 54-66 8034569-6 1994 Expressed ECE was inhibited by phosphoramidon, but not by thiorphan. phosphoramidon 31-45 endothelin converting enzyme 1 Rattus norvegicus 10-13 7993815-5 1994 Addition of the CD10 inhibitor, phosphoramidon, together with IL-1 beta resulted in a left shift in the dose-response curve which corresponded to a 10-fold potentiation of the IL-1 beta effect. phosphoramidon 32-46 membrane metalloendopeptidase Homo sapiens 16-20 7993815-5 1994 Addition of the CD10 inhibitor, phosphoramidon, together with IL-1 beta resulted in a left shift in the dose-response curve which corresponded to a 10-fold potentiation of the IL-1 beta effect. phosphoramidon 32-46 interleukin 1 beta Homo sapiens 176-185 7959879-4 1994 CD10 activity was abolished by specific NEP inhibitors, including thiorphan, retrothiorphan and phosphoramidon. phosphoramidon 96-110 membrane metalloendopeptidase Homo sapiens 0-4 7959879-4 1994 CD10 activity was abolished by specific NEP inhibitors, including thiorphan, retrothiorphan and phosphoramidon. phosphoramidon 96-110 membrane metalloendopeptidase Homo sapiens 40-43 8072216-5 1994 NEP activity in rat kidney was inhibited by specific NEP inhibitors (phosphoramidon, thiorphan, SCH39370, SCH47896 and SCH48446) at micromolar concentrations. phosphoramidon 69-83 membrane metallo-endopeptidase Rattus norvegicus 0-3 8072216-5 1994 NEP activity in rat kidney was inhibited by specific NEP inhibitors (phosphoramidon, thiorphan, SCH39370, SCH47896 and SCH48446) at micromolar concentrations. phosphoramidon 69-83 membrane metallo-endopeptidase Rattus norvegicus 53-56 7522926-14 1994 endothelins are mediated by ETA receptors in the rat spinal cord; (2) that the pressor response and bradycardia are likely due to the activation of the sympatho-adrenal nervous system and to a vagal reflex mechanism, respectively; and (3) that a phosphoramidon-sensitive ECE converts big ET-1 to ET-1 in the rat spinal cord. phosphoramidon 246-260 endothelin 1 Rattus norvegicus 0-11 7938704-3 1994 Thereby, big ET-1 (10 nM) induced a maximally three-fold increase (P < 0.01 vs. basal values) in hepatic glucose production at 60 min, which was almost completely abolished by concomitant infusion of 50 microM phosphoramidon, a sensitive inhibitor of the enzymatic cleavage of big ET-1 to ET-1. phosphoramidon 213-227 endothelin 1 Rattus norvegicus 13-17 7938704-4 1994 The corresponding incremental release of glucose by big ET-1 was 20.9-fold higher in the absence of phosphoramidon than in its presence (P < 0.01). phosphoramidon 100-114 endothelin 1 Rattus norvegicus 56-60 7938704-8 1994 In conclusion, big ET-1 induces hepatic glucose release, which is suggested to depend on intrahepatic conversion of big ET-1 to ET-1 by a phosphoramidon-sensitive pathway. phosphoramidon 138-152 endothelin 1 Rattus norvegicus 19-23 7938704-8 1994 In conclusion, big ET-1 induces hepatic glucose release, which is suggested to depend on intrahepatic conversion of big ET-1 to ET-1 by a phosphoramidon-sensitive pathway. phosphoramidon 138-152 endothelin 1 Rattus norvegicus 120-124 7938704-8 1994 In conclusion, big ET-1 induces hepatic glucose release, which is suggested to depend on intrahepatic conversion of big ET-1 to ET-1 by a phosphoramidon-sensitive pathway. phosphoramidon 138-152 endothelin 1 Rattus norvegicus 120-124 8141343-0 1994 Conversion of big ET-1 in the rat lung: role of phosphoramidon-sensitive endothelin-1-converting enzyme. phosphoramidon 48-62 endothelin 1 Rattus norvegicus 73-85 8192653-2 1994 This hydrolysis was only partially inhibited (40%) by 10 microM phosphoramidon, an inhibitor of endopeptidase-24.11, but was almost totally abolished in the presence of a mixture of 10 microM phosphoramidon and 10 microM captopril, a potent inhibitor of mammalian angiotensin-converting enzyme (ACE). phosphoramidon 64-78 angiotensin I converting enzyme Homo sapiens 295-298 8192653-2 1994 This hydrolysis was only partially inhibited (40%) by 10 microM phosphoramidon, an inhibitor of endopeptidase-24.11, but was almost totally abolished in the presence of a mixture of 10 microM phosphoramidon and 10 microM captopril, a potent inhibitor of mammalian angiotensin-converting enzyme (ACE). phosphoramidon 192-206 angiotensin I converting enzyme Homo sapiens 295-298 8182555-7 1994 A similar effectiveness of phosphoramidon was seen when transforming growth factor-beta 1 was used instead of platelets. phosphoramidon 27-41 transforming growth factor, beta 1 Rattus norvegicus 56-89 8182555-9 1994 We also suggest that the inhibition of ET converting enzyme by phosphoramidon is more effective in the augmented condition of ET-1 production than in the basal condition. phosphoramidon 63-77 endothelin 1 Rattus norvegicus 126-130 7909519-9 1994 In the astrocytic membrane-associated fraction, neuromedin N underwent an additional minor endoproteolytic cleavage at the Pro3-Tyr4 bond elicited by endopeptidase 24.11, as suggested by the protective effect of its blocking agent phosphoramidon. phosphoramidon 231-245 neurotensin Mus musculus 48-60 7519178-6 1994 In the case of substance P, we demonstrate the significance of NEP in modulating the process of downregulation by use of a specific NEP inhibitor, phosphoramidon. phosphoramidon 147-161 tachykinin precursor 1 Homo sapiens 15-26 7519178-6 1994 In the case of substance P, we demonstrate the significance of NEP in modulating the process of downregulation by use of a specific NEP inhibitor, phosphoramidon. phosphoramidon 147-161 membrane metalloendopeptidase Homo sapiens 63-66 7519178-6 1994 In the case of substance P, we demonstrate the significance of NEP in modulating the process of downregulation by use of a specific NEP inhibitor, phosphoramidon. phosphoramidon 147-161 membrane metalloendopeptidase Homo sapiens 132-135 7914787-5 1994 In the glial cell line the hydrolysis of cholecystokinin octapeptide (CCK-8), sulphated or non-sulphated, was inhibited predominantly by the NEP inhibitor, phosphoramidon (PR). phosphoramidon 156-170 cholecystokinin Homo sapiens 41-56 7914787-5 1994 In the glial cell line the hydrolysis of cholecystokinin octapeptide (CCK-8), sulphated or non-sulphated, was inhibited predominantly by the NEP inhibitor, phosphoramidon (PR). phosphoramidon 156-170 cholecystokinin Homo sapiens 70-73 7914787-5 1994 In the glial cell line the hydrolysis of cholecystokinin octapeptide (CCK-8), sulphated or non-sulphated, was inhibited predominantly by the NEP inhibitor, phosphoramidon (PR). phosphoramidon 156-170 membrane metalloendopeptidase Homo sapiens 141-144 8141304-0 1994 Phosphoramidon attenuates big endothelin-1-induced vasoconstriction in canine stomach. phosphoramidon 0-14 endothelin 1 Canis lupus familiaris 30-42 8141304-6 1994 In other experiments, using 15-min peptide infusions, we found that pretreatment with phosphoramidon, an inhibitor of endothelin-converting enzyme, markedly reduced response to big endothelin-1 but not to endothelin-1. phosphoramidon 86-100 endothelin 1 Canis lupus familiaris 181-193 8306034-7 1994 Pretreatment with phosphoramidon abolished the differential effect of acrolein on airway response to NKA. phosphoramidon 18-32 tachykinin precursor 1 Homo sapiens 101-104 8082712-1 1994 The role of phosphoramidon-sensitive endothelin converting enzyme in the release of endogenous endothelin-1 was investigated in anesthetized rats. phosphoramidon 12-26 endothelin 1 Rattus norvegicus 95-107 8082712-7 1994 It is concluded that the release of endogenous endothelin-1 release stimulated by hemorrhage, cytokines and hypoxia is resistant to inhibition by phosphoramidon, and at high doses, phosphoramidon potentiates hemorrhage- and hypoxia-induced increases in endothelin-1 levels, most likely by preventing its degradation. phosphoramidon 146-160 endothelin 1 Rattus norvegicus 47-59 8082712-7 1994 It is concluded that the release of endogenous endothelin-1 release stimulated by hemorrhage, cytokines and hypoxia is resistant to inhibition by phosphoramidon, and at high doses, phosphoramidon potentiates hemorrhage- and hypoxia-induced increases in endothelin-1 levels, most likely by preventing its degradation. phosphoramidon 181-195 endothelin 1 Rattus norvegicus 47-59 8082712-7 1994 It is concluded that the release of endogenous endothelin-1 release stimulated by hemorrhage, cytokines and hypoxia is resistant to inhibition by phosphoramidon, and at high doses, phosphoramidon potentiates hemorrhage- and hypoxia-induced increases in endothelin-1 levels, most likely by preventing its degradation. phosphoramidon 181-195 endothelin 1 Rattus norvegicus 253-265 8032633-10 1994 Neurotensin (1-11) was mainly generated by a phosphoramidon-sensitive cleavage, probably elicited by endopeptidase 24-11. phosphoramidon 45-59 neurotensin Canis lupus familiaris 0-11 7908871-6 1994 In renal brush border membranes, hydrolysis of PYY is substantially (> 75%) inhibited by phosphoramidon, suggesting that endopeptidase-24.11 initiates hydrolysis of PYY in this preparation. phosphoramidon 92-106 peptide YY Homo sapiens 47-50 7908871-6 1994 In renal brush border membranes, hydrolysis of PYY is substantially (> 75%) inhibited by phosphoramidon, suggesting that endopeptidase-24.11 initiates hydrolysis of PYY in this preparation. phosphoramidon 92-106 peptide YY Homo sapiens 168-171 8032603-13 1994 Both ET-1 and ET-3 (in the presence of phosphoramidon)-evoked contractions were significantly enhanced by the presence of the phorbol ester phorbol 12,13-dibutyrate (10(-8) M). phosphoramidon 39-53 endothelin 1 Bos taurus 5-18 8160888-3 1994 Pretreatment with 10 mg of phosphoramidon, an ET-1-converting enzyme inhibitor, blocked the hypertensive response to bET-1. phosphoramidon 27-41 EDN1 Ovis aries 46-50 8160888-7 1994 Phosphoramidon inhibits bET-1-induced hypertension, suggesting that the fetus possesses ET-1-converting enzyme activity. phosphoramidon 0-14 EDN1 Ovis aries 25-29 7512455-0 1994 Modulation of the effect of atrial natriuretic peptide in human and bovine bronchi by phosphoramidon. phosphoramidon 86-100 natriuretic peptide A Bos taurus 28-54 7512455-10 1994 Phosphoramidon potentiated atrial natriuretic peptide-induced relaxation of methacholine-induced tone and the ability of atrial natriuretic peptide to protect against methacholine-induced contraction. phosphoramidon 0-14 natriuretic peptide A Bos taurus 27-53 8141343-7 1994 We tentatively conclude that the phosphoramidon-sensitive conversion of Big ET-T to ET-1 is linked to the pressor action of Big ET-1 in the isolated perfused rat lung. phosphoramidon 33-47 endothelin 1 Rattus norvegicus 84-88 8141343-7 1994 We tentatively conclude that the phosphoramidon-sensitive conversion of Big ET-T to ET-1 is linked to the pressor action of Big ET-1 in the isolated perfused rat lung. phosphoramidon 33-47 endothelin 1 Rattus norvegicus 128-132 8187026-9 1994 Phosphoramidon administered by inhalation elicited a significant (P < 0.01 vs baseline and control solution) potentiation in the airway responsiveness to inhaled NKA, the NKA PD15 value decreasing to 9.45 x 10(-9) mol. phosphoramidon 0-14 tachykinin precursor 1 Homo sapiens 165-168 8187026-9 1994 Phosphoramidon administered by inhalation elicited a significant (P < 0.01 vs baseline and control solution) potentiation in the airway responsiveness to inhaled NKA, the NKA PD15 value decreasing to 9.45 x 10(-9) mol. phosphoramidon 0-14 tachykinin precursor 1 Homo sapiens 174-177 8187026-10 1994 The present study confirms that inhaled NKA induces a dose-related bronchoconstriction in asthmatic patients and demonstrates that inhaled phosphoramidon potentiates NKA-induced bronchoconstriction. phosphoramidon 139-153 tachykinin precursor 1 Homo sapiens 166-169 8020872-1 1994 The structure activity relationship of phosphoramidon analogues was studied for their ability to reduce the hypertensive effect of exogenous proET-1, probably via inhibition of an endothelin converting enzyme activity (ECE). phosphoramidon 39-53 endothelin converting enzyme 1 Homo sapiens 219-222 8020872-4 1994 Furthermore, the tryptophan residue of phosphoramidon appeared to be particularly important for the ECE inhibition, whereas thermolysin inhibition seemed to depend greatly on the leucine residue. phosphoramidon 39-53 endothelin converting enzyme 1 Homo sapiens 100-103 8020872-5 1994 It is concluded that in vivo ECE and thermolysin differ in the way they recognise phosphoramidon. phosphoramidon 82-96 endothelin converting enzyme 1 Homo sapiens 29-32 8020872-6 1994 The existence of an hydrophobic pocket, specific for the recognition of the tryptophan residue of phosphoramidon, could be proposed for ECE. phosphoramidon 98-112 endothelin converting enzyme 1 Homo sapiens 136-139 8181798-1 1994 Neuropeptide gamma (NP gamma) induced a contractile response of the human isolated bronchus which was potentiated by the neutral endopeptidase inhibitor, phosphoramidon, but was not modified by atropine and indomethacin. phosphoramidon 154-168 tachykinin precursor 1 Homo sapiens 0-28 7934630-11 1994 Big ET-1 caused dose-dependent pressor effects in isolated perfused rat kidney and these pressor effects were significantly suppressed by phosphoramidon. phosphoramidon 138-152 endothelin 1 Rattus norvegicus 4-8 7990652-7 1994 On the other hand, in normal rats, the airway responsiveness to inhaled ACh was significantly increased by pretreatment with NEP inhibitor, phosphoramidon (3 mg/kg, i.v. phosphoramidon 140-154 membrane metallo-endopeptidase Rattus norvegicus 125-128 8289588-4 1994 Exposure to phosphoramidon, a metalloproteinase inhibitor, significantly suppressed the pressor response to big ET-1, in a similar fashion. phosphoramidon 12-26 endothelin 1 Rattus norvegicus 112-116 8289588-6 1994 Apparently there is a difference in potency for phosphoramidon-sensitive vasoconstriction of big ET-1 between organs and presumably regional differences in the functional phosphoramidon-sensitive conversion of big ET-1 in vasculatures. phosphoramidon 48-62 endothelin 1 Rattus norvegicus 97-101 8289588-6 1994 Apparently there is a difference in potency for phosphoramidon-sensitive vasoconstriction of big ET-1 between organs and presumably regional differences in the functional phosphoramidon-sensitive conversion of big ET-1 in vasculatures. phosphoramidon 171-185 endothelin 1 Rattus norvegicus 97-101 7691676-5 1993 The neutral endopeptidase inhibitor, phosphoramidon, increased only the response to SP. phosphoramidon 37-51 tachykinin precursor 1 Homo sapiens 84-86 7691676-10 1993 Response to SP is modulated by a phosphoramidon-sensitive enzymatic activity. phosphoramidon 33-47 tachykinin precursor 1 Homo sapiens 12-14 8284261-1 1993 We examined the effects of captopril (an angiotensin-converting enzyme inhibitor) and phosphoramidon (a selective enkephalinase inhibitor) on Tyr-Gly-Gly production during Met-enkephalin hydrolysis in plasma samples taken from individual outbred Swiss-Webster and inbred C57BL/6J and DBA/2J mice. phosphoramidon 86-100 membrane metallo endopeptidase Mus musculus 114-127 8284261-1 1993 We examined the effects of captopril (an angiotensin-converting enzyme inhibitor) and phosphoramidon (a selective enkephalinase inhibitor) on Tyr-Gly-Gly production during Met-enkephalin hydrolysis in plasma samples taken from individual outbred Swiss-Webster and inbred C57BL/6J and DBA/2J mice. phosphoramidon 86-100 pro-opiomelanocortin-alpha Mus musculus 172-186 8238539-3 1993 A small dose of aerosolized ovalbumin (OVA, 0.1%) produced a small increase in RL that was further increased and markedly prolonged by the neutral endopeptidase (NEP) inhibitor phosphoramidon; this bronchoconstrictor effect of OVA was markedly reduced by the NK2-receptor antagonist and was abolished by the combination of the NK1 and NK2-receptor antagonists together. phosphoramidon 177-191 substance-K receptor Cavia porcellus 259-271 8238539-3 1993 A small dose of aerosolized ovalbumin (OVA, 0.1%) produced a small increase in RL that was further increased and markedly prolonged by the neutral endopeptidase (NEP) inhibitor phosphoramidon; this bronchoconstrictor effect of OVA was markedly reduced by the NK2-receptor antagonist and was abolished by the combination of the NK1 and NK2-receptor antagonists together. phosphoramidon 177-191 substance-K receptor Cavia porcellus 335-347 8136718-5 1993 This new enzyme is clearly distinct from neutral endopeptidase (NEP, EC 3.4.24.11) and angiotensin-converting enzyme (ACE,EC 3.4.15.1), since specific inhibitors for these endopeptidases (10 microM phosphoramidon and 1 mM captopril, respectively) had no effect on their activity. phosphoramidon 198-212 membrane metalloendopeptidase Homo sapiens 64-67 8136718-5 1993 This new enzyme is clearly distinct from neutral endopeptidase (NEP, EC 3.4.24.11) and angiotensin-converting enzyme (ACE,EC 3.4.15.1), since specific inhibitors for these endopeptidases (10 microM phosphoramidon and 1 mM captopril, respectively) had no effect on their activity. phosphoramidon 198-212 angiotensin I converting enzyme Homo sapiens 118-121 8223929-0 1993 Endothelium-independent pressor effect of big endothelin-1 and its inhibition by phosphoramidon in rat mesenteric artery. phosphoramidon 81-95 endothelin 1 Rattus norvegicus 46-58 8223929-3 1993 Phosphoramidon suppressed the big endothelin-1-induced pressor action without affecting the action of endothelin-1, irrespective of the presence or absence of the endothelium. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 34-46 8106108-10 1993 Pressor responses induced by big-endothelin-1, -2 and -3 (3, 15 and 10 nmol kg-1, respectively) were markedly reduced (60, 80 and 100%) in the presence of phosphoramidon (10 mg kg-1, i.v.). phosphoramidon 155-169 endothelin 1 Rattus norvegicus 33-56 8106108-18 1993 Phosphoramidon, but not thiorphan, concentration-dependently(10 and 100 microM) reduced big-endothelin-1 (58 and 86% respectively) and big-endothelin-2 (21 and 56%)-mediated responses. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 92-104 8106108-18 1993 Phosphoramidon, but not thiorphan, concentration-dependently(10 and 100 microM) reduced big-endothelin-1 (58 and 86% respectively) and big-endothelin-2 (21 and 56%)-mediated responses. phosphoramidon 0-14 endothelin 2 Rattus norvegicus 139-151 8106108-19 1993 Conversely, the big-endothelin-3 effect was reduced by phosphoramidon only at 100 microM (-70%), while thiorphan acts concentration-dependently (31 and 71% at 10 and 100 microM respectively); thus, in the rat vas deferens, big-endothelin-I and -2 were as potent as their corresponding endothelins, while big-endothelin-3 was about 20 times less potent than endothelin-3.5. phosphoramidon 55-69 endothelin 3 Rattus norvegicus 20-32 8106108-20 1993 The increasing effect of endothelin-2 (194 +/- 30% over baseline) was significantly enhanced by either 10 microM phosphoramidon (277 +/- 42%) or thiorphan (318 +/- 15%). phosphoramidon 113-127 endothelin 2 Rattus norvegicus 25-37 8289588-6 1994 Apparently there is a difference in potency for phosphoramidon-sensitive vasoconstriction of big ET-1 between organs and presumably regional differences in the functional phosphoramidon-sensitive conversion of big ET-1 in vasculatures. phosphoramidon 171-185 endothelin 1 Rattus norvegicus 214-218 8289600-1 1994 Hydrolysis of fragments of the C-terminal and mid-portions of parathyroid hormone (PTH) by a phosphoramidon-insensitive metallo-endopeptidase, previously purified by us from the microvillar membranes of rat kidney, and by the microvillar membranes of rat kidney themselves were investigated using a reverse-phase HPLC, and the amino acid sequences of each produced PTH metabolite were compared after their determination with an automated gas-phase protein sequencer. phosphoramidon 93-107 parathyroid hormone Rattus norvegicus 62-81 8243532-0 1993 Big-endothelin-1 contracts rat isolated uterus via a phosphoramidon-sensitive endothelin ETA receptor-mediated mechanism. phosphoramidon 53-67 endothelin 1 Rattus norvegicus 4-16 8243532-1 1993 The presence of a phosphoramidon-sensitive endothelin-1-converting enzyme was investigated in the rat isolated uterus. phosphoramidon 18-32 endothelin 1 Rattus norvegicus 43-55 8243532-4 1993 The tonic contraction induced by big-endothelin-1 (10 nM) was nearly abolished by phosphoramidon (100 microM), but the response to an equieffective concentration of endothelin-1 (3 nM) was not affected. phosphoramidon 82-96 endothelin 1 Rattus norvegicus 37-49 8217029-1 1993 We reported previously that the endothelin converting enzyme (ECE) inhibitor phosphoramidon lowers mean arterial pressure (MAP) when infused in conscious, spontaneously hypertensive rats (SHRs). phosphoramidon 77-91 endothelin converting enzyme 1 Rattus norvegicus 32-60 8223885-5 1993 Phosphoramidon (1 microM) potentiated the response to substance P without changing the order of potency of natural tachykinins. phosphoramidon 0-14 tachykinin precursor 1 Homo sapiens 54-65 8223885-11 1993 Moreover, a phosphoramidon-sensitive mechanism plays a role in the regulation of the response to substance P. phosphoramidon 12-26 tachykinin precursor 1 Homo sapiens 97-108 8217029-1 1993 We reported previously that the endothelin converting enzyme (ECE) inhibitor phosphoramidon lowers mean arterial pressure (MAP) when infused in conscious, spontaneously hypertensive rats (SHRs). phosphoramidon 77-91 endothelin converting enzyme 1 Rattus norvegicus 62-65 8401914-8 1993 Phosphoramidon (10 microM) or SQ-28,603 (100 microM) totally suppressed the degradation of [125I]-ET-1 by rNEP. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 98-102 8401914-8 1993 Phosphoramidon (10 microM) or SQ-28,603 (100 microM) totally suppressed the degradation of [125I]-ET-1 by rNEP. phosphoramidon 0-14 membrane metallo-endopeptidase Rattus norvegicus 106-110 8210514-1 1993 Intracisternal (ic) injection of the neutral endopeptidase-24.11 inhibitor phosphoramidon (1-100 nmol) produced a dose-dependent inhibition of gastric acid secretion in 2-h pylorus-ligated rats. phosphoramidon 75-89 membrane metallo-endopeptidase Rattus norvegicus 37-64 8210514-6 1993 Moreover, phosphoramidon-induced inhibition of acid was not reduced by the centrally effective bombesin antagonist N-acetyl-GRP(20-26)-O-CH3 or by reserpine pretreatment at a dose effective to antagonize ic neurotensin-induced inhibition in acid secretion. phosphoramidon 10-24 neurotensin Rattus norvegicus 207-218 8338128-3 1993 We therefore studied maximal binding capacity of 125I-labeled ET-1 in the presence or absence of the metalloprotease inhibitors phosphoramidon, which blocks the intracellular processing of Big ET-1 to ET-1, and thiorphan, which does not block this conversion. phosphoramidon 128-142 endothelin 1 Rattus norvegicus 193-197 8338128-3 1993 We therefore studied maximal binding capacity of 125I-labeled ET-1 in the presence or absence of the metalloprotease inhibitors phosphoramidon, which blocks the intracellular processing of Big ET-1 to ET-1, and thiorphan, which does not block this conversion. phosphoramidon 128-142 endothelin 1 Rattus norvegicus 193-197 8338128-4 1993 Phosphoramidon inhibited the release of ET-1 by human umbilical vein endothelial cells, rat aortic endothelial cells, and rat mesangial cells, and increased 1.4- to 17-fold the maximal binding capacity in the three types of cells. phosphoramidon 0-14 endothelin 1 Homo sapiens 40-44 8338128-6 1993 The increase in receptor binding by phosphoramidon was associated with an increase in the functional effect of ET-1, as measured by arachidonic acid release in rat mesangial cells. phosphoramidon 36-50 endothelin 1 Rattus norvegicus 111-115 7689402-15 1993 The facilitatory effect of phosphoramidon (10 microM) on PGS-induced contractions was inhibited by the selective NK1 receptor antagonist, GR71251 (1 microM). phosphoramidon 27-41 substance-P receptor Cavia porcellus 113-125 8335860-6 1993 Phosphoramidon (10(-5) mol/L) enhanced the inhibitory effect of NPY on EFS-induced contractions at 5 Hz. phosphoramidon 0-14 neuropeptide Y Homo sapiens 64-67 8335860-8 1993 Phosphoramidon (10(-5) mol/L) did not affect the frequency response to EFS, but enhanced the inhibitory effect of NPY (3 x 10(-7) mol/L) on frequency response to EFS, resulting in a significant increase in the mean logarithm of frequency that produced 50% of maximal contraction (NPY: 0.79 +/- 0.09 versus NPY plus phosphoramidon: 1.18 +/- 0.15, p < 0.05). phosphoramidon 0-14 neuropeptide Y Homo sapiens 114-117 8335860-8 1993 Phosphoramidon (10(-5) mol/L) did not affect the frequency response to EFS, but enhanced the inhibitory effect of NPY (3 x 10(-7) mol/L) on frequency response to EFS, resulting in a significant increase in the mean logarithm of frequency that produced 50% of maximal contraction (NPY: 0.79 +/- 0.09 versus NPY plus phosphoramidon: 1.18 +/- 0.15, p < 0.05). phosphoramidon 0-14 neuropeptide Y Homo sapiens 280-283 8335860-8 1993 Phosphoramidon (10(-5) mol/L) did not affect the frequency response to EFS, but enhanced the inhibitory effect of NPY (3 x 10(-7) mol/L) on frequency response to EFS, resulting in a significant increase in the mean logarithm of frequency that produced 50% of maximal contraction (NPY: 0.79 +/- 0.09 versus NPY plus phosphoramidon: 1.18 +/- 0.15, p < 0.05). phosphoramidon 0-14 neuropeptide Y Homo sapiens 280-283 8335860-8 1993 Phosphoramidon (10(-5) mol/L) did not affect the frequency response to EFS, but enhanced the inhibitory effect of NPY (3 x 10(-7) mol/L) on frequency response to EFS, resulting in a significant increase in the mean logarithm of frequency that produced 50% of maximal contraction (NPY: 0.79 +/- 0.09 versus NPY plus phosphoramidon: 1.18 +/- 0.15, p < 0.05). phosphoramidon 315-329 neuropeptide Y Homo sapiens 114-117 8518331-2 1993 In this study, we have examined the effects on the ET-1 pathway of 18 h exposure at 37 degrees C of cultured rat aortic smooth muscle cells to dexamethasone (DEX) and phosphoramidon. phosphoramidon 167-181 endothelin 1 Rattus norvegicus 51-55 8337517-5 1993 On the other hand, phosphoramidon and MERGAPTA, inhibitors of neutral endopeptidase and carboxypeptidase N, respectively, strengthened the effect of BK. phosphoramidon 19-33 kininogen 1 Canis lupus familiaris 149-151 8330216-6 1993 The histochemical staining in the transplants and the surrounding host tissue was completely blocked by a 100 nM concentration of the selective NEP inhibitors phosphoramidon or JHF-26, supporting the exclusive localization of NEP by this method. phosphoramidon 159-173 membrane metallo-endopeptidase Rattus norvegicus 144-147 8330216-6 1993 The histochemical staining in the transplants and the surrounding host tissue was completely blocked by a 100 nM concentration of the selective NEP inhibitors phosphoramidon or JHF-26, supporting the exclusive localization of NEP by this method. phosphoramidon 159-173 membrane metallo-endopeptidase Rattus norvegicus 226-229 8390257-3 1993 Inhibitors of angiotensin-converting enzyme (ACE; EC 3.4.15.1) and phosphoramidon, an inhibitor of neutral metalloendopeptidase (NEP; EC 3.4.24.11), were only partially effective in preventing BK degradation in semen. phosphoramidon 67-81 membrane metalloendopeptidase Homo sapiens 99-127 8489505-3 1993 In this paper, the presence of NEP in purified glomeruli from dog kidney was assessed by measuring phosphoramidon- and thiorphan-sensitive [D-Ala2,Leu5]enkephalin-degrading activity. phosphoramidon 99-113 membrane metalloendopeptidase Homo sapiens 31-34 7684296-10 1993 In the presence of phosphoramidon (10 microM), passive sensitization still increased significantly the amplitude of the contractile responses to SP and NKA including that to the maximal concentration given from 74 +/- 4% to 115 +/- 7% (n = 5, P<0.05) and from 104 +/- 9% to 146 +/- 16% (n = 5, P<0.05)of the maximal response to acetylcholine, respectively. phosphoramidon 19-33 tachykinin precursor 1 Homo sapiens 145-147 7684296-10 1993 In the presence of phosphoramidon (10 microM), passive sensitization still increased significantly the amplitude of the contractile responses to SP and NKA including that to the maximal concentration given from 74 +/- 4% to 115 +/- 7% (n = 5, P<0.05) and from 104 +/- 9% to 146 +/- 16% (n = 5, P<0.05)of the maximal response to acetylcholine, respectively. phosphoramidon 19-33 tachykinin precursor 1 Homo sapiens 152-155 7684296-12 1993 The relaxant response to the maximal concentration of VIP given in tissues precontracted with histamine (0.5 mM) was significantly reduced by passive sensitization from 41 +/- 4% to 25 +/- 3% (n = 5,P <0.05) of the amplitude of the precontraction in the absence of phosphoramidon and from 72 +/- 1%to 49 +/- 4% (n = 5, P<0.05) in the presence of phosphoramidon (10 microM). phosphoramidon 268-282 vasoactive intestinal peptide Homo sapiens 54-57 7684296-12 1993 The relaxant response to the maximal concentration of VIP given in tissues precontracted with histamine (0.5 mM) was significantly reduced by passive sensitization from 41 +/- 4% to 25 +/- 3% (n = 5,P <0.05) of the amplitude of the precontraction in the absence of phosphoramidon and from 72 +/- 1%to 49 +/- 4% (n = 5, P<0.05) in the presence of phosphoramidon (10 microM). phosphoramidon 352-366 vasoactive intestinal peptide Homo sapiens 54-57 7684296-13 1993 Passive sensitization significantly shifted to the right the CCRC for VIP as measured by the dose-ratios which were 10.4(95% CL: 6.6-14.1) and 6.4 (95% CL: 3.0-9.8) in the absence and in the presence of phosphoramidon,respectively.6. phosphoramidon 203-217 vasoactive intestinal peptide Homo sapiens 70-73 8395230-5 1993 The inhibitor of neutral endopeptidase, phosphoramidon (10(-8) mol/l), decreased the degradation of bradykinin in the supernatant of endothelial cells; the half-life of bradykinin was then increased from 29 +/- 1 to 46 +/- 2 minutes. phosphoramidon 40-54 kininogen 1 Homo sapiens 100-110 8395230-5 1993 The inhibitor of neutral endopeptidase, phosphoramidon (10(-8) mol/l), decreased the degradation of bradykinin in the supernatant of endothelial cells; the half-life of bradykinin was then increased from 29 +/- 1 to 46 +/- 2 minutes. phosphoramidon 40-54 kininogen 1 Homo sapiens 169-179 7683398-4 1993 The actions of the peptides were enhanced in the combined presence of phosphoramidon, captopril, and bestatin; the potency order remained NKA > SP > NKB. phosphoramidon 70-84 tachykinin precursor 3 Rattus norvegicus 155-158 8518331-5 1993 In contrast, phosphoramidon (100 microM) inhibited ET-1 production by 60%, up-regulated ET-1 receptors and potentiated ET-1-induced calcium mobilization by 75%. phosphoramidon 13-27 endothelin 1 Rattus norvegicus 51-55 8518331-5 1993 In contrast, phosphoramidon (100 microM) inhibited ET-1 production by 60%, up-regulated ET-1 receptors and potentiated ET-1-induced calcium mobilization by 75%. phosphoramidon 13-27 endothelin 1 Rattus norvegicus 88-92 8518331-5 1993 In contrast, phosphoramidon (100 microM) inhibited ET-1 production by 60%, up-regulated ET-1 receptors and potentiated ET-1-induced calcium mobilization by 75%. phosphoramidon 13-27 endothelin 1 Rattus norvegicus 88-92 8518331-6 1993 These results indicate that the regulatory effects of DEX and phosphoramidon on ET-1 receptors are mediated via ET-1 production by the cells. phosphoramidon 62-76 endothelin 1 Rattus norvegicus 80-84 8518331-6 1993 These results indicate that the regulatory effects of DEX and phosphoramidon on ET-1 receptors are mediated via ET-1 production by the cells. phosphoramidon 62-76 endothelin 1 Rattus norvegicus 112-116 8458433-3 1993 The lipoprotein ECE activity, which was optimal at pH 7.0, was inhibited by EDTA, o-phenanthroline, phosphoramidon, thiorphan, phenylmethanesulfonyl fluoride and chymostatin, but not by cysteine or aspartic proteinase inhibitors, suggesting metalloproteinase- and chymotrypsin-like properties. phosphoramidon 100-114 endothelin converting enzyme 1 Homo sapiens 16-19 8482675-6 1993 The effect of FMLP was significantly modified by cholinergic blockade (61.1 +/- 6.9) and by NEP inhibition (thiorphan 38.8 +/- 5.6, phosphoramidon 52.6 +/- 4.2). phosphoramidon 132-146 neprilysin Oryctolagus cuniculus 92-95 8449237-2 1993 injection of endothelin family peptides following administration of phosphoramidon in anesthetized Sprague-Dawley rats. phosphoramidon 68-82 endothelin 1 Homo sapiens 13-23 8449237-6 1993 The pressor response to big ET-1 60 min after phosphoramidon injection was attenuated by roughly 60% indicating a long inhibitory half-life. phosphoramidon 46-60 endothelin 1 Homo sapiens 28-32 8449237-7 1993 Very high doses of big ET-1 (> 20 mg/kg) were capable of over-riding the effect of phosphoramidon and produced characteristic pressor responses suggesting that the inhibition by phosphoramidon can be considered competitive in nature. phosphoramidon 86-100 endothelin 1 Rattus norvegicus 23-27 8449237-7 1993 Very high doses of big ET-1 (> 20 mg/kg) were capable of over-riding the effect of phosphoramidon and produced characteristic pressor responses suggesting that the inhibition by phosphoramidon can be considered competitive in nature. phosphoramidon 181-195 endothelin 1 Rattus norvegicus 23-27 8449237-9 1993 The pressor response to big ET-3 was also inhibited by phosphoramidon. phosphoramidon 55-69 endothelin 3 Rattus norvegicus 28-32 8449237-11 1993 These results are consistent with the idea that a phosphoramidon-sensitive endothelin-converting enzyme is capable of cleaving both big ET-1 and big ET-3 to the active peptides in the rat. phosphoramidon 50-64 endothelin 1 Rattus norvegicus 136-140 8449237-11 1993 These results are consistent with the idea that a phosphoramidon-sensitive endothelin-converting enzyme is capable of cleaving both big ET-1 and big ET-3 to the active peptides in the rat. phosphoramidon 50-64 endothelin 3 Rattus norvegicus 149-153 8448012-3 1993 The NEP inhibitors phosphoramidon and DL-thiorphan (1 microM) inhibited degradation of the substrate by gastric muscle membranes by 100% and by freshly dispersed gastric muscle cells by 55-60%. phosphoramidon 19-33 membrane metalloendopeptidase Homo sapiens 4-7 8448012-4 1993 The phosphoramidon or DL-thiorphan-inhibitable activity, attributed to NEP, of membranes was 112 +/- 4.0 pmol h-1 (micrograms protein)-1 and of cells was 4.2 +/- 0.8 nmol h-1 (10(6) cells)-1. phosphoramidon 4-18 membrane metalloendopeptidase Homo sapiens 71-74 8467870-0 1993 Big endothelin-1 and big endothelin-3 are constrictor agents in the microvasculature: evidence for the local phosphoramidon-sensitive conversion of big endothelin-1. phosphoramidon 109-123 endothelin 1 Rattus norvegicus 4-16 8467870-0 1993 Big endothelin-1 and big endothelin-3 are constrictor agents in the microvasculature: evidence for the local phosphoramidon-sensitive conversion of big endothelin-1. phosphoramidon 109-123 endothelin 3 Rattus norvegicus 25-37 8467870-0 1993 Big endothelin-1 and big endothelin-3 are constrictor agents in the microvasculature: evidence for the local phosphoramidon-sensitive conversion of big endothelin-1. phosphoramidon 109-123 endothelin 1 Rattus norvegicus 152-164 8467870-8 1993 Phosphoramidon (100 nmol) abolished constriction to big ET-1 (100 pmol) but not to ET-1 (10 pmol). phosphoramidon 0-14 endothelin 1 Rattus norvegicus 56-60 8467870-10 1993 Results suggest that a phosphoramidon-sensitive endothelin-converting enzyme situated close to microvascular vessels is important in the conversion of big ET-1. phosphoramidon 23-37 endothelin 1 Rattus norvegicus 155-159 8431480-3 1993 The metalloproteinase inhibitor phosphoramidon inhibited the conversion of big ET-1 into mature ET-1 both in vivo and in cultured endothelial cells, suggesting that ECE may be a neutral metalloproteinase. phosphoramidon 32-46 endothelin 1 Homo sapiens 79-83 8431480-3 1993 The metalloproteinase inhibitor phosphoramidon inhibited the conversion of big ET-1 into mature ET-1 both in vivo and in cultured endothelial cells, suggesting that ECE may be a neutral metalloproteinase. phosphoramidon 32-46 endothelin 1 Homo sapiens 96-100 8431480-3 1993 The metalloproteinase inhibitor phosphoramidon inhibited the conversion of big ET-1 into mature ET-1 both in vivo and in cultured endothelial cells, suggesting that ECE may be a neutral metalloproteinase. phosphoramidon 32-46 endothelin converting enzyme 1 Homo sapiens 165-168 8094056-0 1993 Big endothelin-3-induced hypertension and its inhibition by phosphoramidon in anaesthetized rats. phosphoramidon 60-74 endothelin 3 Rattus norvegicus 4-16 8094056-2 1993 The pressor effect induced by big ET-3 was markedly attenuated by pretreatment with phosphoramidon, 5 mg/kg i.v., a dose which had no effect on the hypertensive action induced by ET-3. phosphoramidon 84-98 endothelin 3 Rattus norvegicus 34-38 8406292-1 1993 The effect of phosphoramidon on the increase in pulmonary inflation pressure (PIP) induced by endothelin-1 (ET-1) administered by aerosol in ovalbumin (OA)-sensitized and challenged guinea-pigs was investigated after pretreatment or not of the animals with the neutral endopeptidase inhibitor, phosphoramidon, the cyclooxygenase inhibitor, indomethacin or the platelet activating factor (PAF) antagonist, BN 50730. phosphoramidon 14-28 endothelin-1 Cavia porcellus 94-106 8406292-1 1993 The effect of phosphoramidon on the increase in pulmonary inflation pressure (PIP) induced by endothelin-1 (ET-1) administered by aerosol in ovalbumin (OA)-sensitized and challenged guinea-pigs was investigated after pretreatment or not of the animals with the neutral endopeptidase inhibitor, phosphoramidon, the cyclooxygenase inhibitor, indomethacin or the platelet activating factor (PAF) antagonist, BN 50730. phosphoramidon 14-28 endothelin-1 Cavia porcellus 108-112 8406292-2 1993 When guinea-pigs were pretreated by phosphoramidon (0.1 mM, aerosol for 15 min), a significant enhancement of PIP was observed after administration of ET-1 (1 or 3 micrograms ml-1, aerosol for 2 min), whereas these doses of the peptide were only slightly active in control animals. phosphoramidon 36-50 endothelin-1 Cavia porcellus 151-155 8406292-9 1993 Moreover, this drug was moderately active in reducing the increase in PIP induced by ET-1, when the animals were pretreated by phosphoramidon. phosphoramidon 127-141 endothelin-1 Cavia porcellus 85-89 8406292-10 1993 These results suggest that a phosphoramidon-sensitive endopeptidase-like enzyme, present in the airway tissue modulates the effect of ET-1. phosphoramidon 29-43 endothelin-1 Cavia porcellus 134-138 7509942-2 1993 The tonic contraction to big ET-1 (10 nM) was markedly blocked by phosphoramidon (100 microM), which did not modify the response to an equipotent concentration of ET-1 (3 nM). phosphoramidon 66-80 endothelin 1 Rattus norvegicus 29-33 7509942-8 1993 Therefore, the rat uterus contains a phosphoramidon-sensitive, calcium-dependent endothelin-converting enzyme that readily converts big ET-1 into ET-1, which then contracts the myometrium via activation of ETA receptors. phosphoramidon 37-51 endothelin 1 Rattus norvegicus 136-140 7509942-8 1993 Therefore, the rat uterus contains a phosphoramidon-sensitive, calcium-dependent endothelin-converting enzyme that readily converts big ET-1 into ET-1, which then contracts the myometrium via activation of ETA receptors. phosphoramidon 37-51 endothelin 1 Rattus norvegicus 146-150 7510004-0 1993 Effects of phosphoramidon in endothelial cell cultures on the endogenous synthesis of endothelin-1 and on conversion of exogenous big endothelin-1 to endothelin-1. phosphoramidon 11-25 endothelin 1 Homo sapiens 86-98 7510004-1 1993 Several studies have shown that phosphoramidon (PHOS) reduces the release of endothelin-1 (ET-1) from cultured endothelial cells. phosphoramidon 32-46 endothelin 1 Homo sapiens 77-89 7510004-1 1993 Several studies have shown that phosphoramidon (PHOS) reduces the release of endothelin-1 (ET-1) from cultured endothelial cells. phosphoramidon 32-46 endothelin 1 Homo sapiens 91-95 7510004-1 1993 Several studies have shown that phosphoramidon (PHOS) reduces the release of endothelin-1 (ET-1) from cultured endothelial cells. phosphoramidon 48-52 endothelin 1 Homo sapiens 77-89 7510004-1 1993 Several studies have shown that phosphoramidon (PHOS) reduces the release of endothelin-1 (ET-1) from cultured endothelial cells. phosphoramidon 48-52 endothelin 1 Homo sapiens 91-95 7510004-6 1993 The concentrations of ET-1 accumulating in the medium over 24 h from BAECs were lowered by PHOS (-27% 10 microM, -76% 100 microM). phosphoramidon 91-95 endothelin 1 Homo sapiens 22-26 7510004-7 1993 In contrast, with EA.hy 926 cells, the same concentrations of PHOS increased by five- to sixfold the amount of ET-1 present in the medium after 24-h incubation. phosphoramidon 62-66 endothelin 1 Homo sapiens 111-115 7510004-8 1993 In other experiments, incubation of big ET-1 (1 microM) with intact BAECs or EA.hy 926 cells resulted in the generation of ET-1, and with both cell types this was inhibited by PHOS (IC50: BAECs = 6.4 microM; EA.hy 926 = 0.26 microM). phosphoramidon 176-180 endothelin 1 Homo sapiens 40-44 7510004-8 1993 In other experiments, incubation of big ET-1 (1 microM) with intact BAECs or EA.hy 926 cells resulted in the generation of ET-1, and with both cell types this was inhibited by PHOS (IC50: BAECs = 6.4 microM; EA.hy 926 = 0.26 microM). phosphoramidon 176-180 endothelin 1 Homo sapiens 123-127 7510006-0 1993 Phosphoramidon inhibits the conversion of big ET-1 into ET-1 in the pithed rat and in isolated perfused rat kidneys. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 46-50 7510006-0 1993 Phosphoramidon inhibits the conversion of big ET-1 into ET-1 in the pithed rat and in isolated perfused rat kidneys. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 56-60 7510006-2 1993 The aim of this study was to test the effects of the endothelin-converting enzyme (ECE) inhibitor phosphoramidon on pressor responses to ET-1 and its precursor, big ET-1, in isolated perfused rat kidneys and in pithed rats. phosphoramidon 98-112 endothelin converting enzyme 1 Rattus norvegicus 53-81 7510006-2 1993 The aim of this study was to test the effects of the endothelin-converting enzyme (ECE) inhibitor phosphoramidon on pressor responses to ET-1 and its precursor, big ET-1, in isolated perfused rat kidneys and in pithed rats. phosphoramidon 98-112 endothelin converting enzyme 1 Rattus norvegicus 83-86 7510006-2 1993 The aim of this study was to test the effects of the endothelin-converting enzyme (ECE) inhibitor phosphoramidon on pressor responses to ET-1 and its precursor, big ET-1, in isolated perfused rat kidneys and in pithed rats. phosphoramidon 98-112 endothelin 1 Rattus norvegicus 137-141 7510006-2 1993 The aim of this study was to test the effects of the endothelin-converting enzyme (ECE) inhibitor phosphoramidon on pressor responses to ET-1 and its precursor, big ET-1, in isolated perfused rat kidneys and in pithed rats. phosphoramidon 98-112 endothelin 1 Rattus norvegicus 165-169 7510006-4 1993 Phosphoramidon (10 microM) selectively inhibited the pressor responses to big ET-1 without altering those to ET-1, norepinephrine, angiotensin I (AT-I), or angiotensin II (AT-II). phosphoramidon 0-14 endothelin 1 Rattus norvegicus 78-82 7510006-4 1993 Phosphoramidon (10 microM) selectively inhibited the pressor responses to big ET-1 without altering those to ET-1, norepinephrine, angiotensin I (AT-I), or angiotensin II (AT-II). phosphoramidon 0-14 angiotensinogen Rattus norvegicus 172-177 7510006-7 1993 Phosphoramidon selectively inhibited the pressor responses to big ET-1 (ID50: 78 micrograms/kg/min) without affecting those to ET-1, AT-I, or AT-II. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 66-70 7510006-8 1993 These data illustrate that the pressor responses to big ET-1 in the rat, both in vivo and in vitro, are due to its conversion into ET-1 by a phosphoramidon-sensitive ECE. phosphoramidon 141-155 endothelin 1 Rattus norvegicus 56-60 7510006-8 1993 These data illustrate that the pressor responses to big ET-1 in the rat, both in vivo and in vitro, are due to its conversion into ET-1 by a phosphoramidon-sensitive ECE. phosphoramidon 141-155 endothelin 1 Rattus norvegicus 131-135 7510006-8 1993 These data illustrate that the pressor responses to big ET-1 in the rat, both in vivo and in vitro, are due to its conversion into ET-1 by a phosphoramidon-sensitive ECE. phosphoramidon 141-155 endothelin converting enzyme 1 Rattus norvegicus 166-169 7510006-9 1993 In the rat, phosphoramidon selectively inhibits ECE but not ACE both in vitro and in vivo. phosphoramidon 12-26 endothelin converting enzyme 1 Rattus norvegicus 48-51 7510007-0 1993 Pharmacologic evidence for the specificity of the phosphoramidon-sensitive endothelin-converting enzyme for big endothelin-1. phosphoramidon 50-64 endothelin 1 Rattus norvegicus 112-124 7510007-2 1993 In these models, big ET-1 consistently induced concentration- or dose-dependent pharmacologic effects sensitive to phosphoramidon (vasopressor or prostanoid-releasing effects). phosphoramidon 115-129 endothelin 1 Rattus norvegicus 21-25 7510007-5 1993 In this model, although big ET-1 induced a phosphoramidon-sensitive increase of the twitch response of the tissue to electrical stimulation, big ET-3, dissolved either in phosphate-buffered saline or acetic acid, remained inactive. phosphoramidon 43-57 endothelin 1 Rattus norvegicus 28-32 7510007-6 1993 Our results, presented in the above-mentioned models, illustrate the capacity of the phosphoramidon-sensitive endothelin-converting enzyme (ECE) to discriminate between human big ET-1 and big ET-3. phosphoramidon 85-99 endothelin converting enzyme 1 Homo sapiens 140-143 7510007-6 1993 Our results, presented in the above-mentioned models, illustrate the capacity of the phosphoramidon-sensitive endothelin-converting enzyme (ECE) to discriminate between human big ET-1 and big ET-3. phosphoramidon 85-99 endothelin 1 Rattus norvegicus 179-183 7510008-5 1993 The production of the C-terminal fragment of big ET-1 could be detected in this partially purified preparation and was inhibited by phosphoramidon (10 microM) but not by thiorphan (10 microM). phosphoramidon 132-146 endothelin-1 Sus scrofa 49-53 8355566-1 1993 Phosphoramidon inhibits both endothelin converting enzyme (ECE) and neutral metalloendopeptidase (NEP). phosphoramidon 0-14 endothelin converting enzyme 1 Rattus norvegicus 29-57 8355566-1 1993 Phosphoramidon inhibits both endothelin converting enzyme (ECE) and neutral metalloendopeptidase (NEP). phosphoramidon 0-14 endothelin converting enzyme 1 Rattus norvegicus 59-62 8355566-1 1993 Phosphoramidon inhibits both endothelin converting enzyme (ECE) and neutral metalloendopeptidase (NEP). phosphoramidon 0-14 membrane metallo-endopeptidase Rattus norvegicus 68-96 8355566-1 1993 Phosphoramidon inhibits both endothelin converting enzyme (ECE) and neutral metalloendopeptidase (NEP). phosphoramidon 0-14 membrane metallo-endopeptidase Rattus norvegicus 98-101 8355566-11 1993 In anesthetized normotensive rats, phosphoramidon (0.01-1.0 mg/kg/min x 30 min) dose-dependently inhibited the BP responses to big endothelin-1 (BET-1) without blocking the pressor responses to ET-1. phosphoramidon 35-49 endothelin 1 Rattus norvegicus 131-143 8355566-14 1993 It is concluded that the antihypertensive action of SCH 32615 and low doses of phosphoramidon can be attributed to the inhibition of NEP which may presumably cause an accumulation of ANF. phosphoramidon 79-93 membrane metallo-endopeptidase Rattus norvegicus 133-136 8355566-14 1993 It is concluded that the antihypertensive action of SCH 32615 and low doses of phosphoramidon can be attributed to the inhibition of NEP which may presumably cause an accumulation of ANF. phosphoramidon 79-93 natriuretic peptide A Rattus norvegicus 183-186 8341132-0 1993 Phosphoramidon-sensitive endothelin converting enzyme in cultured vascular smooth muscle cells converts big endothelin-3 to endothelin-3. phosphoramidon 0-14 endothelin 3 Homo sapiens 108-120 8341132-0 1993 Phosphoramidon-sensitive endothelin converting enzyme in cultured vascular smooth muscle cells converts big endothelin-3 to endothelin-3. phosphoramidon 0-14 endothelin 3 Homo sapiens 124-136 8341132-1 1993 Incubation of big endothelin-3 (big ET-3, 1-41) with the membrane fraction obtained from cultured vascular smooth muscle cells (VSMCs) resulted in time-dependent increases in immunoreactive-ET (IR-ET), which were suppressed by phosphoramidon. phosphoramidon 227-241 endothelin 3 Homo sapiens 18-30 8341132-1 1993 Incubation of big endothelin-3 (big ET-3, 1-41) with the membrane fraction obtained from cultured vascular smooth muscle cells (VSMCs) resulted in time-dependent increases in immunoreactive-ET (IR-ET), which were suppressed by phosphoramidon. phosphoramidon 227-241 endothelin 3 Homo sapiens 36-40 8341132-5 1993 This ET-3 generation from exogenously applied big ET-3 was also suppressed by phosphoramidon. phosphoramidon 78-92 endothelin 3 Homo sapiens 5-9 8341132-5 1993 This ET-3 generation from exogenously applied big ET-3 was also suppressed by phosphoramidon. phosphoramidon 78-92 endothelin 3 Homo sapiens 50-54 8341132-6 1993 We conclude that the phosphoramidon-sensitive ET converting enzyme in VSMCs converts big ET-1 and big ET-3 to their mature form. phosphoramidon 21-35 endothelin 1 Homo sapiens 89-106 1468574-0 1992 Effect of phosphoramidon on big endothelin-2 conversion into endothelin-2 in human renal adenocarcinoma (ACHN) cells. phosphoramidon 10-24 endothelin 2 Homo sapiens 32-44 1468574-0 1992 Effect of phosphoramidon on big endothelin-2 conversion into endothelin-2 in human renal adenocarcinoma (ACHN) cells. phosphoramidon 10-24 endothelin 2 Homo sapiens 61-73 1468574-4 1992 Phosphoramidon decreased the amount of ET-2 and increased that of big ET-2(1-38) dose-dependently. phosphoramidon 0-14 endothelin 2 Homo sapiens 39-43 1468574-4 1992 Phosphoramidon decreased the amount of ET-2 and increased that of big ET-2(1-38) dose-dependently. phosphoramidon 0-14 endothelin 2 Homo sapiens 70-74 1471681-7 1992 Phosphoramidon significantly inhibited the vasoconstrictor effect of big endothelin-1 (p < 0.039, paired t test). phosphoramidon 0-14 endothelin 1 Homo sapiens 73-85 1467845-0 1992 Phosphoramidon blocks big-endothelin-1 but not endothelin-1 enhancement of vascular permeability in the rat. phosphoramidon 0-14 endothelin 1 Homo sapiens 26-38 1467845-11 1992 Pretreatment with phosphoramidon (PA) blocked the response to big-ET-1 in all tissues examined but this inhibitor failed to alter the response to ET-1. phosphoramidon 18-32 endothelin 1 Rattus norvegicus 66-70 1467845-11 1992 Pretreatment with phosphoramidon (PA) blocked the response to big-ET-1 in all tissues examined but this inhibitor failed to alter the response to ET-1. phosphoramidon 34-36 endothelin 1 Rattus norvegicus 66-70 1467845-13 1992 We conclude from these results that the dose-dependent increase in vascular permeability induced by big-ET-1 in various tissues follows its conversion to ET-1 by the endothelin converting enzyme, a PA-sensitive process. phosphoramidon 198-200 endothelin 1 Rattus norvegicus 104-108 1467845-13 1992 We conclude from these results that the dose-dependent increase in vascular permeability induced by big-ET-1 in various tissues follows its conversion to ET-1 by the endothelin converting enzyme, a PA-sensitive process. phosphoramidon 198-200 endothelin 1 Rattus norvegicus 154-158 1469102-9 1992 In human fetal lung organ cultures, inhibition of CD10/NEP with either phosphoramidon or SCH32615 increases thymidine incorporation by 166-182% (P < 0.025). phosphoramidon 71-85 membrane metalloendopeptidase Homo sapiens 50-54 7509932-3 1993 In contrast, ET-1 and ET-3 almost equipotently inhibited forskolin-stimulated cAMP formation in bovine EC pretreated with phosphoramidon, a putative ET-1 converting-enzyme inhibitor. phosphoramidon 122-136 endothelin 1 Bos taurus 13-26 7509932-3 1993 In contrast, ET-1 and ET-3 almost equipotently inhibited forskolin-stimulated cAMP formation in bovine EC pretreated with phosphoramidon, a putative ET-1 converting-enzyme inhibitor. phosphoramidon 122-136 endothelin 1 Bos taurus 13-17 1362724-4 1992 Phosphoramidon (10(-5) M) significantly potentiated relaxations to low doses of VIP with no effect on i-NANC responses. phosphoramidon 0-14 vasoactive intestinal peptide Homo sapiens 80-83 1469102-9 1992 In human fetal lung organ cultures, inhibition of CD10/NEP with either phosphoramidon or SCH32615 increases thymidine incorporation by 166-182% (P < 0.025). phosphoramidon 71-85 membrane metalloendopeptidase Homo sapiens 55-58 1451739-0 1992 The vasoconstrictor action of big endothelin-1 is phosphoramidon-sensitive in rabbit saphenous artery, but not in saphenous vein. phosphoramidon 50-64 endothelin-1 Oryctolagus cuniculus 34-46 1333512-7 1992 In support of this observation, the inhibition of endopeptidase on adult polymorphonuclear neutrophils leukocytes by phosphoramidon was associated with an augmentation of chemotaxis to 10(-9) and 10(-10) mol/L fMLP. phosphoramidon 117-131 formyl peptide receptor 1 Homo sapiens 210-214 1469621-6 1992 Phosphoramidon (100 microM, endothelin-converting enzyme inhibitor) and BQ-123 (0.3 microM, ETA receptor antagonist) abolished the preischemic increase in coronary perfusion pressure induced by big ET-1 as well as its proischemic effect, whereas only BQ-123 abolished the cardiac effect of ET-1. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 198-202 1469621-6 1992 Phosphoramidon (100 microM, endothelin-converting enzyme inhibitor) and BQ-123 (0.3 microM, ETA receptor antagonist) abolished the preischemic increase in coronary perfusion pressure induced by big ET-1 as well as its proischemic effect, whereas only BQ-123 abolished the cardiac effect of ET-1. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 290-294 1475409-7 1992 Formation of the hydrolysis product was prevented by the NEP-24.11-inhibitor phosphoramidon (1 microM). phosphoramidon 77-91 membrane metallo-endopeptidase Rattus norvegicus 57-66 1451739-4 1992 Phosphoramidon (100 microM), a metalloproteinase inhibitor, antagonised the contractile action of big endothelin-1 in the artery but not in the vein. phosphoramidon 0-14 endothelin-1 Oryctolagus cuniculus 102-114 1504735-0 1992 Human brain contains a metalloprotease that converts big endothelin-1 to endothelin-1 and is inhibited by phosphoramidon and EDTA. phosphoramidon 106-120 endothelin 1 Homo sapiens 57-69 1281168-4 1992 Specifically, in tumor necrosis factor (TNF)-treated immunocytes, we demonstrate the effects of increased NEP expression on altering the stimulatory activities of the neuropeptides met-enkephalin, melanocyte-stimulating hormone and substance P. We demonstrate the significance of NEP in modulating these responses through the use of specific enzyme inhibitors such as phosphoramidon, thiorphan and captopril. phosphoramidon 368-382 tumor necrosis factor Homo sapiens 17-38 1281168-4 1992 Specifically, in tumor necrosis factor (TNF)-treated immunocytes, we demonstrate the effects of increased NEP expression on altering the stimulatory activities of the neuropeptides met-enkephalin, melanocyte-stimulating hormone and substance P. We demonstrate the significance of NEP in modulating these responses through the use of specific enzyme inhibitors such as phosphoramidon, thiorphan and captopril. phosphoramidon 368-382 tumor necrosis factor Homo sapiens 40-43 1281168-4 1992 Specifically, in tumor necrosis factor (TNF)-treated immunocytes, we demonstrate the effects of increased NEP expression on altering the stimulatory activities of the neuropeptides met-enkephalin, melanocyte-stimulating hormone and substance P. We demonstrate the significance of NEP in modulating these responses through the use of specific enzyme inhibitors such as phosphoramidon, thiorphan and captopril. phosphoramidon 368-382 membrane metalloendopeptidase Homo sapiens 106-109 1424102-1 1992 The s.c. administration of [Met5]-enkephalin to 10-day-old rats pretreated with the mixture of 3 peptidase inhibitors, amastatin, captopril and phosphoramidon, produced the inhibition of tail-flick response and loss of righting reflex. phosphoramidon 144-158 proenkephalin Rattus norvegicus 34-44 1426005-16 1992 We conclude that in the rat: (1) bigET-1 may affect RVR by both a direct effect and through phosphoramidon-sensitive conversion to ET-1; (2) the direct vasoconstrictor effect of bigET-1 might be expressed during endothelin-converting enzyme inhibition; (3) metalloproteases are involved in ET-1 degradation. phosphoramidon 92-106 endothelin 1 Rattus norvegicus 36-40 1426005-16 1992 We conclude that in the rat: (1) bigET-1 may affect RVR by both a direct effect and through phosphoramidon-sensitive conversion to ET-1; (2) the direct vasoconstrictor effect of bigET-1 might be expressed during endothelin-converting enzyme inhibition; (3) metalloproteases are involved in ET-1 degradation. phosphoramidon 92-106 endothelin 1 Rattus norvegicus 131-135 1422599-15 1992 Collectively, the results indicate that the haemodynamic effects of proendothelin-2 and -3 in vivo in conscious rats are probably due to their conversion to endothelin-2 and -3, respectively, by an enzyme(s) that is inhibited by phosphoramidon. phosphoramidon 229-243 endothelin 2 Rattus norvegicus 71-90 1398887-0 1992 Phosphoramidon-sensitive effects of big endothelins in the perfused rabbit kidney. phosphoramidon 0-14 endothelin 1 Homo sapiens 40-51 1398887-5 1992 A metalloprotease inhibitor, phosphoramidon (100 microM, 60 minutes), reduced the prostanoid release and pressor responses induced by big endothelin-1 and -2 without affecting the response induced by endothelin-1, -2, and -3. phosphoramidon 29-43 endothelin-1 Oryctolagus cuniculus 138-157 1398887-6 1992 These results suggest the presence of a phosphoramidon-sensitive endothelin converting enzyme that converts the precursors of endothelin-1 and -2, but not of endothelin-3, in the renal vasculature of the rabbit. phosphoramidon 40-54 endothelin-1 Oryctolagus cuniculus 126-145 1329092-4 1992 This value is in line with the concentrations obtained with [Met]enkephalin, tested in the presence of the specific neutral endopeptidase 24.11 inhibitor phosphoramidon, and this opioid"s synthetic analog [D-Ala2, Met5]enkephalin which, like [D-Ala2]deltorphin I, is resistant to proteolytic degradation. phosphoramidon 154-168 membrane metalloendopeptidase Homo sapiens 116-143 1516701-3 1992 Phosphoramidon, an inhibitor of neutral endopeptidase 24,11, almost completely suppressed the production of three fragments, but one fragment was not affected by the inhibitor. phosphoramidon 0-14 membrane metallo-endopeptidase Rattus norvegicus 32-59 1516701-4 1992 Analysis of N-terminal sequences of the degradation products revealed that the phosphoramidon-sensitive fragments were generated by cleavage at the Ser5-Leu6 bond of endothelin 1 that was identical with its cleavage site by purified rat endopeptidase 24,11, reported previously. phosphoramidon 79-93 endothelin 1 Rattus norvegicus 166-178 1528868-1 1992 A phosphoramidon-sensitive, membrane-bound metalloprotease that cleaves big endothelin 1 (big-ET-1) to ET-1 was obtained from human umbilical vein endothelial cells and also from bovine aortic endothelial cells by isolation of plasma-membrane vesicles free of lysosomes. phosphoramidon 2-16 endothelin 1 Homo sapiens 76-88 1528868-1 1992 A phosphoramidon-sensitive, membrane-bound metalloprotease that cleaves big endothelin 1 (big-ET-1) to ET-1 was obtained from human umbilical vein endothelial cells and also from bovine aortic endothelial cells by isolation of plasma-membrane vesicles free of lysosomes. phosphoramidon 2-16 endothelin 1 Homo sapiens 94-98 1528868-1 1992 A phosphoramidon-sensitive, membrane-bound metalloprotease that cleaves big endothelin 1 (big-ET-1) to ET-1 was obtained from human umbilical vein endothelial cells and also from bovine aortic endothelial cells by isolation of plasma-membrane vesicles free of lysosomes. phosphoramidon 2-16 endothelin 1 Homo sapiens 103-107 1400023-3 1992 Phosphoramidon significantly potentiated the endothelin-1-induced contraction in a concentration-dependent fashion in both guinea pig trachea and human bronchus, and it shifted the concentration-response curves to the left. phosphoramidon 0-14 endothelin-1 Cavia porcellus 45-57 1400023-6 1992 Phosphoramidon significantly potentiated the endothelin-1-induced contraction in the capsaicin-treated tissues, suggesting that endothelin-1 causes the contraction, at least in part, without releasing tachykinins. phosphoramidon 0-14 endothelin 1 Homo sapiens 45-57 1400023-6 1992 Phosphoramidon significantly potentiated the endothelin-1-induced contraction in the capsaicin-treated tissues, suggesting that endothelin-1 causes the contraction, at least in part, without releasing tachykinins. phosphoramidon 0-14 endothelin 1 Homo sapiens 128-140 1381726-7 1992 Lysylbradykinin was also degraded by NEP-24.11 (0.80 +/- 0.19 nmol/min per well); however, in the presence of phosphoramidon, AmM-mediated conversion to bradykinin (3.74 +/- 0.46 nmol/min per well) could be demonstrated. phosphoramidon 110-124 kininogen 1 Homo sapiens 5-15 1527713-0 1992 Phosphoramidon abolishes the increases in endothelin-1 release induced by ischemia-hypoxia in isolated perfused guinea pig lungs. phosphoramidon 0-14 endothelin-1 Cavia porcellus 42-54 7509998-4 1993 A major portion of phosphoramidon-sensitive ECE activity was distributed with a single peak at the approximately 1.05-1.2 M sucrose region, where it appeared to be cosedimented with membrane vesicles that contained the two different marker enzymes for Golgi apparatus. phosphoramidon 19-33 endothelin converting enzyme 1 Rattus norvegicus 44-47 7509999-7 1993 A number of studies have reported that the final processing step in ET-1 biosynthesis by the hypothetical endothelin-converting enzyme (ECE) is inhibited by phosphoramidon (PHOS). phosphoramidon 157-171 endothelin 1 Bos taurus 68-72 7509999-7 1993 A number of studies have reported that the final processing step in ET-1 biosynthesis by the hypothetical endothelin-converting enzyme (ECE) is inhibited by phosphoramidon (PHOS). phosphoramidon 157-171 endothelin converting enzyme 1 Homo sapiens 136-139 7509999-7 1993 A number of studies have reported that the final processing step in ET-1 biosynthesis by the hypothetical endothelin-converting enzyme (ECE) is inhibited by phosphoramidon (PHOS). phosphoramidon 173-177 endothelin 1 Bos taurus 68-72 7509999-7 1993 A number of studies have reported that the final processing step in ET-1 biosynthesis by the hypothetical endothelin-converting enzyme (ECE) is inhibited by phosphoramidon (PHOS). phosphoramidon 173-177 endothelin converting enzyme 1 Homo sapiens 136-139 7510001-7 1993 Phosphoramidon (10 microM) infused TK blocked (92 +/- 1% inhibition) the renal responses to bET-1 and reduced the overflow of ET-1-like material onto the tissues without affecting ET-1-induced renal vasoconstriction. phosphoramidon 0-14 endothelin-1 Oryctolagus cuniculus 93-97 7510001-7 1993 Phosphoramidon (10 microM) infused TK blocked (92 +/- 1% inhibition) the renal responses to bET-1 and reduced the overflow of ET-1-like material onto the tissues without affecting ET-1-induced renal vasoconstriction. phosphoramidon 0-14 endothelin-1 Oryctolagus cuniculus 126-130 7510001-8 1993 Incubation of bET-1 with rabbit renal cortical microsomes (100 micrograms protein) resulted in the generation of ET-1-like activity, as assessed by bioassay, which was inhibited by phosphoramidon (10 microM). phosphoramidon 181-195 endothelin-1 Oryctolagus cuniculus 15-19 1393287-8 1992 Incubation of human isolated bronchi with the NEP inhibitor phosphoramidon (10(-5) M) induced a rightward shift of the concentration-response curve induced by big ET-1 (10(-9) M to 3 x 10(-7) M). phosphoramidon 60-74 membrane metalloendopeptidase Homo sapiens 46-49 1393287-8 1992 Incubation of human isolated bronchi with the NEP inhibitor phosphoramidon (10(-5) M) induced a rightward shift of the concentration-response curve induced by big ET-1 (10(-9) M to 3 x 10(-7) M). phosphoramidon 60-74 endothelin 1 Homo sapiens 163-167 1393292-2 1992 It has been demonstrated previously that conversion of big endothelin-1 (bET-1) to endothelin-1 (ET-1) is inhibited in vitro and in vivo by phosphoramidon. phosphoramidon 140-154 endothelin 1 Rattus norvegicus 59-71 1393292-2 1992 It has been demonstrated previously that conversion of big endothelin-1 (bET-1) to endothelin-1 (ET-1) is inhibited in vitro and in vivo by phosphoramidon. phosphoramidon 140-154 endothelin 1 Rattus norvegicus 83-95 1393292-2 1992 It has been demonstrated previously that conversion of big endothelin-1 (bET-1) to endothelin-1 (ET-1) is inhibited in vitro and in vivo by phosphoramidon. phosphoramidon 140-154 endothelin 1 Rattus norvegicus 74-78 1393292-4 1992 Here we expand upon our previous observation that rat brain contains phosphoramidon-inhibitable endothelin converting enzyme (ECE) and show that this activity is not uniformly distributed throughout the brain. phosphoramidon 69-83 endothelin converting enzyme 1 Rattus norvegicus 126-129 1393292-10 1992 Washing of the pellet with KCl (1 M) and extraction with the detergent CHAPS (20 mM) revealed a phosphoramidon-inhibitable ECE within the residual particulate fraction (nominally classified as the cytoskeletal fraction). phosphoramidon 96-110 endothelin converting enzyme 1 Rattus norvegicus 123-126 1393292-14 1992 These data show that rat brain contains a phosphoramidon- and EDTA-inhibitable ECE which maybe similar to that present in endothelial cells. phosphoramidon 42-56 endothelin converting enzyme 1 Rattus norvegicus 79-82 1497648-1 1992 Experiments were conducted to determine the importance of the carbohydrate moiety of phosphoramidon in the inhibition of the pressor response to big endothelin-1 in anesthetized rats. phosphoramidon 85-99 endothelin 1 Rattus norvegicus 149-161 1497648-2 1992 Big endothelin-1 produced a 42% increase in mean arterial pressure which was nearly abolished by co-infusion of phosphoramidon. phosphoramidon 112-126 endothelin 1 Rattus norvegicus 4-16 1378731-4 1992 Transient transfection of COS-7 cells with the cloned preproET-3 cDNA resulted in the production of mature ET-3 and this production was inhibited by phosphoramidon, a metaloprotease inhibitor. phosphoramidon 149-163 endothelin 3 Rattus norvegicus 54-64 1378731-4 1992 Transient transfection of COS-7 cells with the cloned preproET-3 cDNA resulted in the production of mature ET-3 and this production was inhibited by phosphoramidon, a metaloprotease inhibitor. phosphoramidon 149-163 endothelin 3 Rattus norvegicus 60-64 1378731-5 1992 This suggested that a phosphoramidon sensitive mechanism was involved in the production of ET-3 in the transfected COS-7 cells. phosphoramidon 22-36 endothelin 3 Rattus norvegicus 91-95 1504735-0 1992 Human brain contains a metalloprotease that converts big endothelin-1 to endothelin-1 and is inhibited by phosphoramidon and EDTA. phosphoramidon 106-120 endothelin 1 Homo sapiens 73-85 1397024-7 1992 at the dose of 5 mg/kg, 5 min before the challenge, phosphoramidon almost totally inhibited the bronchoconstrictor and pressor responses induced by 10 nmol/kg big ET-1, whereas thiorphan (5 mg/kg) partially reduced the increase in PIP and exerted a minimal effect on the changes in MBP. phosphoramidon 52-66 endothelin-1 Cavia porcellus 163-167 1618346-0 1992 Phosphoramidon-sensitive endothelin-converting enzyme in vascular endothelial cells converts big endothelin-1 and big endothelin-3 to their mature form. phosphoramidon 0-14 endothelin 1 Homo sapiens 97-109 1618346-0 1992 Phosphoramidon-sensitive endothelin-converting enzyme in vascular endothelial cells converts big endothelin-1 and big endothelin-3 to their mature form. phosphoramidon 0-14 endothelin 3 Homo sapiens 118-130 1618346-2 1992 This increasing activity was markedly suppressed by phosphoramidon, which is known to inhibit the conversion of big ET-1(1-39) to ET-1(1-21). phosphoramidon 52-66 endothelin 1 Homo sapiens 116-120 1618346-2 1992 This increasing activity was markedly suppressed by phosphoramidon, which is known to inhibit the conversion of big ET-1(1-39) to ET-1(1-21). phosphoramidon 52-66 endothelin 1 Homo sapiens 130-134 1602404-14 1992 Furthermore, phosphoramidon (0.25 mg/kg/min x 30) abolished pressor response to big endothelin-1 (5 micrograms/kg, i.v.) phosphoramidon 13-27 endothelin 1 Rattus norvegicus 84-96 1629095-7 1992 Phosphoramidon, an inhibitor of metalloproteinase, suppressed the pressor effect of big ET-1 (P less than 0.01) and the increase in the concentration of ET-1 in the perfusate (P less than 0.05). phosphoramidon 0-14 endothelin-1 Oryctolagus cuniculus 88-92 1629095-7 1992 Phosphoramidon, an inhibitor of metalloproteinase, suppressed the pressor effect of big ET-1 (P less than 0.01) and the increase in the concentration of ET-1 in the perfusate (P less than 0.05). phosphoramidon 0-14 endothelin-1 Oryctolagus cuniculus 153-157 1504719-0 1992 Phosphoramidon potentiates the contractile response to endothelin-3, but not endothelin-1 in isolated airway tissue. phosphoramidon 0-14 endothelin 3 Homo sapiens 55-67 1507681-4 1992 We studied the effect of phosphoramidon on bronchoconstriction induced by ET-1. phosphoramidon 25-39 endothelin-1 Cavia porcellus 74-78 1507681-8 1992 Phosphoramidon potentiated ET-1 induced bronchoconstriction significantly. phosphoramidon 0-14 endothelin-1 Cavia porcellus 27-31 1507681-11 1992 sGaw, after inhalation of phosphoramidon, was significantly reduced when exposed to ET-1. phosphoramidon 26-40 endothelin-1 Cavia porcellus 84-88 1507681-12 1992 Phosphoramidon also potentiated ET-1 induced bronchoconstriction in vivo. phosphoramidon 0-14 endothelin-1 Cavia porcellus 32-36 1507681-15 1992 Phosphoramidon inhibited an analysis of ET-1. phosphoramidon 0-14 endothelin-1 Cavia porcellus 40-44 1504719-2 1992 Phosphoramidon (10 microM) markedly increased the contractile response to endothelin-3 in human and rabbit bronchus in vitro. phosphoramidon 0-14 endothelin 3 Homo sapiens 74-86 1504719-3 1992 In human tissue the contractile response to 0.3 microM endothelin-3 was significantly increased from 54 +/- 12% to 137 +/- 34% (of the response to 1 nM acetylcholine) in the presence of phosphoramidon. phosphoramidon 186-200 endothelin 3 Homo sapiens 55-67 1504719-16 1992 These results suggest that a phosphoramidon-sensitive enzyme (probably neutral endopeptidase) found in lung, may be responsible for local degradation of endothelin-3, but not endothelin-l in human and rabbit isolated bronchus. phosphoramidon 29-43 endothelin 3 Homo sapiens 153-165 1318210-5 1992 The neutral endopeptidase inhibitor phosphoramidon (1 microM) increased the potency of ANF-(5-27) in both epithelium-intact and epithelium-denuded guinea-pig tracheal rings. phosphoramidon 36-50 natriuretic peptide A Rattus norvegicus 87-90 1318210-6 1992 In contrast, removal of the epithelium from rat trachea, or pretreatment with phosphoramidon (1 microM) decreased relaxant responsiveness to ANF-(5-27). phosphoramidon 78-92 natriuretic peptide A Rattus norvegicus 141-144 1540181-2 1992 ECEs derived from these epithelial cells were very similar to the endothelial ECE in the following biochemical properties: 1) The optimum pH was 7.0; 2) the Km value for big ET-1 was approximately 30 microM; 3) the enzyme was potently inhibited by EDTA, o-phenanthroline and phosphoramidon; and 4) the enzyme did not convert big ET-2 or big ET-3. phosphoramidon 275-289 endothelin converting enzyme 1 Homo sapiens 0-3 1312017-3 1992 However, addition of phosphoramidon, an inhibitor of ET-converting enzyme, to the medium reduced the production of ET-1 and thus the receptors on HUVECs were made available for exogenously added [125I]ET-1. phosphoramidon 21-35 endothelin 1 Homo sapiens 115-119 1312017-3 1992 However, addition of phosphoramidon, an inhibitor of ET-converting enzyme, to the medium reduced the production of ET-1 and thus the receptors on HUVECs were made available for exogenously added [125I]ET-1. phosphoramidon 21-35 endothelin 1 Homo sapiens 201-205 1540181-2 1992 ECEs derived from these epithelial cells were very similar to the endothelial ECE in the following biochemical properties: 1) The optimum pH was 7.0; 2) the Km value for big ET-1 was approximately 30 microM; 3) the enzyme was potently inhibited by EDTA, o-phenanthroline and phosphoramidon; and 4) the enzyme did not convert big ET-2 or big ET-3. phosphoramidon 275-289 endothelin 1 Homo sapiens 174-178 1540181-3 1992 These data suggest that phosphoramidon-sensitive ECE is involved in the processing of big ET-1 to ET-1 in the renal tubule. phosphoramidon 24-38 endothelin converting enzyme 1 Homo sapiens 49-52 1540181-3 1992 These data suggest that phosphoramidon-sensitive ECE is involved in the processing of big ET-1 to ET-1 in the renal tubule. phosphoramidon 24-38 endothelin 1 Homo sapiens 90-102 1731782-6 1992 Phosphoramidon specifically inhibited the Big ET-1 pressor response. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 46-50 1377128-6 1992 However, with high concentrations of endothelins (greater than 10(-9) M, second stage of contraction), phosphoramidon was less potent than epithelium removal in enhancing the contractile responses. phosphoramidon 103-117 endothelin 1 Homo sapiens 37-48 1311412-3 1992 The latter but not the former activity was inhibited in a concentration-dependent manner by phosphoramidon (approximate IC50, 1 microM) and converted bET-1 to ET-1 at a rate of 0.6 nmol/hr/mg of protein. phosphoramidon 92-106 endothelin 1 Rattus norvegicus 151-155 1311412-6 1992 Within the rat brain, phosphoramidon-inhibitable conversion of bET-1 to ET-1 was detected principally in the cytoskeletal fraction, i.e., that fraction from the membrane that was not solubilized by detergent treatment. phosphoramidon 22-36 endothelin 1 Rattus norvegicus 64-68 1310003-9 1992 Both agents markedly inhibited the degradation of GRP, indicating that this process involves a lysosomal pathway and a phosphoramidon-sensitive pathway, possibly involving the EC 3.4.24.11 enzyme. phosphoramidon 119-133 gastrin releasing peptide Homo sapiens 50-53 1309957-4 1992 The conclusion that this alpha-MSH resulted from conversion of the parasite ACTH by neutral endopeptidase 24.11 (NEP) present on these cells was supported by the fact that the alpha-MSH level in the medium was markedly reduced by addition of the specific NEP inhibitor phosphoramidon. phosphoramidon 269-283 proopiomelanocortin Homo sapiens 25-34 1309957-4 1992 The conclusion that this alpha-MSH resulted from conversion of the parasite ACTH by neutral endopeptidase 24.11 (NEP) present on these cells was supported by the fact that the alpha-MSH level in the medium was markedly reduced by addition of the specific NEP inhibitor phosphoramidon. phosphoramidon 269-283 proopiomelanocortin Homo sapiens 76-80 1309957-4 1992 The conclusion that this alpha-MSH resulted from conversion of the parasite ACTH by neutral endopeptidase 24.11 (NEP) present on these cells was supported by the fact that the alpha-MSH level in the medium was markedly reduced by addition of the specific NEP inhibitor phosphoramidon. phosphoramidon 269-283 membrane metalloendopeptidase Homo sapiens 84-111 1309957-4 1992 The conclusion that this alpha-MSH resulted from conversion of the parasite ACTH by neutral endopeptidase 24.11 (NEP) present on these cells was supported by the fact that the alpha-MSH level in the medium was markedly reduced by addition of the specific NEP inhibitor phosphoramidon. phosphoramidon 269-283 membrane metalloendopeptidase Homo sapiens 113-116 1309957-4 1992 The conclusion that this alpha-MSH resulted from conversion of the parasite ACTH by neutral endopeptidase 24.11 (NEP) present on these cells was supported by the fact that the alpha-MSH level in the medium was markedly reduced by addition of the specific NEP inhibitor phosphoramidon. phosphoramidon 269-283 proopiomelanocortin Homo sapiens 176-185 1309958-4 1992 The addition to the incubation medium of phosphoramidon, a specific inhibitor of neutral endopeptidase 24.11, blocked inactivation of granulocytes by ACTH. phosphoramidon 41-55 proopiomelanocortin Homo sapiens 150-154 1596675-14 1992 ET-1-induced accumulation of [3H]-InsPs was not significantly affected by indomethacin (5 microM), nordihydroguaiaretic acid (NDGA, 10 microM), WEB 2086 (10 microM) or phosphoramidon (10 microM).4. phosphoramidon 168-182 endothelin 1 Rattus norvegicus 0-4 1579051-0 1992 Big endothelin-1-induced sudden death is inhibited by phosphoramidon in mice. phosphoramidon 54-68 endothelin 1 Mus musculus 4-16 1282965-7 1992 In all tissues studied, the ECE activity was significantly inhibited by phosphoramidon or ethylenediaminetetra-acetate. phosphoramidon 72-86 endothelin converting enzyme 1 Homo sapiens 28-31 1579051-4 1992 A metalloproteinase inhibitor, phosphoramidon, although failing to inhibit sudden death induced by ET-1, suppressed bET-1-induced lethality and elevation of plasma IR-ET-1 probably due to an inhibition of the enzymatic conversion of bET-1 to ET-1. phosphoramidon 31-45 endothelin 1 Mus musculus 117-121 1579051-4 1992 A metalloproteinase inhibitor, phosphoramidon, although failing to inhibit sudden death induced by ET-1, suppressed bET-1-induced lethality and elevation of plasma IR-ET-1 probably due to an inhibition of the enzymatic conversion of bET-1 to ET-1. phosphoramidon 31-45 endothelin 1 Mus musculus 117-121 1959670-0 1991 Phosphoramidon inhibits the generation of endothelin-1 from exogenously applied big endothelin-1 in cultured vascular endothelial cells and smooth muscle cells. phosphoramidon 0-14 endothelin 1 Homo sapiens 42-54 1755833-2 1991 The concentration of both big ET-1 and ET-1 was significantly increased in EA.hy 926 culture medium by phosphoramidon, a metalloproteinase inhibitor, suggesting that phosphoramidon sensitive protease(s) may be responsible for the degradation of ET-1 and big ET-1. phosphoramidon 103-117 endothelin 1 Homo sapiens 30-34 1755833-2 1991 The concentration of both big ET-1 and ET-1 was significantly increased in EA.hy 926 culture medium by phosphoramidon, a metalloproteinase inhibitor, suggesting that phosphoramidon sensitive protease(s) may be responsible for the degradation of ET-1 and big ET-1. phosphoramidon 103-117 endothelin 1 Homo sapiens 39-43 1755833-2 1991 The concentration of both big ET-1 and ET-1 was significantly increased in EA.hy 926 culture medium by phosphoramidon, a metalloproteinase inhibitor, suggesting that phosphoramidon sensitive protease(s) may be responsible for the degradation of ET-1 and big ET-1. phosphoramidon 103-117 endothelin 1 Homo sapiens 39-43 1755833-2 1991 The concentration of both big ET-1 and ET-1 was significantly increased in EA.hy 926 culture medium by phosphoramidon, a metalloproteinase inhibitor, suggesting that phosphoramidon sensitive protease(s) may be responsible for the degradation of ET-1 and big ET-1. phosphoramidon 103-117 endothelin 1 Homo sapiens 39-43 1815503-3 1991 The solubilized proteinase was capable of converting big ET-1 to ET-1 with an optimum pH of 6.5, and the conversion was dose-dependently suppressed by phosphoramidon (IC50 = 0.5 microM). phosphoramidon 151-165 endothelin 1 Rattus norvegicus 57-69 1953706-0 1991 Importance of the C-terminal region of big endothelin-1 for specific conversion by phosphoramidon-sensitive endothelin converting enzyme. phosphoramidon 83-97 endothelin 1 Homo sapiens 43-55 1953706-1 1991 Based on our previous findings that phosphoramidon-sensitive endothelin (ET) converting enzyme (ECE) converts human big ET-1 but does not big ET-3, we investigated structural requirement for substrate peptide. phosphoramidon 36-50 endothelin converting enzyme 1 Homo sapiens 96-99 1953706-1 1991 Based on our previous findings that phosphoramidon-sensitive endothelin (ET) converting enzyme (ECE) converts human big ET-1 but does not big ET-3, we investigated structural requirement for substrate peptide. phosphoramidon 36-50 endothelin 1 Homo sapiens 120-124 1797310-10 1991 Phosphoramidon (50 microM), a metalloprotease inhibitor, markedly reduced the eicosanoid releasing properties of big-ET-1 (n = 4, P less than 0.01) in guinea-pig perfused lungs without affecting the release stimulated by ET-1. phosphoramidon 0-14 endothelin 1 Homo sapiens 117-121 1797310-10 1991 Phosphoramidon (50 microM), a metalloprotease inhibitor, markedly reduced the eicosanoid releasing properties of big-ET-1 (n = 4, P less than 0.01) in guinea-pig perfused lungs without affecting the release stimulated by ET-1. phosphoramidon 0-14 endothelin 1 Homo sapiens 221-225 1959670-0 1991 Phosphoramidon inhibits the generation of endothelin-1 from exogenously applied big endothelin-1 in cultured vascular endothelial cells and smooth muscle cells. phosphoramidon 0-14 endothelin 1 Homo sapiens 84-96 1959670-5 1991 The apparent conversion of exogenously applied big ET-1 to ET-1 and its inhibition by phosphoramidon were observed using cultured VSMCs, although the enzyme inhibitor did not influence the basal secretion of IR-ET from VSMCs. phosphoramidon 86-100 endothelin 1 Homo sapiens 51-63 1872872-1 1991 Incubation of big endothelin-1 (big ET-1, 1-39) with the membrane fraction obtained from cultured vascular smooth muscle cells (VSMCs) resulted in an increase in immunoreactive-ET (IR-ET), which was inhibited by EDTA but not by phosphoramidon, a metalloproteinase inhibitor. phosphoramidon 228-242 endothelin 1 Homo sapiens 18-30 1766477-0 1991 Presence of a phosphoramidon-sensitive endothelin-converting enzyme which converts big-endothelin-1, but not big-endothelin-3, in the rat vas deferens. phosphoramidon 14-28 endothelin 1 Rattus norvegicus 87-99 1766477-6 1991 Treatment of the preparations with phosphoramidon (50 mumol/l) markedly reduced the twitch enhancement by big-ET-1 without affecting the response to ET-1. phosphoramidon 35-49 endothelin 1 Rattus norvegicus 110-114 1766477-7 1991 Our results suggest the presence of a specific phosphoramidon-sensitive endothelin-converting enzyme which converts big-ET-1 to ET-1 in the rat vas deferens. phosphoramidon 47-61 endothelin 1 Rattus norvegicus 120-124 1766477-7 1991 Our results suggest the presence of a specific phosphoramidon-sensitive endothelin-converting enzyme which converts big-ET-1 to ET-1 in the rat vas deferens. phosphoramidon 47-61 endothelin 1 Rattus norvegicus 128-132 1778905-7 1991 The endopeptidase inhibitors phosphoramidon and thiorphan (5 x 10(-6) M) potentiated the action of VIP. phosphoramidon 29-43 VIP peptides Cavia porcellus 99-102 1872872-1 1991 Incubation of big endothelin-1 (big ET-1, 1-39) with the membrane fraction obtained from cultured vascular smooth muscle cells (VSMCs) resulted in an increase in immunoreactive-ET (IR-ET), which was inhibited by EDTA but not by phosphoramidon, a metalloproteinase inhibitor. phosphoramidon 228-242 endothelin 1 Homo sapiens 36-40 1872872-6 1991 This ET-1 generation from exogenously applied big ET-1 was markedly inhibited by the addition of phosphoramidon, although the inhibitor did not influence the basal secretion of ET-1-like materials. phosphoramidon 97-111 endothelin 1 Homo sapiens 5-9 1872872-6 1991 This ET-1 generation from exogenously applied big ET-1 was markedly inhibited by the addition of phosphoramidon, although the inhibitor did not influence the basal secretion of ET-1-like materials. phosphoramidon 97-111 endothelin 1 Homo sapiens 50-54 1872872-6 1991 This ET-1 generation from exogenously applied big ET-1 was markedly inhibited by the addition of phosphoramidon, although the inhibitor did not influence the basal secretion of ET-1-like materials. phosphoramidon 97-111 endothelin 1 Homo sapiens 50-54 1782996-0 1991 Influence of thiorphan and phosphoramidon on the relaxant effect of vasoactive intestinal polypeptide and non-adrenergic non-cholinergic neurone stimulation in the rat gastric fundus. phosphoramidon 27-41 vasoactive intestinal peptide Rattus norvegicus 68-101 1912989-15 1991 6 The results are consistent with the involvement of phosphoramidon-sensitive enzyme systems in the conversion of human proendothelin [1-38] to endothelin-1 in vivo. phosphoramidon 53-67 endothelin 1 Homo sapiens 144-156 1788141-2 1991 125I-labeled endothelin-1 was degraded by both tissues in a phosphoramidon-sensitive way, suggesting a role of endopeptidase 24.11 in the in vitro metabolism of this peptide. phosphoramidon 60-74 endothelin 1 Homo sapiens 13-25 2069564-0 1991 Phosphoramidon inhibits the conversion of intracisternally administered big endothelin-1 to endothelin-1. phosphoramidon 0-14 endothelin 1 Canis lupus familiaris 76-88 2069564-0 1991 Phosphoramidon inhibits the conversion of intracisternally administered big endothelin-1 to endothelin-1. phosphoramidon 0-14 endothelin 1 Canis lupus familiaris 92-104 2069564-6 1991 All changes induced by big ET-1 were effectively prevented with phosphoramidon. phosphoramidon 64-78 endothelin 1 Canis lupus familiaris 27-31 1650147-4 1991 Simultaneous intravenous infusion of phosphoramidon (0.25 mg.kg-1.min-1), an inhibitor of metalloprotease activity including neutral endopeptidase EC 3.4.24.11 (NEP), completely prevented these effects of Big ET. phosphoramidon 37-51 membrane metallo-endopeptidase Rattus norvegicus 161-164 1647702-3 1991 Infusion of the NEP inhibitor phosphoramidon increased [ANP] and urine guanosine 3",5"-cyclic monophosphate (cGMP) excretion in both weanling and adult rats. phosphoramidon 30-44 membrane metallo-endopeptidase Rattus norvegicus 16-19 2059203-0 1991 Evidence for phosphoramidon-sensitive conversion of big endothelin-1 to endothelin-1 in isolated rat mesenteric artery. phosphoramidon 13-27 endothelin 1 Rattus norvegicus 56-68 2059203-0 1991 Evidence for phosphoramidon-sensitive conversion of big endothelin-1 to endothelin-1 in isolated rat mesenteric artery. phosphoramidon 13-27 endothelin 1 Rattus norvegicus 72-84 2059203-1 1991 The effect of phosphoramidon, a metalloproteinase inhibitor, on the pressor response to big endothelin-1 (big ET-1) in the isolated perfused rat mesenteric artery was examined. phosphoramidon 14-28 endothelin 1 Rattus norvegicus 92-104 2059203-1 1991 The effect of phosphoramidon, a metalloproteinase inhibitor, on the pressor response to big endothelin-1 (big ET-1) in the isolated perfused rat mesenteric artery was examined. phosphoramidon 14-28 endothelin 1 Rattus norvegicus 110-114 2059203-5 1991 Big ET-1 (5 X 10(-8) M)-induced pressor action was accompanied by an increase in immunoreactive (IR)-ET in the perfusate, and this increase was suppressed by the addition of phosphoramidon. phosphoramidon 174-188 endothelin 1 Rattus norvegicus 4-8 1650011-5 1991 The neutral endopeptidase inhibitor phosphoramidon (10(-5) M) potentiated the effect of VIP, so that the CBF dose-response curve for VIP was shifted to lower concentrations by 0.5 log U. phosphoramidon 36-50 VIP peptides Oryctolagus cuniculus 88-91 1650011-5 1991 The neutral endopeptidase inhibitor phosphoramidon (10(-5) M) potentiated the effect of VIP, so that the CBF dose-response curve for VIP was shifted to lower concentrations by 0.5 log U. phosphoramidon 36-50 VIP peptides Oryctolagus cuniculus 133-136 1650011-6 1991 The administration of VIP increased cyclic AMP levels in epithelial cells, an effect that was also potentiated by phosphoramidon. phosphoramidon 114-128 VIP peptides Oryctolagus cuniculus 22-25 1851748-4 1991 Inhibition of GRP degradation by human H345 cell membranes through the use of phenanthroline or phosphoramidon permitted the development of binding assays for the GRP receptor in detergent-solubilized crude membrane preparations. phosphoramidon 96-110 gastrin releasing peptide Homo sapiens 14-17 1710881-4 1991 Phosphoramidon (10(-7) to 10(-5) M) potentiated the substance P-induced contraction in a dose-dependent fashion, and phosphoramidon shifted the dose-response curve to lower concentrations. phosphoramidon 0-14 tachykinin precursor 1 Homo sapiens 52-63 1833101-10 1991 NEP activity in the rat kidney was inhibited by the specific NEP inhibitors (SCH39370, phosphoramidon and thiorphan) at micromolar concentrations. phosphoramidon 87-101 membrane metallo-endopeptidase Rattus norvegicus 0-3 1833101-10 1991 NEP activity in the rat kidney was inhibited by the specific NEP inhibitors (SCH39370, phosphoramidon and thiorphan) at micromolar concentrations. phosphoramidon 87-101 membrane metallo-endopeptidase Rattus norvegicus 61-64 2018520-2 1991 The hydrolysis of LHRH by pig kidney brush border membranes is inhibited by phosphoramidon (I50 = 5.6 nM) implicating endopeptidase-24.11 in the initiation of hydrolysis. phosphoramidon 76-90 gonadotropin-releasing hormone receptor Sus scrofa 18-22 2018530-3 1991 Specific [125I]-ET-1 (50 pM) binding (defined with 100 nM ET-1) to A10 cell membranes was increased in a concentration dependent manner by the selective NEP inhibitors thiorphan, phosphoramidon, and SQ 28,603 [(+/-)-N-[2-(mercaptomethyl)-1-oxo-3-phenylpropyl]-beta-alanine] with EC50 values of 9.4, 28.4, and 5.7 nM respectively. phosphoramidon 179-193 membrane metalloendopeptidase Homo sapiens 153-156 2018530-6 1991 Thiorphan, phosphoramidon, and SQ 28,603 inhibited A10 cell NEP activity with IC50 values of 5.3, 36.5, and 6.0 nM respectively, which was similar to values obtained with KNEP (3.6, 22.6, and 3.5 nM). phosphoramidon 11-25 membrane metalloendopeptidase Homo sapiens 60-63 2045432-8 1991 Inhibition of NEP in uterine strips with phosphoramidon resulted in a marked potentiation of oxytocin-induced contractions. phosphoramidon 41-55 membrane metallo-endopeptidase Rattus norvegicus 14-17 1991823-3 1991 Furthermore, since neutral endopeptidase 24.11 (enkephalinase; CD10/NEP) exists in invertebrate immunocyte membranes, we demonstrate that its specific inhibitor, phosphoramidon, potentiates the effects of the heptapeptide in inducing conformational change in both human and invertebrate granulocytes. phosphoramidon 162-176 membrane metalloendopeptidase Homo sapiens 19-46 1652635-3 1991 The tracheal relaxing activity of VIP was potentiated by enkephalinase inhibitors, thiorphan and phosphoramidon, while the activity of HDM was not potentiated. phosphoramidon 97-111 VIP peptides Cavia porcellus 34-37 1825449-2 1991 Addition of ANF but not [Tyr8]ANF-(5-27) decreased ciliary beat frequency in a dose-dependent fashion; the maximal decrease from the baseline value was 24.1 +/- 1.5% (+/- SE, P less than 0.001), and a half-maximal inhibitory concentration (IC50) was 3 x 10(-12) M. Inhibition of neutral endopeptidase activity by phosphoramidon (10(-6) M) or thiorphan (10(-6) M) potentiated the effect of ANF so that the dose-response curve for ANF was shifted to lower concentrations by approximately 0.5 log units (P less than 0.05, in each case). phosphoramidon 313-327 natriuretic peptides A Oryctolagus cuniculus 12-15 1825449-4 1991 The intracellular cGMP levels were increased by ANF, an effect that was further potentiated by phosphoramidon or thiorphan. phosphoramidon 95-109 natriuretic peptides A Oryctolagus cuniculus 48-51 1991823-3 1991 Furthermore, since neutral endopeptidase 24.11 (enkephalinase; CD10/NEP) exists in invertebrate immunocyte membranes, we demonstrate that its specific inhibitor, phosphoramidon, potentiates the effects of the heptapeptide in inducing conformational change in both human and invertebrate granulocytes. phosphoramidon 162-176 membrane metalloendopeptidase Homo sapiens 63-67 1991823-3 1991 Furthermore, since neutral endopeptidase 24.11 (enkephalinase; CD10/NEP) exists in invertebrate immunocyte membranes, we demonstrate that its specific inhibitor, phosphoramidon, potentiates the effects of the heptapeptide in inducing conformational change in both human and invertebrate granulocytes. phosphoramidon 162-176 membrane metalloendopeptidase Homo sapiens 68-71 1992461-6 1991 However, the metalloprotease inhibitors phosphoramidon and thiorphan dose-dependently inhibited the pressor response to big ET-1, although phosphoramidon was substantially more potent than thiorphan. phosphoramidon 139-153 endothelin 1 Rattus norvegicus 124-128 1992461-8 1991 In a rabbit lung membrane preparation, ECE activity was identified that was blocked by the metalloprotease inhibitors phosphoramidon and 1,10-phenanthroline in a concentration-dependent manner. phosphoramidon 118-132 endothelin converting enzyme 1 Rattus norvegicus 39-42 1993071-0 1991 Phosphoramidon inhibits the intracellular conversion of big endothelin-1 to endothelin-1 in cultured endothelial cells. phosphoramidon 0-14 endothelin 1 Homo sapiens 60-72 1993071-0 1991 Phosphoramidon inhibits the intracellular conversion of big endothelin-1 to endothelin-1 in cultured endothelial cells. phosphoramidon 0-14 endothelin 1 Homo sapiens 76-88 2206130-0 1990 Phosphoramidon, a metalloproteinase inhibitor, suppresses the secretion of endothelin-1 from cultured endothelial cells by inhibiting a big endothelin-1 converting enzyme. phosphoramidon 0-14 endothelin 1 Homo sapiens 75-87 1991995-3 1991 The enzymatic activity was characterized as NEP on the basis of the values of kinetic parameters (Km = 61 microM, Kcat = 1,692 min-1, and Kcat/Km = 28 min-1 microM-1) and the values of IC50 of two NEP inhibitors phosphoramidon and thiorphan (7.4 nM and 8.4 nM, respectively). phosphoramidon 212-226 membrane metalloendopeptidase Homo sapiens 44-47 1725435-5 1991 When cultured ECs were incubated with phosphoramidon, time-dependent secretion of ET-1 and CTF from the cells was markedly suppressed. phosphoramidon 38-52 endothelin 1 Rattus norvegicus 82-94 1725435-6 1991 In contrast, the secretion of big ET-1 was increased by phosphoramidon. phosphoramidon 56-70 endothelin 1 Rattus norvegicus 34-38 1725435-8 1991 Moreover, phosphoramidon potently inhibited the hypertensive effect of big ET-1 without affecting the ET-1-induced hypertension in anesthetized rats. phosphoramidon 10-24 endothelin 1 Rattus norvegicus 75-79 1725435-9 1991 From these findings, it seems reasonable to consider that phosphoramidon-sensitive and membrane-bound metalloproteinase, which is not a neutral endopeptidase 24.11, is the most plausible candidate for big ET-1-converting enzyme in vivo. phosphoramidon 58-72 endothelin 1 Rattus norvegicus 205-209 1826753-7 1991 The effect of big-ET-1[1-38], but not ET-1, was blocked by pretreatment with the enzyme inhibitor phosphoramidon (10 mg/kg, s.c., 30 min prior), implying that the big-ET-1[1-38] must first be enzymatically cleaved, presumably to ET-1, in order to elicit the abdominal constriction response. phosphoramidon 98-112 endothelin 1 Mus musculus 18-22 1875792-0 1991 Phosphoramidon prevents cerebral vasospasm following subarachnoid hemorrhage in dogs: the relationship to endothelin-1 levels in the cerebrospinal fluid. phosphoramidon 0-14 endothelin 1 Canis lupus familiaris 106-118 1875792-1 1991 There is increasing evidence that the conversion of big endothelin-1 (big ET-1) to endothelin-1 (ET-1) is specifically inhibited by the metalloproteinase inhibitor phosphoramidon. phosphoramidon 164-178 endothelin 1 Canis lupus familiaris 56-68 1875792-1 1991 There is increasing evidence that the conversion of big endothelin-1 (big ET-1) to endothelin-1 (ET-1) is specifically inhibited by the metalloproteinase inhibitor phosphoramidon. phosphoramidon 164-178 endothelin 1 Canis lupus familiaris 74-78 1875792-1 1991 There is increasing evidence that the conversion of big endothelin-1 (big ET-1) to endothelin-1 (ET-1) is specifically inhibited by the metalloproteinase inhibitor phosphoramidon. phosphoramidon 164-178 endothelin 1 Canis lupus familiaris 83-95 1875792-1 1991 There is increasing evidence that the conversion of big endothelin-1 (big ET-1) to endothelin-1 (ET-1) is specifically inhibited by the metalloproteinase inhibitor phosphoramidon. phosphoramidon 164-178 endothelin 1 Canis lupus familiaris 97-101 1943466-0 1991 Phosphoramidon inhibits the vasoconstrictor effects evoked by big endothelin-1 but not the elevation of plasma endothelin-1 in vivo. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 66-78 1943466-1 1991 Intravenous injections of big endothelin (ET)-1 (700 pmol/kg) in the pig increased arterial plasma levels of ET-1-like immunoreactivity (ET-1-LI) from 11.1 +/- 0.7 pM to 46.3 +/- 6.7 pM in the control situation and from 11.5 +/- 0.4 pM to 58.2 +/- 17 pM in the presence of the neutral endopeptidase inhibitor phosphoramidon (3 mg/kg). phosphoramidon 309-323 endothelin 1 Rattus norvegicus 30-40 1943480-0 1991 Functional evidence for the presence of a phosphoramidon-sensitive enzyme in rat brain that converts big endothelin-1 to endothelin-1. phosphoramidon 42-56 endothelin 1 Rattus norvegicus 105-117 1943480-0 1991 Functional evidence for the presence of a phosphoramidon-sensitive enzyme in rat brain that converts big endothelin-1 to endothelin-1. phosphoramidon 42-56 endothelin 1 Rattus norvegicus 121-133 1943480-7 1991 Pretreatment with phosphoramidon, a metalloprotease inhibitor (90 nmol), abolished the hemodynamic responses elicited by BigET-1 (MAP = -9 +/- 2%; RBF = -3 +/- 2%) but not those produced by ET-1. phosphoramidon 18-32 microtubule-associated protein 9 Rattus norvegicus 121-138 1943480-7 1991 Pretreatment with phosphoramidon, a metalloprotease inhibitor (90 nmol), abolished the hemodynamic responses elicited by BigET-1 (MAP = -9 +/- 2%; RBF = -3 +/- 2%) but not those produced by ET-1. phosphoramidon 18-32 endothelin 1 Rattus norvegicus 124-128 20504728-0 1991 Phosphoramidon potentiates the endothelin-1-induced bronchopulmonary response in guinea-pigs. phosphoramidon 0-14 endothelin-1 Cavia porcellus 31-43 20504728-1 1991 We investigated the effect of the endopeptidase-inhibitor, phosphoramidon, on the bronchopulmonary response induced by endothelin-1 in vivo or in isolated perfused lungs. phosphoramidon 59-73 endothelin-1 Cavia porcellus 119-131 20504728-3 1991 When awake animals were pretreated by an aerosol of phosphoramidon (0.1 mM, for 15 min), the bronchopulmonary response induced by 1 and 3 ?g/ml endothelin-1 was markedly enhanced. phosphoramidon 52-66 endothelin-1 Cavia porcellus 144-156 20504728-5 1991 Treatment of awake animals with an aerosol of phosphoramidon before lung recollection led to a significant potentiation of the endothelin-1-induced increase in pulmonary inflation pressure. phosphoramidon 46-60 endothelin-1 Cavia porcellus 127-139 20504728-6 1991 These results demonstrate that phosphoramidon potentiates the in vivo and in vitro bronchopulmonary response evoked by low doses of endothelin-1 and suggest that endopeptidase-like enzymes present in the airway tissue modulate the effect of the peptide. phosphoramidon 31-45 endothelin-1 Cavia porcellus 132-144 2174414-5 1990 Upon incubation of alpha-MSH with GLL-19 and G361 cell membranes, 3 degradation products were completely abolished in the presence of phosphoramidon. phosphoramidon 134-148 proopiomelanocortin Homo sapiens 19-28 2082818-5 1990 It exhibited optimal activity against Azocoll at pH 5 and 45 degrees C. It was stable at low pH and heat labile above 50 degrees C. It exhibited specificity toward peptide bonds formed by the amino group of hydrophobic amino acids (isoleucine, leucine, and phenylalanine) and its NH2-terminal amino acid sequence showed a high degree of similarity with that of Bacillus subtilis neutral metalloprotease A. Acidolysin is the first phosphoramidon-sensitive, acidic zinc metalloprotease reported. phosphoramidon 430-444 CA_C1293 Clostridium acetobutylicum ATCC 824 387-402 2082818-5 1990 It exhibited optimal activity against Azocoll at pH 5 and 45 degrees C. It was stable at low pH and heat labile above 50 degrees C. It exhibited specificity toward peptide bonds formed by the amino group of hydrophobic amino acids (isoleucine, leucine, and phenylalanine) and its NH2-terminal amino acid sequence showed a high degree of similarity with that of Bacillus subtilis neutral metalloprotease A. Acidolysin is the first phosphoramidon-sensitive, acidic zinc metalloprotease reported. phosphoramidon 430-444 CA_C1293 Clostridium acetobutylicum ATCC 824 468-483 1963889-6 1990 The reduction between 5 min and 4 h was not offset by an appreciable increase in the number of irregular neutrophils, unless NEP was inhibited by phosphoramidon. phosphoramidon 146-160 membrane metallo-endopeptidase Rattus norvegicus 125-128 1992461-0 1991 Phosphoramidon blocks the pressor activity of porcine big endothelin-1-(1-39) in vivo and conversion of big endothelin-1-(1-39) to endothelin-1-(1-21) in vitro. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 58-70 1992461-0 1991 Phosphoramidon blocks the pressor activity of porcine big endothelin-1-(1-39) in vivo and conversion of big endothelin-1-(1-39) to endothelin-1-(1-21) in vitro. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 108-120 1992461-0 1991 Phosphoramidon blocks the pressor activity of porcine big endothelin-1-(1-39) in vivo and conversion of big endothelin-1-(1-39) to endothelin-1-(1-21) in vitro. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 108-120 1992461-6 1991 However, the metalloprotease inhibitors phosphoramidon and thiorphan dose-dependently inhibited the pressor response to big ET-1, although phosphoramidon was substantially more potent than thiorphan. phosphoramidon 40-54 endothelin 1 Rattus norvegicus 124-128 1725321-3 1991 Phosphoramidon reduced the secretion of ET-1 and concomitantly enhanced the release of big ET-1 from cultured ECs. phosphoramidon 0-14 endothelin 1 Bos taurus 40-44 1725321-3 1991 Phosphoramidon reduced the secretion of ET-1 and concomitantly enhanced the release of big ET-1 from cultured ECs. phosphoramidon 0-14 endothelin 1 Bos taurus 91-95 1725347-0 1991 Human big endothelin releases prostacyclin in vivo and in vitro through a phosphoramidon-sensitive conversion to endothelin-1. phosphoramidon 74-88 endothelin 1 Homo sapiens 10-20 1725347-0 1991 Human big endothelin releases prostacyclin in vivo and in vitro through a phosphoramidon-sensitive conversion to endothelin-1. phosphoramidon 74-88 endothelin 1 Homo sapiens 113-125 1725347-10 1991 We further suggest that to induce the release of prostanoids in perfused lungs, human big ET needs to be converted to ET-1 by a phosphoramidon-sensitive endothelin-converting enzyme (ECE). phosphoramidon 128-142 endothelin 1 Homo sapiens 118-122 1725347-10 1991 We further suggest that to induce the release of prostanoids in perfused lungs, human big ET needs to be converted to ET-1 by a phosphoramidon-sensitive endothelin-converting enzyme (ECE). phosphoramidon 128-142 endothelin converting enzyme 1 Homo sapiens 153-181 1725347-10 1991 We further suggest that to induce the release of prostanoids in perfused lungs, human big ET needs to be converted to ET-1 by a phosphoramidon-sensitive endothelin-converting enzyme (ECE). phosphoramidon 128-142 endothelin converting enzyme 1 Homo sapiens 183-186 1725371-3 1991 In phosphoramidon-treated guinea pigs, ET-1 (5 micrograms/ml) exposure for 30 min evoked a slight but non-significant enhancement of the ACh-induced BR. phosphoramidon 3-17 endothelin-1 Cavia porcellus 39-43 1725374-2 1991 The formation of this ET-1-like activity from bET was partially inhibited by phosphoramidon (54 micrograms/ml), but not by pepstatin-A (1 microgram/ml), epoxysuccinyl-L-leucylamido(guanidino)butane (E-64, 10 micrograms/ml) or phenylmethylsulfonyl fluoride (PMSF, 25 micrograms/ml). phosphoramidon 77-91 endothelin 1 Homo sapiens 22-26 1709505-2 1990 Phosphoramidon (0.002-2.0 nmol), an endopeptidase-24.11 inhibitor, simultaneously injected with SP or NK A, remarkably enhanced and prolonged SP- or NK A-induced behavioural response in a dose-dependent manner. phosphoramidon 0-14 tachykinin 1 Mus musculus 102-106 1709505-2 1990 Phosphoramidon (0.002-2.0 nmol), an endopeptidase-24.11 inhibitor, simultaneously injected with SP or NK A, remarkably enhanced and prolonged SP- or NK A-induced behavioural response in a dose-dependent manner. phosphoramidon 0-14 tachykinin 1 Mus musculus 149-153 1709505-5 1990 When phosphoramidon was injected together with bestatin and captopril which have no significant effect alone, SP- or NK A-induced behavioral response was significantly increased. phosphoramidon 5-19 tachykinin 1 Mus musculus 117-121 2175178-4 1990 The degradation of BNP was significantly reduced by phosphoramidon (t1/2, 11.28 +/- 0.49 min) and captopril (t1/2, 6.99 +/- 0.34 min). phosphoramidon 52-66 natriuretic peptide B Rattus norvegicus 19-22 2241940-0 1990 Inhibition of biological actions of big endothelin-1 by phosphoramidon. phosphoramidon 56-70 endothelin 1 Rattus norvegicus 40-52 2241940-3 1990 Phosphoramidon blocked the vasoconstriction caused by 30 nM big ET-1, but was ineffective on the action of 0.3 nM ET-1. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 64-68 2241940-4 1990 Also in vivo, phosphoramidon had no effect on the ET-1-induced pressor actions, but blocked the pressor and airway-contractile responses to big ET-1 in rats and/or guinea pigs. phosphoramidon 14-28 endothelin 1 Rattus norvegicus 144-148 2241940-5 1990 Thus, it is likely that the vascular responses to exogenous big ET-1 are at least in part due to its conversion to ET-1 by a phosphoramidon-sensitive ET converting enzyme(s) in the vascular smooth muscle in vitro and in vivo. phosphoramidon 125-139 endothelin 1 Rattus norvegicus 64-68 2241940-5 1990 Thus, it is likely that the vascular responses to exogenous big ET-1 are at least in part due to its conversion to ET-1 by a phosphoramidon-sensitive ET converting enzyme(s) in the vascular smooth muscle in vitro and in vivo. phosphoramidon 125-139 endothelin 1 Rattus norvegicus 115-119 2206130-0 1990 Phosphoramidon, a metalloproteinase inhibitor, suppresses the secretion of endothelin-1 from cultured endothelial cells by inhibiting a big endothelin-1 converting enzyme. phosphoramidon 0-14 endothelin 1 Homo sapiens 140-152 2206130-1 1990 Time-dependent secretion of immunoreactive-endothelin (IR-ET) from cultured porcine aortic endothelial cells was markedly suppressed by phosphoramidon is due to proteinase inhibitor. phosphoramidon 136-150 endogenous retrovirus group K member 25 Homo sapiens 161-171 2206130-2 1990 Analysis of the culture supernatant with or without phosphoramidon by reverse-phase high performance liquid chromatography confirmed that the suppression of IR-ET secretion by phosphoramidon is due to a decreae in secretion of endothelin-1-like materials. phosphoramidon 176-190 endothelin 1 Homo sapiens 227-239 2206130-4 1990 These data strongly suggest that phosphoramidon suppresses the secretion of ET-1 from cultured endothelial cells by inhibiting the conversion of big ET-1 to ET-1. phosphoramidon 33-47 endothelin 1 Homo sapiens 76-80 2206130-4 1990 These data strongly suggest that phosphoramidon suppresses the secretion of ET-1 from cultured endothelial cells by inhibiting the conversion of big ET-1 to ET-1. phosphoramidon 33-47 endothelin 1 Homo sapiens 149-161 2226629-0 1990 Phosphoramidon, a metalloproteinase inhibitor, suppresses the hypertensive effect of big endothelin-1. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 89-101 1694188-3 1990 Enzyme staining was completely blocked by three potent NEP inhibitors (thiorphan, phosphoramidon, and JHF-26) at a concentration of 50 nM, supporting the specificity of this method to visualize sites of NEP activity selectively. phosphoramidon 82-96 membrane metallo-endopeptidase Rattus norvegicus 55-58 1694188-3 1990 Enzyme staining was completely blocked by three potent NEP inhibitors (thiorphan, phosphoramidon, and JHF-26) at a concentration of 50 nM, supporting the specificity of this method to visualize sites of NEP activity selectively. phosphoramidon 82-96 membrane metallo-endopeptidase Rattus norvegicus 203-206 2376002-6 1990 Phosphoramidon, thiorphan and metal ion chelators inhibited NEP-like activity of all the 3 tissues studied; other protease inhibitors, however, were ineffective. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 60-63 2187492-2 1990 The protease inhibitors aprotinin, leupeptin, phosphoramidon, and soybean trypsin inhibitors significantly potentiated the bronchodilator response to VIP. phosphoramidon 46-60 vasoactive intestinal peptide Homo sapiens 150-153 2476956-11 1989 In the presence of phosphoramidon, removal of the epithelium slightly enhanced the contractile responses to NKA and [Nle]NKA(4-10) but not to SP and NKB. phosphoramidon 19-33 tachykinin precursor 1 Homo sapiens 108-111 2695341-3 1989 Phosphoramidon potentiated responses to VIP in intact but not de-epithelialised preparations, and had no effect on i-NANC responses. phosphoramidon 0-14 VIP peptides Cavia porcellus 40-43 2482461-3 1989 Endopeptidase-24.11 (EC 3.4.24.11) purified from C6 cell membranes also cleaved SP at the same three peptide bonds in a manner sensitive to phosphoramidon. phosphoramidon 140-154 tachykinin precursor 1 Homo sapiens 80-82 2196967-6 1990 The supersensitivity to VIP, following epithelium removal was abolished by phosphoramidon or thiorphan (NEP inhibitors), but unaffected by captopril (an ACE inhibitor). phosphoramidon 75-89 VIP peptides Cavia porcellus 24-27 2375683-3 1990 The activity of NEP assessed by an NEP inhibitor phosphoramidon-sensitive Met5-enkephalin degrading activity was present in neutrophils (59.0 +/- 9.1 pmol/min 10(6) cells); however, the NEP activity was virtually absent in mononuclear cells, eosinophils and basophils. phosphoramidon 49-63 membrane metalloendopeptidase Homo sapiens 16-19 2375683-3 1990 The activity of NEP assessed by an NEP inhibitor phosphoramidon-sensitive Met5-enkephalin degrading activity was present in neutrophils (59.0 +/- 9.1 pmol/min 10(6) cells); however, the NEP activity was virtually absent in mononuclear cells, eosinophils and basophils. phosphoramidon 49-63 membrane metalloendopeptidase Homo sapiens 35-38 2375683-3 1990 The activity of NEP assessed by an NEP inhibitor phosphoramidon-sensitive Met5-enkephalin degrading activity was present in neutrophils (59.0 +/- 9.1 pmol/min 10(6) cells); however, the NEP activity was virtually absent in mononuclear cells, eosinophils and basophils. phosphoramidon 49-63 membrane metalloendopeptidase Homo sapiens 35-38 2138018-6 1990 Thus, we conclude that cultured bovine aortic endothelial cells produce a potentially novel phosphoramidon-insensitive metalloendopeptidase that removes the COOH-terminal tripeptide from 125I-hANF. phosphoramidon 92-106 HESX homeobox 1 Homo sapiens 192-196 1689554-2 1990 The tissues were placed in organ baths containing modified Krebs-Ringer solution, and isometric contractions to SP were monitored in the presence of phosphoramidon, an inhibitor of neutral endopeptidase (NEP). phosphoramidon 149-163 neprilysin Oryctolagus cuniculus 181-202 1689554-2 1990 The tissues were placed in organ baths containing modified Krebs-Ringer solution, and isometric contractions to SP were monitored in the presence of phosphoramidon, an inhibitor of neutral endopeptidase (NEP). phosphoramidon 149-163 neprilysin Oryctolagus cuniculus 204-207 2159651-6 1990 The neutral endopeptidase inhibitor phosphoramidon (5 x 10(-6) M) enhanced responses of NS to VIP but did not affect responses to NS in the absence of VIP. phosphoramidon 36-50 VIP peptides Cavia porcellus 94-97 2405705-9 1990 Metabolism of the aminopeptidase-resistant analogue [D-Ala2][Leu5]enkephalin by membranes was unaffected by amastatin and weakly inhibited by phosphoramidon affected by amastatin and weakly inhibited by phosphoramidon and captopril. phosphoramidon 142-156 proenkephalin Rattus norvegicus 66-76 2405705-9 1990 Metabolism of the aminopeptidase-resistant analogue [D-Ala2][Leu5]enkephalin by membranes was unaffected by amastatin and weakly inhibited by phosphoramidon affected by amastatin and weakly inhibited by phosphoramidon and captopril. phosphoramidon 203-217 proenkephalin Rattus norvegicus 66-76 1712001-2 1990 To determine whether NEP regulates SP-induced activation of human neutrophils, we examined the effect of the NEP inhibitor phosphoramidon on SP-induced superoxide generation and chemotaxis in human blood neutrophils. phosphoramidon 123-137 tachykinin precursor 1 Homo sapiens 141-143 1712001-5 1990 Thus, phosphoramidon (10(-6) M) shifted the dose-response curves of SP-induced superoxide generation and chemotaxis of the neutrophils to the left by 0.5-0.6 log. phosphoramidon 6-20 tachykinin precursor 1 Homo sapiens 68-70 1712001-6 1990 Phosphoramidon prevented the hydrolysis of SP by the neutrophils, the NEP activity of the neutrophils being assessed as 125 +/- 13 pmol of SP/min/10(6) cells. phosphoramidon 0-14 tachykinin precursor 1 Homo sapiens 43-45 1712001-6 1990 Phosphoramidon prevented the hydrolysis of SP by the neutrophils, the NEP activity of the neutrophils being assessed as 125 +/- 13 pmol of SP/min/10(6) cells. phosphoramidon 0-14 tachykinin precursor 1 Homo sapiens 139-141 8269939-1 1993 Phosphoramidon-sensitive endothelin-converting enzyme of bovine endothelial cells showed substrate selectivity for big endothelin-1 (ET-1) when compared to big ET-1(1-38), big ET-2(1-37), big ET-2(1-38) and big ET-3(1-41). phosphoramidon 0-14 endothelin 1 Bos taurus 119-131 8269939-1 1993 Phosphoramidon-sensitive endothelin-converting enzyme of bovine endothelial cells showed substrate selectivity for big endothelin-1 (ET-1) when compared to big ET-1(1-38), big ET-2(1-37), big ET-2(1-38) and big ET-3(1-41). phosphoramidon 0-14 endothelin 1 Bos taurus 133-137 8269939-1 1993 Phosphoramidon-sensitive endothelin-converting enzyme of bovine endothelial cells showed substrate selectivity for big endothelin-1 (ET-1) when compared to big ET-1(1-38), big ET-2(1-37), big ET-2(1-38) and big ET-3(1-41). phosphoramidon 0-14 endothelin 1 Bos taurus 160-164 8269939-1 1993 Phosphoramidon-sensitive endothelin-converting enzyme of bovine endothelial cells showed substrate selectivity for big endothelin-1 (ET-1) when compared to big ET-1(1-38), big ET-2(1-37), big ET-2(1-38) and big ET-3(1-41). phosphoramidon 0-14 endothelin 2 Bos taurus 176-180 8269939-1 1993 Phosphoramidon-sensitive endothelin-converting enzyme of bovine endothelial cells showed substrate selectivity for big endothelin-1 (ET-1) when compared to big ET-1(1-38), big ET-2(1-37), big ET-2(1-38) and big ET-3(1-41). phosphoramidon 0-14 endothelin 2 Bos taurus 192-196 2483550-3 1989 The enkephalinase (endopeptidase 24.11) inhibitor phosphoramidon (10(-5) M) potentiated the effect of SP (10(-7) M). phosphoramidon 50-64 tachykinin precursor 1 Homo sapiens 102-104 2593007-5 1989 The specificity of the method was demonstrated using the selective NEP inhibitors thiorphan, phosphoramidon, and JHF26. phosphoramidon 93-107 membrane metallo-endopeptidase Rattus norvegicus 67-70 2476956-11 1989 In the presence of phosphoramidon, removal of the epithelium slightly enhanced the contractile responses to NKA and [Nle]NKA(4-10) but not to SP and NKB. phosphoramidon 19-33 tachykinin precursor 1 Homo sapiens 121-124 2548762-2 1989 Relative to baseline values in rats with remnant kidneys, phosphoramidon led to elevations of plasma ANP levels and concomitant increases in urinary sodium excretion, fractional excretion of sodium, glomerular filtration rate, filtration fraction, and urinary cyclic GMP excretion. phosphoramidon 58-72 natriuretic peptide A Rattus norvegicus 101-104 2479934-7 1989 Intra-NTS injection of phosphoramidon, an inhibitor of endo 24.11 activity, completely blocked the effects of a subsequent injection of SP. phosphoramidon 23-37 tachykinin precursor 1 Homo sapiens 136-138 2554881-8 1989 The cleavage of CCK-8 and gastrin analogues was inhibited by ACE inhibitors (Captopril and EDTA), but not by other enzyme inhibitors (phosphoramidon, thiorphan, bestatin etc.). phosphoramidon 134-148 cholecystokinin Oryctolagus cuniculus 16-19 2554881-8 1989 The cleavage of CCK-8 and gastrin analogues was inhibited by ACE inhibitors (Captopril and EDTA), but not by other enzyme inhibitors (phosphoramidon, thiorphan, bestatin etc.). phosphoramidon 134-148 gastrin Oryctolagus cuniculus 26-33 2478526-5 1989 The peptidase activity of alpha 2 M-VVP complex was inhibited by low-molecular-weight inhibitors such as phosphoramidon, but IgG antibody against VVP failed to neutralize its peptidase activity. phosphoramidon 105-119 alpha-2-macroglobulin Homo sapiens 26-35 2531377-5 1989 Degradation of ANF was inhibited by EDTA and phosphoramidon. phosphoramidon 45-59 natriuretic peptide A Homo sapiens 15-18 2461706-1 1988 Hydrolysis of peptides by the phosphoramidon-insensitive rat kidney enzyme "endopeptidase-2" and by rat microvillar membranes. phosphoramidon 30-44 meprin A subunit alpha Rattus norvegicus 76-91 2521492-6 1989 The activity was blocked by two selective inhibitors of NEP, thiorphan and phosphoramidon. phosphoramidon 75-89 membrane metalloendopeptidase Homo sapiens 56-59 2521492-7 1989 CALLA antigen purified from the NALM-6 leukemic cell line by affinity to 44C10-IgG Sepharose retained a peptidase activity that was completely blocked by thiorphan and phosphoramidon. phosphoramidon 168-182 membrane metalloendopeptidase Homo sapiens 0-5 2531122-7 1989 This activity could be blocked by phosphoramidon, a specific inhibitor of NEP. phosphoramidon 34-48 membrane metalloendopeptidase Homo sapiens 74-77 2745298-4 1989 Phosphoramidon (10(-5) M) did not change resting tension but shifted the concentration-response curves to neurotensin to lower concentrations (P less than 0.001), whereas inhibitors of kininase II, aminopeptidases, serine proteases, and carboxypeptidase N were without effect. phosphoramidon 0-14 neurotensin/neuromedin N Cavia porcellus 106-117 2745298-5 1989 Removing the epithelium increased the contractile response to neurotensin (P less than 0.001), and phosphoramidon further increased the response to neurotensin in these tissues (P less than 0.001). phosphoramidon 99-113 neurotensin/neuromedin N Cavia porcellus 148-159 2558508-2 1989 Each kininase activity was determined by measuring the hydrolysis of bradykinin in the presence of specific inhibitors of kininase I (2-mercaptomethyl-3-guanidinoethylthiopropanoic acid), kininase II (captopril) and NEP (phosphoramidon) in 8 normal subjects. phosphoramidon 221-235 kininogen 1 Homo sapiens 69-79 2463769-2 1989 Leucine-thiorphan and phosphoramidon shifted the concentration-response curves of SP to lower concentrations in all tissues studied, but the sensitivity to SP was greater and the effect of leucine-thiorphan was less in the ferret, a finding that correlated with the observation that the ferret ileum contained substantially less NEP activity than rat ileum. phosphoramidon 22-36 membrane metallo-endopeptidase Rattus norvegicus 329-332 2464059-8 1989 NKA- and NKB-induced contractions were also enhanced significantly by phosphoramidon. phosphoramidon 70-84 tachykinin-3 Cavia porcellus 9-12 2601566-1 1989 The potencies of thiorphan and phosphoramidon as inhibitors of neutral endopeptidase 24.11 (NEP) are significantly affected by pH. phosphoramidon 31-45 membrane metallo-endopeptidase Rattus norvegicus 63-90 2601566-1 1989 The potencies of thiorphan and phosphoramidon as inhibitors of neutral endopeptidase 24.11 (NEP) are significantly affected by pH. phosphoramidon 31-45 membrane metallo-endopeptidase Rattus norvegicus 92-95 2601566-4 1989 NEP activity is readily inhibited by phosphoramidon upon mixing, while thiorphan becomes a more potent inhibitor only after preincubation with the enzyme. phosphoramidon 37-51 membrane metallo-endopeptidase Rattus norvegicus 0-3 2463981-8 1988 The tachykinin antagonist [D-Arg1,D-Pro2,D-Trp7,9,Leu11]-substance P abolished the effects of phosphoramidon on the atropine-resistant response to vagus nerve stimulation (2 Hz, P less than 0.005). phosphoramidon 94-108 arginase-1 Cavia porcellus 29-33 3259597-5 1988 IL-1 beta was protected by the presence in the incubation medium of phosphoramidon, a specific inhibitor of endopeptidase 24.11. phosphoramidon 68-82 interleukin 1 beta Homo sapiens 0-9 3288636-2 1988 This activity, present in plasma membrane-enriched fractions of neutrophil lysates, was also inhibited over 90% by phosphoramidon, an inhibitor of neutral endopeptidase (NEP, EC 3.4.24.11). phosphoramidon 115-129 membrane metalloendopeptidase Homo sapiens 147-168 3288636-2 1988 This activity, present in plasma membrane-enriched fractions of neutrophil lysates, was also inhibited over 90% by phosphoramidon, an inhibitor of neutral endopeptidase (NEP, EC 3.4.24.11). phosphoramidon 115-129 membrane metalloendopeptidase Homo sapiens 170-173 2448422-8 1988 Degradation of MBP in myelin membranes was partially inhibited by only 5-20% using leupeptin (20 microM) but up to 50% by dithiothreitol mM), phenylmethylsulphonyl fluoride (1 mM), and phosphoramidon (50 microM) but up to 50% by dithiothreitol (DDT, 10 mM). phosphoramidon 185-199 myelin basic protein Rattus norvegicus 15-18 2445957-2 1987 The calpain inhibitor leupeptin and the enkephalinase inhibitors thiorphan and phosphoramidon increased markedly SPLI overflow, whereas the two ACE inhibitors, captopril and enalaprilat (up to 10 microM in the superfusing medium), were inactive. phosphoramidon 79-93 membrane metallo-endopeptidase Rattus norvegicus 40-53 2969444-5 1988 Phosphoramidon, an inhibitor of endopeptidase, prevented the degradation of ANP in proximal convoluted tubule and glomerulus by 68% and 89%, respectively, but not in cortical thick ascending limb and cortical collecting tubule. phosphoramidon 0-14 natriuretic peptide A Homo sapiens 76-79 2966343-2 1988 Cleavage at this site represents the major ANF degradative activity in rat kidney, and is inhibited by the known metalloendoprotease inhibitors, thiorphan, phosphoramidon and zincov with IC50 values in the nanomolar range. phosphoramidon 156-170 natriuretic peptide A Rattus norvegicus 43-46 2980283-2 1988 This study investigated the effect of enkephalinase inhibition with phosphoramidon (10(-5) M) on contractile responses to neurokinin A, eledoisin, physalaemin and substance P in human isolated bronchial smooth muscle. phosphoramidon 68-82 tachykinin precursor 1 Homo sapiens 122-134 3117045-1 1987 Purification and properties of the phosphoramidon-insensitive endopeptidase ("endopeptidase-2") from rat kidney. phosphoramidon 35-49 meprin A subunit alpha Rattus norvegicus 78-94 3539055-1 1986 The effect of the enkephalinase inhibitor phosphoramidon on the withdrawal syndrome following acute and chronic morphine-induced physical dependence in mice, was investigated. phosphoramidon 42-56 membrane metallo endopeptidase Mus musculus 18-31 2878955-9 1987 Both the carboxypeptidase and aminopeptidase activities had neutral pH optima and were inhibited by o-phenanthroline, but were unaffected by inhibitors of neutral endopeptidases (phosphoramidon) or angiotensin-converting enzyme (Captopril). phosphoramidon 179-193 carboxypeptidase Q Homo sapiens 30-44 3443423-10 1987 It is concluded that bestatin and phosphoramidon, injected into the carotid artery, inhibit the activity of aminopeptidase and "enkephalinase", thus producing an accumulation of enkephalins in the central nervous system. phosphoramidon 34-48 membrane metallo-endopeptidase Rattus norvegicus 127-142 2826799-3 1987 The enzymatic preparation from membranes is inhibited by low concentrations of the ACE inhibitors, SQ 14225 and SQ 20881 (IC50 of 0.6 and 15 nM, respectively), and is weakly inhibited by the neutral endopeptidase inhibitors, phosphoramidon and thiorphan (IC50 of 30 microM and ca. phosphoramidon 225-239 angiotensin I converting enzyme Rattus norvegicus 83-86 2877660-4 1986 When Leu-enkephalin was the substrate, however, the effects of phosphoramidon and bestatin were marked and those of N-ethylmaleimide and diisopropylphosphorofluoridate were negligibly small. phosphoramidon 63-77 prodynorphin Mus musculus 5-19 3548829-5 1987 Formation of neurotensin-(1-11) and -(1-10) was completely inhibited by phosphoramidon (Ki = 6 nM), an inhibitor of endopeptidase 24.11, but not by captopril, an inhibitor of peptidyl dipeptidase A. Incubation of neurotensin with purified endopeptidase 24.11 from pig stomach also resulted in cleavage of the Tyr-11-Ile-12 and Pro-10-Tyr-11 bonds. phosphoramidon 72-86 neurotensin Homo sapiens 13-24 3548829-5 1987 Formation of neurotensin-(1-11) and -(1-10) was completely inhibited by phosphoramidon (Ki = 6 nM), an inhibitor of endopeptidase 24.11, but not by captopril, an inhibitor of peptidyl dipeptidase A. Incubation of neurotensin with purified endopeptidase 24.11 from pig stomach also resulted in cleavage of the Tyr-11-Ile-12 and Pro-10-Tyr-11 bonds. phosphoramidon 72-86 neurotensin Sus scrofa 213-224 3548429-8 1987 [3H]LHRH was cleaved by BBM or by endopeptidase-24.11 from porcine PT to metabolites 2, 4, small amounts of 3, and less than Glu-His-Trp-Ser-Tyr-Gly, but cleavage was strongly inhibited by the specific inhibitor phosphoramidon. phosphoramidon 212-226 gonadotropin releasing hormone 1 Rattus norvegicus 4-8 3540390-3 1986 Additionally, the enkephalin-hydrolyzing aminopeptidase, endopeptidase-24.11 and peptidyl dipeptidase A in rat vas deferens were found to be inhibited maximally with 1 microM of amastatin, 1 microM of phosphoramidon and 1 microM of captopril, respectively. phosphoramidon 201-215 proenkephalin Rattus norvegicus 18-28 2412213-2 1985 GRP10 was catabolized by gastric muscle peptidases (specific activity 1.8 nmol min-1 mg-1 protein) by hydrolysis of the His8-Leu9 bond and catabolism was inhibited by phosphoramidon (I50 approx. phosphoramidon 167-181 gastrin releasing peptide Homo sapiens 0-5 3532054-8 1986 In contrast, the formation of YGG was completely prevented by Thiorphan (IC50 value = 9 nM) and phosphoramidon, two inhibitors of "enkephalinase" (EC 3.4.24.11; membrane metallo-endopeptidase), thus identifying the latter as the YGG-forming enzyme. phosphoramidon 96-110 membrane metallo-endopeptidase Rattus norvegicus 131-145 3090452-1 1986 Both the MAO-B inhibitor deprenyl (2.5-10 mg/kg, ip, 60 min prior) and the MAO-B substrate beta-phenylethylamine (PEA, 40 micrograms, icv) potentiated the analgesic action of the enkephalinase inhibitor phosphoramidon (250 micrograms, icv) in animals allowed normal sleep. phosphoramidon 203-217 monoamine oxidase B Rattus norvegicus 75-80 2995126-5 1985 A combination of phosphoramidon and bestatin abolished the hydrolysis of neurokinin B by synaptic membranes. phosphoramidon 17-31 tachykinin precursor 3 Sus scrofa 73-85 3901041-1 1985 Intraventricular administration of enkephalinase inhibitor, phosphoramidon (1 X 10(-8)-5.6 X 10(-7) moles ICV) induced a behavioural syndrome consisting of excessive grooming with the body scratching as the most prominent symptom and wet-dog-shakes (WDS). phosphoramidon 60-74 membrane metallo-endopeptidase Rattus norvegicus 35-48 3957894-2 1986 The inhibitor constant of PLT, Ki, and the dissociation constant of thermolysin(E)-PLT(I) complex, Kd, are found to be smaller by a factor of 4 to 300, depending on pH, resulting in stronger binding, than those of talopeptin and phosphoramidon, but all of them show similar pH dependence. phosphoramidon 229-243 N-acylethanolamine acid amidase Homo sapiens 26-29 3957894-2 1986 The inhibitor constant of PLT, Ki, and the dissociation constant of thermolysin(E)-PLT(I) complex, Kd, are found to be smaller by a factor of 4 to 300, depending on pH, resulting in stronger binding, than those of talopeptin and phosphoramidon, but all of them show similar pH dependence. phosphoramidon 229-243 N-acylethanolamine acid amidase Homo sapiens 83-86 3123978-1 1986 Enkephalinase inhibitors phosphoramidon, thiorphan or phelorphan suppressed naloxone-precipitated withdrawal symptoms in acute and chronic morphine dependent mice and rats. phosphoramidon 25-39 membrane metallo endopeptidase Mus musculus 0-13 3909153-3 1985 These cells cleaved the NEP substrate glutaryl (Glut)-Ala-Ala-Phe-(4-methoxynaphthylamine) (Glut-Ala-Ala-Phe-MNA) at a rate of 9.5 nmol X hr-1 per 10(6) cells, and phosphoramidon (1 microM) inhibited the hydrolysis by 90%. phosphoramidon 164-178 membrane metalloendopeptidase Homo sapiens 24-27 3909153-6 1985 A washed membrane fraction from human neutrophils rapidly cleaved 0.5 mM Glut-Ala-Ala-Phe-MNA (96 nmol X min-1 X mg-1) and the hydrolysis was inhibited by phosphoramidon and by specific antiserum to human renal NEP. phosphoramidon 155-169 membrane metalloendopeptidase Homo sapiens 211-214 3909153-8 1985 The membrane-bound enzyme cleaved the peptide substrates at the same site as the homogeneous human renal NEP, and phosphoramidon and thiorphan inhibited the hydrolysis. phosphoramidon 114-128 membrane metalloendopeptidase Homo sapiens 105-108 2409961-6 1985 Synaptic membrane preparations from human striatum and diencephalon hydrolysed substance P at the same sites as did preparations of pig striatal synaptic membranes, and hydrolysis was substantially abolished by phosphoramidon. phosphoramidon 211-225 tachykinin precursor 1 Homo sapiens 79-90 2412213-2 1985 GRP10 was catabolized by gastric muscle peptidases (specific activity 1.8 nmol min-1 mg-1 protein) by hydrolysis of the His8-Leu9 bond and catabolism was inhibited by phosphoramidon (I50 approx. phosphoramidon 167-181 CD59 molecule (CD59 blood group) Homo sapiens 79-89 2412213-2 1985 GRP10 was catabolized by gastric muscle peptidases (specific activity 1.8 nmol min-1 mg-1 protein) by hydrolysis of the His8-Leu9 bond and catabolism was inhibited by phosphoramidon (I50 approx. phosphoramidon 167-181 CD7 molecule Homo sapiens 125-129 2412213-4 1985 The same bond in GRP10 was cleaved by purified endopeptidase-24.11, and hydrolysis was equally sensitive to inhibition by phosphoramidon. phosphoramidon 122-136 gastrin releasing peptide Homo sapiens 17-22 2412213-7 1985 It is concluded that a membrane-bound peptidase in the stomach wall catabolizes and inactivates GRP10 and SP and that, in its specificity and sensitivity to phosphoramidon, this peptidase resembles endopeptidase-24.11. phosphoramidon 157-171 gastrin releasing peptide Homo sapiens 96-101 2412213-7 1985 It is concluded that a membrane-bound peptidase in the stomach wall catabolizes and inactivates GRP10 and SP and that, in its specificity and sensitivity to phosphoramidon, this peptidase resembles endopeptidase-24.11. phosphoramidon 157-171 tachykinin precursor 1 Homo sapiens 106-108 2409262-6 1985 The degradation of porcine insulin in subcutaneous tissue was inhibited by bacitracin, leupeptin, phosphoramidon, and Z-Gly-Pro-Leu-Gly, though the human insulin degradation was not. phosphoramidon 98-112 insulin Homo sapiens 27-34 6617101-3 1983 Dipeptidyl peptidase IV activity of human renal microvilli could be inhibited by di-isopropylphosphorofluoridate and neutral endopeptidase activity by phosphoramidon. phosphoramidon 151-165 dipeptidyl peptidase 4 Homo sapiens 0-23 6395608-2 1984 Both N2O (70% in 30% O2) and the relatively selective enkephalinase inhibitor phosphoramidon (350 micrograms i.c.v. phosphoramidon 78-92 membrane metallo-endopeptidase Rattus norvegicus 54-67 6395608-5 1984 The rapidly developed tolerance to N2O analgesia does not affect the anaesthetic state since the animals remained motionless for the duration of exposure lasting 3 h. In the animals treated with the enkephalinase inhibitor phosphoramidon, no development of tolerance to N2O-antinociception occurred during the exposure lasting 3 h. The results indicate that tolerance to N2O analgesia can be abolished by activation of the enkephalinergic system, which might suggest a possible insufficiency of this system during tolerance to N2O. phosphoramidon 223-237 membrane metallo-endopeptidase Rattus norvegicus 199-212 6433386-1 1984 In order to elucidate the relationship between REM sleep and the enkephalinergic system, the effects of REM sleep deprivation (REMSD), stress and the enkephalinase inhibitor phosphoramidon on handling-induced convulsions were studied in mice. phosphoramidon 174-188 membrane metallo endopeptidase Mus musculus 150-163 6190172-2 1983 The hydrolysis of an enkephalin analogue (Tyr-D-Ala-Gly-Phe-Leu) at the Gly-Phe bond was completely inhibited by phosphoramidon. phosphoramidon 113-127 proenkephalin Sus scrofa 21-31 33917140-11 2021 The ECE inhibitor phosphoramidon induced autophagy. phosphoramidon 18-32 endothelin converting enzyme 1 Homo sapiens 4-7 7052059-4 1982 The hydrolysis of the Gly3-Phe4 bond of Leu-enkephalin by synaptic membranes prepared from pig brain was partially inhibited by phosphoramidon and thiorphan. phosphoramidon 128-142 proenkephalin Sus scrofa 44-54 33917140-12 2021 Furthermore, phosphoramidon inhibited ER stress and the NLRP3 inflammasome in tubular epithelial cells. phosphoramidon 13-27 NLR family pyrin domain containing 3 Homo sapiens 56-61 33917140-13 2021 In an adenine diet-induced CKD mouse model, phosphoramidon attenuated the progression of CKD by regulating autophagy, the NLRP3 inflammasome and ER stress. phosphoramidon 44-58 NLR family, pyrin domain containing 3 Mus musculus 122-127 31077356-7 2019 177 Lu-DOTAGA-PEG2 -RM26 demonstrated quantitative labeling yield at high molar activity (450 GBq/mumol), high in vivo stability (5 min pi >98% of radioligand remained when coinjected with phosphoramidon), high affinity to GRPR (KD = 0.4 +- 0.2 nM), and favorable biodistribution (1 hr pi tumor uptake was higher than in healthy tissues, including the kidneys). phosphoramidon 192-206 insulin-like growth factor 2 Mus musculus 14-18 33256013-2 2020 Treatment of mice with the neprilysin (NEP)-inhibitor phosphoramidon was previously shown to improve the metabolic stability and tumor uptake of biodegradable radiopeptides. phosphoramidon 54-68 membrane metallo endopeptidase Mus musculus 27-37 33256013-2 2020 Treatment of mice with the neprilysin (NEP)-inhibitor phosphoramidon was previously shown to improve the metabolic stability and tumor uptake of biodegradable radiopeptides. phosphoramidon 54-68 membrane metallo endopeptidase Mus musculus 39-42 31204686-0 2019 Structures of soluble rabbit neprilysin complexed with phosphoramidon or thiorphan. phosphoramidon 55-69 membrane metalloendopeptidase Homo sapiens 29-39 30963606-7 2019 111 In-SB9 was more stable than 111 In-AMBA, but coinjection of the neprilysin (NEP) inhibitor phosphoramidon (PA) stabilized both in vivo. phosphoramidon 95-109 membrane metallo endopeptidase Mus musculus 68-78 30963606-7 2019 111 In-SB9 was more stable than 111 In-AMBA, but coinjection of the neprilysin (NEP) inhibitor phosphoramidon (PA) stabilized both in vivo. phosphoramidon 95-109 membrane metallo endopeptidase Mus musculus 80-83 30963606-7 2019 111 In-SB9 was more stable than 111 In-AMBA, but coinjection of the neprilysin (NEP) inhibitor phosphoramidon (PA) stabilized both in vivo. phosphoramidon 111-113 membrane metallo endopeptidase Mus musculus 68-78 31204686-2 2019 The structure of the soluble extracellular domain (residues 55-750) of rabbit neprilysin was solved both in its native form at 2.1 A resolution, and bound to the inhibitors phosphoramidon and thiorphan at 2.8 and 3.0 A resolution, respectively. phosphoramidon 173-187 membrane metalloendopeptidase Homo sapiens 78-88 29556947-5 2018 A novel approach to increase in vivo stability of radiopeptides is by co-administration of the neutral endopeptidase (NEP) inhibitor, phosphoramidon (PA). phosphoramidon 134-148 membrane metallo endopeptidase Mus musculus 95-116 30897789-5 2019 Their biological profiles were compared in PC-3 cells and in mice without or with coinjection of phosphoramidon (PA) to induce transient neprilysin (NEP) inhibition in vivo. phosphoramidon 97-111 membrane metallo endopeptidase Mus musculus 137-147 30897789-5 2019 Their biological profiles were compared in PC-3 cells and in mice without or with coinjection of phosphoramidon (PA) to induce transient neprilysin (NEP) inhibition in vivo. phosphoramidon 97-111 membrane metallo endopeptidase Mus musculus 149-152 30897789-5 2019 Their biological profiles were compared in PC-3 cells and in mice without or with coinjection of phosphoramidon (PA) to induce transient neprilysin (NEP) inhibition in vivo. phosphoramidon 113-115 membrane metallo endopeptidase Mus musculus 137-147 30897789-5 2019 Their biological profiles were compared in PC-3 cells and in mice without or with coinjection of phosphoramidon (PA) to induce transient neprilysin (NEP) inhibition in vivo. phosphoramidon 113-115 membrane metallo endopeptidase Mus musculus 149-152 30537985-3 2018 We found that 5-hydroxyindolacetic acid (5-HIAA), the final metabolite of serotonin, considered until now as a dead-end and inactive product of serotonin catabolism, significantly reduces brain Abeta in the transgenic APPSWE mouse model for AD-related Abeta pathology and in the phosphoramidon-induced cerebral NEP inhibition mouse model. phosphoramidon 279-293 histocompatibility 2, class II antigen A, beta 1 Mus musculus 194-199 30871262-2 2019 Switching radiometal from 68Ga to 111In impaired tumor targeting in mice, but coinjection of the neprilysin (NEP)-inhibitor phosphoramidon (PA) stabilized 111In-SB3 in circulation and remarkably increased tumor uptake. phosphoramidon 124-138 membrane metallo endopeptidase Mus musculus 97-107 30871262-2 2019 Switching radiometal from 68Ga to 111In impaired tumor targeting in mice, but coinjection of the neprilysin (NEP)-inhibitor phosphoramidon (PA) stabilized 111In-SB3 in circulation and remarkably increased tumor uptake. phosphoramidon 124-138 membrane metallo endopeptidase Mus musculus 109-112 30871262-2 2019 Switching radiometal from 68Ga to 111In impaired tumor targeting in mice, but coinjection of the neprilysin (NEP)-inhibitor phosphoramidon (PA) stabilized 111In-SB3 in circulation and remarkably increased tumor uptake. phosphoramidon 140-142 membrane metallo endopeptidase Mus musculus 97-107 30871262-2 2019 Switching radiometal from 68Ga to 111In impaired tumor targeting in mice, but coinjection of the neprilysin (NEP)-inhibitor phosphoramidon (PA) stabilized 111In-SB3 in circulation and remarkably increased tumor uptake. phosphoramidon 140-142 membrane metallo endopeptidase Mus musculus 109-112 30002107-13 2019 Coadministration of phosphoramidon or thiorphan increases 177Lu-DOTA-MG11 uptake significantly in the CCK2R(+) tumors and stomach. phosphoramidon 20-34 cholecystokinin B receptor Homo sapiens 102-107 29556947-5 2018 A novel approach to increase in vivo stability of radiopeptides is by co-administration of the neutral endopeptidase (NEP) inhibitor, phosphoramidon (PA). phosphoramidon 134-148 membrane metallo endopeptidase Mus musculus 118-121 29556947-5 2018 A novel approach to increase in vivo stability of radiopeptides is by co-administration of the neutral endopeptidase (NEP) inhibitor, phosphoramidon (PA). phosphoramidon 150-152 membrane metallo endopeptidase Mus musculus 95-116 29556947-5 2018 A novel approach to increase in vivo stability of radiopeptides is by co-administration of the neutral endopeptidase (NEP) inhibitor, phosphoramidon (PA). phosphoramidon 150-152 membrane metallo endopeptidase Mus musculus 118-121 29556947-18 2018 CONCLUSIONS: Co-administration of PA increased in vivo tumor targeting capacity of [111In]SB3, making this an attractive combination for GRPR-targeted tumor imaging. phosphoramidon 34-36 gastrin releasing peptide receptor Mus musculus 137-141 26882895-12 2016 During the dose dependence study in mice, PA turned out to be more efficacious in enhancing tumor uptake of [(111)In-DOTA]MG11 in the CCK2R-positive tumors compared to equimolar amounts of TO. phosphoramidon 42-44 cholecystokinin B receptor Mus musculus 134-139 30082509-0 2018 Phosphoramidon inhibits the integral membrane protein zinc metalloprotease ZMPSTE24. phosphoramidon 0-14 zinc metallopeptidase STE24 Homo sapiens 75-83 30082509-3 2018 As part of an effort to understand the structural and functional relationships between ZMPSTE24 and soluble zinc metalloproteases, the inhibition of ZMPSTE24 by phosphoramidon [N-(alpha-rhamnopyranosyl-oxyhydroxyphosphinyl)-Leu-Trp], a transition-state analog and competitive inhibitor of multiple soluble zinc metalloproteases, especially gluzincins, has been characterized functionally and structurally. phosphoramidon 161-175 zinc metallopeptidase STE24 Homo sapiens 149-157 30082509-4 2018 The functional results, the determination of preliminary IC50 values by the use of an intramolecular quenched-fluorescence fluorogenic peptide assay, indicate that phosphoramidon inhibits ZMPSTE24 in a manner consistent with competitive inhibition. phosphoramidon 164-178 zinc metallopeptidase STE24 Homo sapiens 188-196 30082509-5 2018 The structural results, a 3.85 A resolution X-ray crystal structure of a ZMPSTE24-phosphoramidon complex, indicate that the overall binding mode observed between phosphoramidon and soluble gluzincins is conserved. phosphoramidon 82-96 zinc metallopeptidase STE24 Homo sapiens 73-81 29664606-7 2018 Coinjection of the radioconjugates with the neprilysin (NEP)-inhibitor phosphoramidon led to full stabilization of 111In/177Lu-SB3 in peripheral mouse blood and resulted in markedly enhanced radiolabel uptake in the PC-3 tumors. phosphoramidon 71-85 membrane metallo endopeptidase Mus musculus 44-54 29664606-7 2018 Coinjection of the radioconjugates with the neprilysin (NEP)-inhibitor phosphoramidon led to full stabilization of 111In/177Lu-SB3 in peripheral mouse blood and resulted in markedly enhanced radiolabel uptake in the PC-3 tumors. phosphoramidon 71-85 membrane metallo endopeptidase Mus musculus 56-59 28636973-4 2017 On the other hand, in-situ inhibition of neutral endopeptidase (NEP) by coinjection of phosphoramidon (PA) was shown to significantly improve the in vivo stability and tumor uptake of biodegradable radiopeptides. phosphoramidon 87-101 membrane metallo endopeptidase Mus musculus 41-62 28636973-4 2017 On the other hand, in-situ inhibition of neutral endopeptidase (NEP) by coinjection of phosphoramidon (PA) was shown to significantly improve the in vivo stability and tumor uptake of biodegradable radiopeptides. phosphoramidon 87-101 membrane metallo endopeptidase Mus musculus 64-67 28636973-4 2017 On the other hand, in-situ inhibition of neutral endopeptidase (NEP) by coinjection of phosphoramidon (PA) was shown to significantly improve the in vivo stability and tumor uptake of biodegradable radiopeptides. phosphoramidon 103-105 membrane metallo endopeptidase Mus musculus 41-62 28636973-4 2017 On the other hand, in-situ inhibition of neutral endopeptidase (NEP) by coinjection of phosphoramidon (PA) was shown to significantly improve the in vivo stability and tumor uptake of biodegradable radiopeptides. phosphoramidon 103-105 membrane metallo endopeptidase Mus musculus 64-67 27840228-10 2017 Both phosphoramidon (inhibitor of the known dynorphin converting enzyme neprilysin) and opiorphin (inhibitor of neprilysin and aminopeptidase N) blocked cortical bioconversion to dynorphin B(1-7), wheras only opiorphin blocked striatal bioconversion to dynorphin B(2-13). phosphoramidon 5-19 membrane metalloendopeptidase Homo sapiens 72-82 27840228-10 2017 Both phosphoramidon (inhibitor of the known dynorphin converting enzyme neprilysin) and opiorphin (inhibitor of neprilysin and aminopeptidase N) blocked cortical bioconversion to dynorphin B(1-7), wheras only opiorphin blocked striatal bioconversion to dynorphin B(2-13). phosphoramidon 5-19 opiorphin prepropeptide Homo sapiens 209-218 26882895-1 2016 BACKGROUND: We have recently shown that treatment of mice with the neutral endopeptidase (NEP) inhibitor phosphoramidon (PA) improves the bioavailability and tumor uptake of biodegradable radiopeptides. phosphoramidon 105-119 membrane metallo endopeptidase Mus musculus 90-93 26882895-1 2016 BACKGROUND: We have recently shown that treatment of mice with the neutral endopeptidase (NEP) inhibitor phosphoramidon (PA) improves the bioavailability and tumor uptake of biodegradable radiopeptides. phosphoramidon 121-123 membrane metallo endopeptidase Mus musculus 90-93 26882895-15 2016 NEP inhibition with the clinically tested NEP inhibitors TO and Race resulted in significant enhancement of tumor-to-kidney ratios vs. CONTROLS: However, compared with PA, TO and its prodrug Race induced less potent increases of tumor uptake, highlighting the significance of inhibitor type, administration route, and dose for implementing a first proof-of-principle study in human. phosphoramidon 168-170 membrane metallo endopeptidase Mus musculus 0-3 27062279-11 2016 In P1 arteries, constriction to thrombin or A23187 was inhibited by endothelial-denudation, by ET-1 receptor antagonists (BQ123 plus BQ788) or by inhibition of endothelin-converting enzyme (phosphoramidon or SM19712). phosphoramidon 190-204 coagulation factor II Mus musculus 32-40 26158215-7 2015 Coinjection of the NEP inhibitor phosphoramidon (PA) with radiolabeled gastrin and other peptide analogs has been recently proposed as a new promising strategy to increase bioavailability and tumor-localization of radiopeptides in tumor sites. phosphoramidon 33-47 membrane metalloendopeptidase Homo sapiens 19-22 26881775-6 2016 Accordingly, in functional experiments, CD10-A375 showed significantly greater cell proliferation in vitro and higher tumorigenicity in vivo; CD10 enzymatic inhibitors, thiorphan and phosphoramidon, significantly blocked the tumor growth of CD10-A375 in mice. phosphoramidon 183-197 membrane metallo endopeptidase Mus musculus 40-44 26881775-6 2016 Accordingly, in functional experiments, CD10-A375 showed significantly greater cell proliferation in vitro and higher tumorigenicity in vivo; CD10 enzymatic inhibitors, thiorphan and phosphoramidon, significantly blocked the tumor growth of CD10-A375 in mice. phosphoramidon 183-197 membrane metallo endopeptidase Mus musculus 142-146 26881775-6 2016 Accordingly, in functional experiments, CD10-A375 showed significantly greater cell proliferation in vitro and higher tumorigenicity in vivo; CD10 enzymatic inhibitors, thiorphan and phosphoramidon, significantly blocked the tumor growth of CD10-A375 in mice. phosphoramidon 183-197 membrane metallo endopeptidase Mus musculus 142-146 26844849-6 2016 After coinjection of the NEP inhibitor, phosphoramidon (PA), the stability of [(111)In]CP04 and [(111)In-DOTA]MG0 in peripheral mouse blood increased, with an exceptional >14-fold improvement monitored for [(111)In-DOTA]MG11. phosphoramidon 56-58 membrane metallo endopeptidase Mus musculus 25-28 26300210-7 2015 Secondly, we noted impressive enhancement of [(111)In]1/2/3 localization in AR42J and A431-CCK2R(+) tumors in mice after PA coinjection. phosphoramidon 121-123 cholecystokinin B receptor Mus musculus 91-96 26996808-6 2016 Modeling was performed using the experimental 3D structure of human endothelin-converting enzyme-1 in the presence of the metabolite phosphoramidon. phosphoramidon 133-147 endothelin converting enzyme 1 Homo sapiens 68-98 26844849-6 2016 After coinjection of the NEP inhibitor, phosphoramidon (PA), the stability of [(111)In]CP04 and [(111)In-DOTA]MG0 in peripheral mouse blood increased, with an exceptional >14-fold improvement monitored for [(111)In-DOTA]MG11. phosphoramidon 40-54 membrane metallo endopeptidase Mus musculus 25-28 26722377-4 2016 Here we show for the first time that co-injection of a NEP inhibitor (phosphoramidon (PA)) can lead to an impressive enhancement of diagnostic sensitivity and therapeutic efficacy of the theranostic (68)Ga-/(177)Lu-JMV4168 GRPR-antagonist. phosphoramidon 70-84 membrane metallo endopeptidase Mus musculus 55-58 26722377-4 2016 Here we show for the first time that co-injection of a NEP inhibitor (phosphoramidon (PA)) can lead to an impressive enhancement of diagnostic sensitivity and therapeutic efficacy of the theranostic (68)Ga-/(177)Lu-JMV4168 GRPR-antagonist. phosphoramidon 70-84 gastrin releasing peptide receptor Mus musculus 223-227 26722377-4 2016 Here we show for the first time that co-injection of a NEP inhibitor (phosphoramidon (PA)) can lead to an impressive enhancement of diagnostic sensitivity and therapeutic efficacy of the theranostic (68)Ga-/(177)Lu-JMV4168 GRPR-antagonist. phosphoramidon 86-88 membrane metallo endopeptidase Mus musculus 55-58 26722377-4 2016 Here we show for the first time that co-injection of a NEP inhibitor (phosphoramidon (PA)) can lead to an impressive enhancement of diagnostic sensitivity and therapeutic efficacy of the theranostic (68)Ga-/(177)Lu-JMV4168 GRPR-antagonist. phosphoramidon 86-88 gastrin releasing peptide receptor Mus musculus 223-227 26722377-11 2016 This data shows that co-injection of the enzyme inhibitor PA greatly enhances the theranostic potential of GRPR-radioantagonists for future application in PCa patients. phosphoramidon 58-60 gastrin releasing peptide receptor Homo sapiens 107-111 26158215-7 2015 Coinjection of the NEP inhibitor phosphoramidon (PA) with radiolabeled gastrin and other peptide analogs has been recently proposed as a new promising strategy to increase bioavailability and tumor-localization of radiopeptides in tumor sites. phosphoramidon 33-47 gastrin Homo sapiens 71-78 26158215-7 2015 Coinjection of the NEP inhibitor phosphoramidon (PA) with radiolabeled gastrin and other peptide analogs has been recently proposed as a new promising strategy to increase bioavailability and tumor-localization of radiopeptides in tumor sites. phosphoramidon 49-51 membrane metalloendopeptidase Homo sapiens 19-22 26158215-7 2015 Coinjection of the NEP inhibitor phosphoramidon (PA) with radiolabeled gastrin and other peptide analogs has been recently proposed as a new promising strategy to increase bioavailability and tumor-localization of radiopeptides in tumor sites. phosphoramidon 49-51 gastrin Homo sapiens 71-78 26158215-8 2015 Specifically, co-administration of PA with the truncated gastrin analog [(111)In-DOTA]MG11 ([((111)In-DOTA)DGlu(10)]gastrin(10-17)) impressively enhanced the levels of intact radiopeptide in mouse circulation and has led to an 8-fold increase of CCK2R-positive tumor uptake in SCID mice. phosphoramidon 35-37 gastrin Mus musculus 116-123 24000822-0 2014 Exploring mode of phosphoramidon and Abeta peptide binding to hECE-1 by molecular dynamics and docking studies. phosphoramidon 18-32 endothelin converting enzyme 1 Homo sapiens 62-68 25457559-5 2015 Oral gamma-hydroxybutyrate also counteracted phosphoramidon-induced brain neprilysin inhibition and Abeta accumulation. phosphoramidon 45-59 membrane metallo endopeptidase Mus musculus 74-84 25457559-5 2015 Oral gamma-hydroxybutyrate also counteracted phosphoramidon-induced brain neprilysin inhibition and Abeta accumulation. phosphoramidon 45-59 amyloid beta (A4) precursor protein Mus musculus 100-105 24287321-4 2014 Through single coinjection of the neutral endopeptidase inhibitor phosphoramidon (PA), we were able to provoke remarkable rises in the percentages of circulating intact somatostatin, gastrin, and bombesin radiopeptides in mouse models, resulting in a remarkable increase in uptake in tumor xenografts in mice. phosphoramidon 66-80 gastrin Mus musculus 183-190 24287321-4 2014 Through single coinjection of the neutral endopeptidase inhibitor phosphoramidon (PA), we were able to provoke remarkable rises in the percentages of circulating intact somatostatin, gastrin, and bombesin radiopeptides in mouse models, resulting in a remarkable increase in uptake in tumor xenografts in mice. phosphoramidon 82-84 gastrin Mus musculus 183-190 24000822-2 2014 In the present study we have performed molecular dynamics (MD) simulation of crystal structure complex of hECE-1 and its inhibitor phosphoramidon with Zn ion to understand the dynamic behavior of active site residues. phosphoramidon 131-145 endothelin converting enzyme 1 Homo sapiens 106-112 24000822-4 2014 The L-leucyl-L-tryptophan moiety and N-phosphoryl moiety of phosphoramidon was found in the S1 and S2 pockets of hECE-1 respectively. phosphoramidon 60-74 endothelin converting enzyme 1 Homo sapiens 113-119 25836673-5 2015 Chick embryos treated by phosphoramidon, which blocks the generation of endothelin-3, failed to develop enteric ganglia in the very distal bowel, characteristic of an HSCR-like phenotype. phosphoramidon 25-39 endothelin 3 Gallus gallus 72-84 25488751-5 2015 While we found that radiolabeled peptides based on the native kallidin sequence were ineffective at visualizing B1R-positive tumors, peptidase inhibition with phosphoramidon greatly enhanced B1R visualization in vivo. phosphoramidon 159-173 bradykinin receptor B1 Homo sapiens 191-194 25286347-4 2014 In addition, to improve in vivo stability of the peptide against in vivo degradation by the protease neutral endopeptidase (NEP), the authors coinjected [(177)Lu]DOTA-GRP(13-27) with the potent NEP inhibitor phosphoramidon (PA). phosphoramidon 208-222 membrane metallo endopeptidase Mus musculus 101-122 25286347-4 2014 In addition, to improve in vivo stability of the peptide against in vivo degradation by the protease neutral endopeptidase (NEP), the authors coinjected [(177)Lu]DOTA-GRP(13-27) with the potent NEP inhibitor phosphoramidon (PA). phosphoramidon 208-222 membrane metallo endopeptidase Mus musculus 124-127 25286347-4 2014 In addition, to improve in vivo stability of the peptide against in vivo degradation by the protease neutral endopeptidase (NEP), the authors coinjected [(177)Lu]DOTA-GRP(13-27) with the potent NEP inhibitor phosphoramidon (PA). phosphoramidon 224-226 membrane metallo endopeptidase Mus musculus 101-122 25286347-4 2014 In addition, to improve in vivo stability of the peptide against in vivo degradation by the protease neutral endopeptidase (NEP), the authors coinjected [(177)Lu]DOTA-GRP(13-27) with the potent NEP inhibitor phosphoramidon (PA). phosphoramidon 224-226 membrane metallo endopeptidase Mus musculus 124-127 25286347-10 2014 From biodistribution and ex vivo autoradiography studies, coadministration of both lysine and PA with [(177)Lu]DOTA-GRP(13-27) appeared to induce a clear improvement of tumor uptake as well as lower levels of renal radioactivity, causing a promising ninefold increase in tumor/kidney ratios. phosphoramidon 94-96 gastrin releasing peptide Mus musculus 116-119 25165447-5 2014 Of particular interest are endopeptidases that are sensitive to the neprilysin (NEP) inhibitors thiorphan and phosphoramidon (i.e., are "NEP-like") as these inhibitors induce a dramatic increase in Abeta levels in rodents. phosphoramidon 110-124 membrane metalloendopeptidase Homo sapiens 68-78 25165447-5 2014 Of particular interest are endopeptidases that are sensitive to the neprilysin (NEP) inhibitors thiorphan and phosphoramidon (i.e., are "NEP-like") as these inhibitors induce a dramatic increase in Abeta levels in rodents. phosphoramidon 110-124 membrane metalloendopeptidase Homo sapiens 80-83 25165447-5 2014 Of particular interest are endopeptidases that are sensitive to the neprilysin (NEP) inhibitors thiorphan and phosphoramidon (i.e., are "NEP-like") as these inhibitors induce a dramatic increase in Abeta levels in rodents. phosphoramidon 110-124 membrane metalloendopeptidase Homo sapiens 137-140 25165447-5 2014 Of particular interest are endopeptidases that are sensitive to the neprilysin (NEP) inhibitors thiorphan and phosphoramidon (i.e., are "NEP-like") as these inhibitors induce a dramatic increase in Abeta levels in rodents. phosphoramidon 110-124 amyloid beta precursor protein Homo sapiens 198-203 23963369-5 2013 Inhibition studies suggested that processes sensitive to insulin and phosphoramidon, which inhibit neprilysin, insulin-degrading enzyme, and endothelin-converting enzyme, are involved not only in degradation, but also in elimination of hAbeta(1-40). phosphoramidon 69-83 membrane metallo endopeptidase Mus musculus 99-109 23963369-5 2013 Inhibition studies suggested that processes sensitive to insulin and phosphoramidon, which inhibit neprilysin, insulin-degrading enzyme, and endothelin-converting enzyme, are involved not only in degradation, but also in elimination of hAbeta(1-40). phosphoramidon 69-83 insulin degrading enzyme Mus musculus 111-135 23528219-2 2013 Both are degraded by the neutral endopeptidase (NEP) which can be blocked by phosphoramidon. phosphoramidon 77-91 membrane metalloendopeptidase Homo sapiens 25-46 23911580-8 2013 The inhibition of ECE-1 activity was very strong, similar to the classic ECE inhibitor phosphoramidon, the addition of exogenous zinc restored enzymatic activity. phosphoramidon 87-101 endothelin converting enzyme 1 Rattus norvegicus 18-23 23911580-8 2013 The inhibition of ECE-1 activity was very strong, similar to the classic ECE inhibitor phosphoramidon, the addition of exogenous zinc restored enzymatic activity. phosphoramidon 87-101 endothelin converting enzyme 1 Rattus norvegicus 18-21 23868737-1 2013 OBJECTIVE: Previous in vitro studies have shown that the degradation of [Leu5]enkephalin during incubation with cerebral membrane preparations is almost completely prevented by a mixture of three peptidase inhibitors such as amastatin, captopril, and phosphoramidon. phosphoramidon 251-265 proenkephalin Rattus norvegicus 78-88 24069438-8 2013 Notably, purified LasB reproduced most of the effects of the LasB-containing secretomes, and these were drastically reduced in the presence of the LasB-selective inhibitor, phosphoramidon. phosphoramidon 173-187 elastase LasB Pseudomonas aeruginosa PAO1 18-22 24069438-8 2013 Notably, purified LasB reproduced most of the effects of the LasB-containing secretomes, and these were drastically reduced in the presence of the LasB-selective inhibitor, phosphoramidon. phosphoramidon 173-187 elastase LasB Pseudomonas aeruginosa PAO1 61-65 24069438-8 2013 Notably, purified LasB reproduced most of the effects of the LasB-containing secretomes, and these were drastically reduced in the presence of the LasB-selective inhibitor, phosphoramidon. phosphoramidon 173-187 elastase LasB Pseudomonas aeruginosa PAO1 61-65 23528219-2 2013 Both are degraded by the neutral endopeptidase (NEP) which can be blocked by phosphoramidon. phosphoramidon 77-91 membrane metalloendopeptidase Homo sapiens 48-51 23528219-10 2013 The inhibition of sweating by phosphoramidon may involve an increase in SP, a reduction in CGRP-degradation fragments or a direct inhibitory action of phosphoramidon. phosphoramidon 30-44 tachykinin precursor 1 Homo sapiens 72-74 23528219-10 2013 The inhibition of sweating by phosphoramidon may involve an increase in SP, a reduction in CGRP-degradation fragments or a direct inhibitory action of phosphoramidon. phosphoramidon 30-44 calcitonin related polypeptide alpha Homo sapiens 91-95 22554773-9 2012 Nebulized phosphoramidon (1 mM, 1 min), a neutral endopeptidase 24.11 inhibitor, significantly enhanced the response induced by toluene (135 ppm, 10 min) compared with nebulized 0.9% saline (1 min). phosphoramidon 10-24 membrane metallo-endopeptidase Rattus norvegicus 42-69 23113990-3 2012 To explore the structural differences between XCE and ECE-1, homology model of XCE was built using the complex structure of ECE-1 with phosphoramidon (pdb-id: 3DWB) as template. phosphoramidon 135-149 endothelin converting enzyme like 1 Homo sapiens 79-82 23113990-4 2012 Phosphoramidon was docked into the binding site of XCE whereas phosphate oxygen of the inhibitor was used as water molecule to design the apo forms of both enzymes. phosphoramidon 0-14 endothelin converting enzyme like 1 Homo sapiens 51-54 22387410-8 2012 OCCs are resistant to Abeta challenge in any of the conditions tested (variation of [K+]e, presence or absence of serum, or addition of the neprilysin blocker phosphoramidon). phosphoramidon 159-173 membrane metallo endopeptidase Mus musculus 140-150 22642296-9 2012 SC44463, BB94 and Phosphoramidon were computationally docked into the 3 day structure of the human MMP7 ZBD and TAD and thermolysin using the docking program GOLD. phosphoramidon 18-32 matrix metallopeptidase 7 Homo sapiens 99-103 21937235-4 2011 Recently, the X-ray crystal structure of human NEP complexed with phosphoramidon has been reported and provided insights into the active site specificity of NEP. phosphoramidon 66-80 membrane metalloendopeptidase Homo sapiens 47-50 21937235-4 2011 Recently, the X-ray crystal structure of human NEP complexed with phosphoramidon has been reported and provided insights into the active site specificity of NEP. phosphoramidon 66-80 membrane metalloendopeptidase Homo sapiens 157-160 21651905-6 2011 Application of captopril 1 muM (angiotensin-converting enzyme inhibitor) or phosphoramidon 10 muM (neutral endopeptidase inhibitor) induced a leftward shift of bradykinin-elicited responses in human umbilical vein with endothelium while no effect was observed in tissues denuded of endothelium under the same treatment. phosphoramidon 76-90 latexin Homo sapiens 94-97 21651905-6 2011 Application of captopril 1 muM (angiotensin-converting enzyme inhibitor) or phosphoramidon 10 muM (neutral endopeptidase inhibitor) induced a leftward shift of bradykinin-elicited responses in human umbilical vein with endothelium while no effect was observed in tissues denuded of endothelium under the same treatment. phosphoramidon 76-90 kininogen 1 Homo sapiens 160-170 21459096-8 2011 The neutral endopeptidase (NEP) inhibitor, phosphoramidon, blocked inactivation of CNP and CD-NP, but not BNP or DNP. phosphoramidon 43-57 membrane metalloendopeptidase Homo sapiens 4-25 21459096-8 2011 The neutral endopeptidase (NEP) inhibitor, phosphoramidon, blocked inactivation of CNP and CD-NP, but not BNP or DNP. phosphoramidon 43-57 membrane metalloendopeptidase Homo sapiens 27-30 21459096-8 2011 The neutral endopeptidase (NEP) inhibitor, phosphoramidon, blocked inactivation of CNP and CD-NP, but not BNP or DNP. phosphoramidon 43-57 2',3'-cyclic nucleotide 3' phosphodiesterase Homo sapiens 83-86 21174590-3 2011 RESULTS: In human umbilical vein endothelial cells, both phosphoramidon, an inhibitor of ECE-1, and TIMP-2 decreased VEGF-induced ET-1 production. phosphoramidon 57-71 endothelin converting enzyme 1 Homo sapiens 89-94 21224067-2 2011 Endopeptidases sensitive to inhibition by thiorphan and phosphoramidon are especially important, because these inhibitors induce dramatic Abeta accumulation (~30- to 50-fold) and pathological deposition in rodents. phosphoramidon 56-70 amyloid beta (A4) precursor protein Mus musculus 138-143 21224067-4 2011 However, genetic ablation of NEP results in only modest increases (~1.5- to 2-fold) in Abeta, indicating that other thiorphan/phosphoramidon-sensitive endopeptidases are at work. phosphoramidon 126-140 membrane metallo endopeptidase Mus musculus 29-32 21224067-5 2011 Of particular interest is the NEP homolog neprilysin 2 (NEP2), which is thiorphan/phosphoramidon-sensitive and degrades Abeta. phosphoramidon 82-96 membrane metallo endopeptidase Mus musculus 30-33 21224067-5 2011 Of particular interest is the NEP homolog neprilysin 2 (NEP2), which is thiorphan/phosphoramidon-sensitive and degrades Abeta. phosphoramidon 82-96 membrane metallo-endopeptidase-like 1 Mus musculus 42-54 21224067-5 2011 Of particular interest is the NEP homolog neprilysin 2 (NEP2), which is thiorphan/phosphoramidon-sensitive and degrades Abeta. phosphoramidon 82-96 membrane metallo-endopeptidase-like 1 Mus musculus 56-60 21224067-5 2011 Of particular interest is the NEP homolog neprilysin 2 (NEP2), which is thiorphan/phosphoramidon-sensitive and degrades Abeta. phosphoramidon 82-96 amyloid beta (A4) precursor protein Mus musculus 120-125 21224067-10 2011 Treatment of these double-knockout mice with phosphoramidon resulted in elevations of Abeta, suggesting that yet other NEP-like Abeta-degrading endopeptidases are contributing to Abeta catabolism. phosphoramidon 45-59 amyloid beta (A4) precursor protein Mus musculus 86-91 21224067-10 2011 Treatment of these double-knockout mice with phosphoramidon resulted in elevations of Abeta, suggesting that yet other NEP-like Abeta-degrading endopeptidases are contributing to Abeta catabolism. phosphoramidon 45-59 membrane metallo endopeptidase Mus musculus 119-122 21224067-10 2011 Treatment of these double-knockout mice with phosphoramidon resulted in elevations of Abeta, suggesting that yet other NEP-like Abeta-degrading endopeptidases are contributing to Abeta catabolism. phosphoramidon 45-59 amyloid beta (A4) precursor protein Mus musculus 128-133 21224067-10 2011 Treatment of these double-knockout mice with phosphoramidon resulted in elevations of Abeta, suggesting that yet other NEP-like Abeta-degrading endopeptidases are contributing to Abeta catabolism. phosphoramidon 45-59 amyloid beta (A4) precursor protein Mus musculus 128-133 20941644-0 2011 Intranasal phosphoramidon increases beta-amyloid levels in wild-type and NEP/NEP2-deficient mice. phosphoramidon 11-25 tensin 2 Mus musculus 73-76 20941644-0 2011 Intranasal phosphoramidon increases beta-amyloid levels in wild-type and NEP/NEP2-deficient mice. phosphoramidon 11-25 membrane metallo-endopeptidase-like 1 Mus musculus 77-81 20941644-5 2011 An alternative model of amyloidosis utilizes intracerebroventricular infusion of thiorphan or phosphoramidon to block the activity of key Abeta degrading enzymes (NEP, NEP2) resulting in accumulation of Abeta. phosphoramidon 94-108 amyloid beta precursor protein Homo sapiens 138-143 20941644-5 2011 An alternative model of amyloidosis utilizes intracerebroventricular infusion of thiorphan or phosphoramidon to block the activity of key Abeta degrading enzymes (NEP, NEP2) resulting in accumulation of Abeta. phosphoramidon 94-108 membrane metalloendopeptidase Homo sapiens 163-166 20941644-5 2011 An alternative model of amyloidosis utilizes intracerebroventricular infusion of thiorphan or phosphoramidon to block the activity of key Abeta degrading enzymes (NEP, NEP2) resulting in accumulation of Abeta. phosphoramidon 94-108 membrane metalloendopeptidase like 1 Homo sapiens 168-172 20941644-5 2011 An alternative model of amyloidosis utilizes intracerebroventricular infusion of thiorphan or phosphoramidon to block the activity of key Abeta degrading enzymes (NEP, NEP2) resulting in accumulation of Abeta. phosphoramidon 94-108 amyloid beta precursor protein Homo sapiens 203-208 20941644-6 2011 Here, we demonstrate that intranasal administration of phosphoramidon produces significantly elevated cerebral Abeta levels in wild-type mice. phosphoramidon 55-69 amyloid beta (A4) precursor protein Mus musculus 111-116 20941644-7 2011 Furthermore, intranasal phosphoramidon administration in double knockout mice lacking NEP and NEP2 also showed increased levels of Abeta(40). phosphoramidon 24-38 tensin 2 Mus musculus 86-89 20941644-7 2011 Furthermore, intranasal phosphoramidon administration in double knockout mice lacking NEP and NEP2 also showed increased levels of Abeta(40). phosphoramidon 24-38 membrane metallo-endopeptidase-like 1 Mus musculus 94-98 20941644-7 2011 Furthermore, intranasal phosphoramidon administration in double knockout mice lacking NEP and NEP2 also showed increased levels of Abeta(40). phosphoramidon 24-38 amyloid beta (A4) precursor protein Mus musculus 131-136 20941644-8 2011 These data show that intranasal delivery of drugs can be used to model AD and suggest that other phosphoramidon-sensitive peptidases are degrading Abeta in NEP/NEP2-deficient mice. phosphoramidon 97-111 amyloid beta (A4) precursor protein Mus musculus 147-152 20941644-8 2011 These data show that intranasal delivery of drugs can be used to model AD and suggest that other phosphoramidon-sensitive peptidases are degrading Abeta in NEP/NEP2-deficient mice. phosphoramidon 97-111 tensin 2 Mus musculus 156-159 20941644-8 2011 These data show that intranasal delivery of drugs can be used to model AD and suggest that other phosphoramidon-sensitive peptidases are degrading Abeta in NEP/NEP2-deficient mice. phosphoramidon 97-111 membrane metallo-endopeptidase-like 1 Mus musculus 160-164 21174590-3 2011 RESULTS: In human umbilical vein endothelial cells, both phosphoramidon, an inhibitor of ECE-1, and TIMP-2 decreased VEGF-induced ET-1 production. phosphoramidon 57-71 vascular endothelial growth factor A Homo sapiens 117-121 21174590-3 2011 RESULTS: In human umbilical vein endothelial cells, both phosphoramidon, an inhibitor of ECE-1, and TIMP-2 decreased VEGF-induced ET-1 production. phosphoramidon 57-71 endothelin 1 Homo sapiens 130-134 18586023-9 2008 In contrast, treatment with phosphoramidon further enhanced left ventricular endothelin-1 level and norepinephrine overflow, and significantly worsened cardiac dysfunction after ischemia/reperfusion. phosphoramidon 28-42 endothelin 1 Rattus norvegicus 77-89 20088804-4 2010 Of particular interest are endopeptidases that are sensitive to the neprilysin inhibitors thiorphan and phosphoramidon (i.e. "NEP-like") as these inhibitors induce a dramatic increase in Abeta levels resulting in rapid plaque formation in wild-type rodents. phosphoramidon 104-118 membrane metalloendopeptidase Homo sapiens 68-78 20088804-4 2010 Of particular interest are endopeptidases that are sensitive to the neprilysin inhibitors thiorphan and phosphoramidon (i.e. "NEP-like") as these inhibitors induce a dramatic increase in Abeta levels resulting in rapid plaque formation in wild-type rodents. phosphoramidon 104-118 membrane metalloendopeptidase Homo sapiens 126-129 20088804-4 2010 Of particular interest are endopeptidases that are sensitive to the neprilysin inhibitors thiorphan and phosphoramidon (i.e. "NEP-like") as these inhibitors induce a dramatic increase in Abeta levels resulting in rapid plaque formation in wild-type rodents. phosphoramidon 104-118 amyloid beta precursor protein Homo sapiens 187-192 19962413-2 2010 The big ET-1-induced vasoconstriction (a) developed more rapidly (i.e., was greater in the first 30 min) in the diabetic group than in the age-matched controls, and (b) in each group was largely suppressed by phosphoramidon [nonselective endothelin-converting enzyme (ECE)/neutral endopeptidase (NEP) inhibitor] or CGS35066 (selective ECE inhibitor), but not by thiorphan (selective NEP inhibitor). phosphoramidon 209-223 endothelin 1 Rattus norvegicus 8-12 19151386-6 2009 ET-1 precursor big ET-1 elicited time-dependent vasoconstriction over 20 minutes, which was blocked by the ECE-1 inhibitor phosphoramidon. phosphoramidon 123-137 endothelin 1 Homo sapiens 0-4 19151386-6 2009 ET-1 precursor big ET-1 elicited time-dependent vasoconstriction over 20 minutes, which was blocked by the ECE-1 inhibitor phosphoramidon. phosphoramidon 123-137 endothelin 1 Homo sapiens 19-23 19151386-6 2009 ET-1 precursor big ET-1 elicited time-dependent vasoconstriction over 20 minutes, which was blocked by the ECE-1 inhibitor phosphoramidon. phosphoramidon 123-137 endothelin converting enzyme 1 Homo sapiens 107-112 20796280-7 2010 Phosphoramidon increased sperm progressive motility and its effects were reduced in the presence of the tachykinin receptor antagonists SR140333 (NK1 receptor-selective) and SR48968 (NK2 receptor-selective) but unmodified in the presence of SR142801 (NK3 receptor-selective). phosphoramidon 0-14 tachykinin receptor 1 Homo sapiens 146-158 20796280-7 2010 Phosphoramidon increased sperm progressive motility and its effects were reduced in the presence of the tachykinin receptor antagonists SR140333 (NK1 receptor-selective) and SR48968 (NK2 receptor-selective) but unmodified in the presence of SR142801 (NK3 receptor-selective). phosphoramidon 0-14 tachykinin receptor 2 Homo sapiens 183-195 20796280-7 2010 Phosphoramidon increased sperm progressive motility and its effects were reduced in the presence of the tachykinin receptor antagonists SR140333 (NK1 receptor-selective) and SR48968 (NK2 receptor-selective) but unmodified in the presence of SR142801 (NK3 receptor-selective). phosphoramidon 0-14 tachykinin receptor 3 Homo sapiens 251-263 20522806-4 2010 METHODS AND RESULTS: After NO synthase inhibition (L-NAME), thrombin contracted aged arteries, which was inhibited by endothelial denudation, ET(A) receptor antagonism (BQ123), and ECE inhibition (phosphoramidon, SM19712) or by inhibiting exocytosis (TAT-NSF, N-ethylmaleimide-sensitive factor inhibitor). phosphoramidon 197-211 coagulation factor II, thrombin Homo sapiens 60-68 19780404-3 2009 In recent studies we found that pharmacological inhibition of NEP by phosphoramidon resulted in elevated plasma levels of SP and greater oxidative stress. phosphoramidon 69-83 membrane metallo-endopeptidase Rattus norvegicus 62-65 19520130-10 2009 The enhanced effect of the combination of substance P with morphine was reduced significantly by co-administration of phosphoramidon, an inhibitor of endopeptidase-24.11. phosphoramidon 118-132 tachykinin 1 Mus musculus 42-53 18992253-5 2009 Here, we present the crystal structure of the extracellular domain (residues 90-770) of human ECE-1 (C428S) with the generic metalloprotease inhibitor phosphoramidon determined at 2.38 A resolution. phosphoramidon 151-165 endothelin converting enzyme 1 Homo sapiens 94-99 18804491-6 2008 The acidic (pH optimum 5.5), membrane-bound, thiorphan- (ED(50) 1.2+/-0.2 nM) and phosphoramidon (ED(50) 150+/-25 pM) sensitive, endothelin-1 inactivating peptidase (K(M) 0.12+/-0.03 microM) was present in the mucosal cells of duodenum and small intestine. phosphoramidon 82-96 endothelin 1 Rattus norvegicus 129-141 18772340-5 2008 Furthermore, we have previously shown that both the endothelin-converting enzyme-1 (ECE-1) inhibitor, phosphoramidon, as well as a novel ET-1 receptor A antagonist synthesized by our group, control premature delivery in a mouse model of inflammation-associated preterm delivery. phosphoramidon 102-116 endothelin converting enzyme 1 Mus musculus 84-89 18463098-8 2008 Interestingly, the mRNA levels of endogenous fly NEP genes and phosphoramidon-sensitive NEP activity declined during aging in fly brains, as observed in mammals. phosphoramidon 63-77 Neprilysin 1 Drosophila melanogaster 88-91 18758506-5 2008 In our previous work, we have shown that blockade of ET-1 synthesis through the use of the metalloproteinase inhibitor phosphoramidon results in control of preterm labor. phosphoramidon 119-133 endothelin 1 Mus musculus 53-57 18607539-2 2008 Male Sprague-Dawley rats (180g) were fed MgD (approximately 50 mg Mg/kg) or Mg-sufficient (MgS, 608 mg Mg/kg) diets for 7 days +/- NEP inhibitor phosphoramidon (PR, 5 mg/kg/day, s.c.). phosphoramidon 145-159 membrane metallo-endopeptidase Rattus norvegicus 131-134 18645412-7 2008 The constriction response to topically applied 100 nM CARTp was blocked by both the endothelin A (ETA) receptor antagonist BQ-123 (10 microM) and the inhibitor of endothelin-converting enzyme, phosphoramidon (100 nM). phosphoramidon 193-207 CART prepropeptide Rattus norvegicus 54-59 17643133-4 2007 KEY RESULTS: ECE-1 activity was completely inhibited by CGS-26303 25 microM and phosphoramidon 100 microM. phosphoramidon 80-94 endothelin converting enzyme 1 Homo sapiens 13-18 18307123-1 2008 Phosphoramidon blocks the formation of endothelin-1 (ET-1), a proinflammatory mediator implicated in the pathogenesis of a variety of lung diseases. phosphoramidon 0-14 endothelin 1 Homo sapiens 39-51 18307123-1 2008 Phosphoramidon blocks the formation of endothelin-1 (ET-1), a proinflammatory mediator implicated in the pathogenesis of a variety of lung diseases. phosphoramidon 0-14 endothelin 1 Homo sapiens 53-57 18307123-4 2008 The results indicate that phosphoramidon significantly reduces LPS-induced pulmonary inflammation as measured by lung histology, neutrophil content of bronchoalveolar lavage (BAL) fluid, percent tumor necrosis factor receptor 1 (TNFR1)-labeled BAL macrophages, and alveolar septal cell apoptosis. phosphoramidon 26-40 TNF receptor superfamily member 1A Homo sapiens 195-227 18307123-4 2008 The results indicate that phosphoramidon significantly reduces LPS-induced pulmonary inflammation as measured by lung histology, neutrophil content of bronchoalveolar lavage (BAL) fluid, percent tumor necrosis factor receptor 1 (TNFR1)-labeled BAL macrophages, and alveolar septal cell apoptosis. phosphoramidon 26-40 TNF receptor superfamily member 1A Homo sapiens 229-234 18296865-1 2008 Previous in vitro studies have shown that the degradation of [Leu(5)]enkephalin during incubation with cerebral membrane preparations is almost completely prevented by a mixture of three peptidase inhibitors: amastatin, captopril, and phosphoramidon. phosphoramidon 235-249 proenkephalin Rattus norvegicus 69-79 18322380-2 2008 The results obtained revealed that intracerebroventricular injection of the protease inhibitor phosphoramidon into wild-type mice for up to a month elevated the soluble and deposited brain Abeta levels and concomitantly induced the neurodegeneration of distinct hippocampal neurons as well as neuroinflammation. phosphoramidon 95-109 amyloid beta (A4) precursor protein Mus musculus 189-194 18055635-7 2007 This endopeptidase activity was inhibited by the neprilysin inhibitors phosphoramidon (IC(50,) 0.15 micromol l(-1)) and thiorphan (IC(50,) 1.2 micromol l(-1)). phosphoramidon 71-85 Neprilysin-like 11 Drosophila melanogaster 49-59 17643133-5 2007 CGS-26303 and phosphoramidon, though not thiorphan, a neutral endopeptidase (NEP) inhibitor, stimulated ECE-1 expression in cells (maximal effect at 16 h, 25 microM). phosphoramidon 14-28 endothelin converting enzyme 1 Homo sapiens 104-109 17904426-6 2007 ECE and its product ET-1(1-21) were detected in aorta and vena cava, and the ECE inhibitors phosphoramidon and CGS-26393 reduced big ET-1-induced contraction. phosphoramidon 92-106 endothelin converting enzyme 1 Rattus norvegicus 77-80 17878706-1 2007 Previous in vitro studies have shown that the degradation of [Met(5)]enkephalin-Arg(6)-Phe(7) during incubation with cerebral membrane preparations is largely prevented by a mixture of three peptidase inhibitors: amastatin, captopril, and phosphoramidon. phosphoramidon 239-253 proenkephalin Rattus norvegicus 69-79 17466482-4 2007 In endothelium-intact rings, phosphoramidon (1 mmol/l), a nonselective ECE/neutral endopeptidase (NEP) inhibitor, produced a rightward displacement of the concentration-response curves and reduced the maximal contractile response to Big-ET-1. phosphoramidon 29-43 endothelin converting enzyme 1 Rattus norvegicus 71-74 17196890-6 2007 Furthermore, pretreatment with ET converting enzyme inhibitor phosphoramidon (10 nmol) abolished the cardiovascular effects evoked by icv injection of ET-1(1-31) or big ET-1. phosphoramidon 62-76 endothelin 1 Rattus norvegicus 151-155 17196890-6 2007 Furthermore, pretreatment with ET converting enzyme inhibitor phosphoramidon (10 nmol) abolished the cardiovascular effects evoked by icv injection of ET-1(1-31) or big ET-1. phosphoramidon 62-76 endothelin 1 Rattus norvegicus 169-173 17507367-8 2007 Finally, treatment of cultured myofibroblasts with an NEP inhibitor (phosphoramidon) downregulated the expression of profibrotic transforming growth factor-beta1, whereas addition of BK decreased the expression of collagens I and III which was reversed by a BK-2R antagonist. phosphoramidon 69-83 membrane metalloendopeptidase Homo sapiens 54-57 17466482-4 2007 In endothelium-intact rings, phosphoramidon (1 mmol/l), a nonselective ECE/neutral endopeptidase (NEP) inhibitor, produced a rightward displacement of the concentration-response curves and reduced the maximal contractile response to Big-ET-1. phosphoramidon 29-43 membrane metallo-endopeptidase Rattus norvegicus 98-101 17466482-4 2007 In endothelium-intact rings, phosphoramidon (1 mmol/l), a nonselective ECE/neutral endopeptidase (NEP) inhibitor, produced a rightward displacement of the concentration-response curves and reduced the maximal contractile response to Big-ET-1. phosphoramidon 29-43 endothelin 1 Rattus norvegicus 237-241 17466482-5 2007 However, in endothelium-denuded rings phosphoramidon reduced the maximum contraction for Big-ET-1 but did not alter the potency when compared to the curves obtained in the absence of the inhibitor. phosphoramidon 38-52 endothelin 1 Rattus norvegicus 93-97 17028040-8 2006 Thus, our main purpose for this study was to examine the effects of both big ET-1 and ET-1 to clarify the role of phosphoramidon in inhibiting the conversion of big ET-1 to ET-1, by investigating the systemic blood pressure, microvascular blood flow velocity, and diameters of arterioles and venules of the rat mesentery. phosphoramidon 114-128 endothelin 1 Rattus norvegicus 165-177 17157960-2 2007 In this study we show that membranes prepared from embryos of Drosophila melanogaster possess neprilysin-like activity that is inhibited by phosphoramidon and thiorphan, both inhibitors of mammalian neprilysin. phosphoramidon 140-154 membrane metalloendopeptidase Homo sapiens 94-104 17157960-2 2007 In this study we show that membranes prepared from embryos of Drosophila melanogaster possess neprilysin-like activity that is inhibited by phosphoramidon and thiorphan, both inhibitors of mammalian neprilysin. phosphoramidon 140-154 membrane metalloendopeptidase Homo sapiens 199-209 17112488-7 2006 Phosphoramidon, a neprilysin inhibitor, attenuated these effects of neprilysin. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 18-28 17112488-7 2006 Phosphoramidon, a neprilysin inhibitor, attenuated these effects of neprilysin. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 68-78 17028040-17 2006 In the second group of experiments, cumulative injections of phosphoramidon (30 mg/kg/10 min) were administered 10 min prior to the infusion of big ET-1. phosphoramidon 61-75 endothelin 1 Rattus norvegicus 148-152 17028040-18 2006 Phosphoramidon significantly suppressed the long-lasting significant pressor effect and significantly inhibited the dose-dependent increase and dose-dependent decrease in the microvascular blood flow velocity produced by big ET-1 in the rat mesenteric microcirculation. phosphoramidon 0-14 endothelin 1 Rattus norvegicus 225-229 17028040-20 2006 Moreover, phosphoramidon markedly inhibited the conversion of big ET-1 to ET-1 in the rat mesenteric microcirculation, which may suggest an inhibition of the enzyme which converts big ET-1 to ET-1. phosphoramidon 10-24 endothelin 1 Rattus norvegicus 66-78 17028040-20 2006 Moreover, phosphoramidon markedly inhibited the conversion of big ET-1 to ET-1 in the rat mesenteric microcirculation, which may suggest an inhibition of the enzyme which converts big ET-1 to ET-1. phosphoramidon 10-24 endothelin 1 Rattus norvegicus 184-196 16633356-13 2006 Additionally, by measuring the production of ET-1(1-31), we showed that a chymase-like enzyme is involved in this process when ECE and NEP are inhibited by phosphoramidon. phosphoramidon 156-170 neprilysin Oryctolagus cuniculus 135-138 15874973-9 2005 Extraluminal administration of PD-145065, BQ-123, and phosphoramidon blocked the constriction response to CART peptide (P<0.01). phosphoramidon 54-68 CART prepropeptide Rattus norvegicus 106-110 16406141-2 2006 By using dermal microdialysis we explored the effect of phosphoramidon (NEP blocker), captopril (ACE blocker) and a mixture of both drugs on the intensity of electrically-induced CGRP-mediated neurogenic flare. phosphoramidon 56-70 calcitonin related polypeptide alpha Homo sapiens 179-183 16406141-5 2006 Electrically released CGRP levels could be measured directly in perfusates containing phosphoramidon and the mixture. phosphoramidon 86-100 calcitonin related polypeptide alpha Homo sapiens 22-26 16406141-6 2006 Again, CGRP levels were elevated in phosphoramidon treated sites, and significantly reduced upon adding captopril. phosphoramidon 36-50 calcitonin related polypeptide alpha Homo sapiens 7-11 16391412-5 2005 Therapeutic administration of phosphoramidon, an inhibitor of ECE-1 activity, not only led to a 53.2% drop in the ET-1, but also produced a dose-dependent reduction (up to 50.9%) in the mucosal level of leptin and up to 42.3% decline in the rate of ulcer healing. phosphoramidon 30-44 endothelin converting enzyme 1 Rattus norvegicus 62-67 16391412-5 2005 Therapeutic administration of phosphoramidon, an inhibitor of ECE-1 activity, not only led to a 53.2% drop in the ET-1, but also produced a dose-dependent reduction (up to 50.9%) in the mucosal level of leptin and up to 42.3% decline in the rate of ulcer healing. phosphoramidon 30-44 endothelin 1 Rattus norvegicus 114-118 16391412-5 2005 Therapeutic administration of phosphoramidon, an inhibitor of ECE-1 activity, not only led to a 53.2% drop in the ET-1, but also produced a dose-dependent reduction (up to 50.9%) in the mucosal level of leptin and up to 42.3% decline in the rate of ulcer healing. phosphoramidon 30-44 leptin Rattus norvegicus 203-209 16169283-5 2005 The combined NEP/endothelin-converting enzyme inhibitor (NEP/ECE inhibitor), phosphoramidon (10 microM) or the specific inhibitor of the NEP, thiorphan (10 microM) resulted in an enhanced magnitude of CNP-induced relaxation without significant change in the EC50 both on endothelium intact and endothelium deprived preparations. phosphoramidon 77-91 natriuretic peptide C Homo sapiens 201-204 15963503-8 2005 Inhibition of NEP with phosphoramidon increased flare intensity (P < 0.002) and size (P < 0.01), while blocking ACE had no effect on neurogenic vasodilation. phosphoramidon 23-37 membrane metalloendopeptidase Homo sapiens 14-17 15963503-9 2005 CGRP release could be measured in microdialysis samples after phosphoramidon perfusion only (P < 0.03), not in samples with captopril or saline perfusion. phosphoramidon 62-76 calcitonin related polypeptide alpha Homo sapiens 0-4 15993898-7 2005 Both NEP(-/-) mice and NEP(+/+) mice pretreated with the NEP antagonist phosphoramidon (10 mg/kg s.c.) had significant elevations of lung MPO and worsened lung histology compared to NEP(+/+) mice given elastase alone. phosphoramidon 72-86 membrane metallo endopeptidase Mus musculus 5-8 15993898-7 2005 Both NEP(-/-) mice and NEP(+/+) mice pretreated with the NEP antagonist phosphoramidon (10 mg/kg s.c.) had significant elevations of lung MPO and worsened lung histology compared to NEP(+/+) mice given elastase alone. phosphoramidon 72-86 membrane metallo endopeptidase Mus musculus 23-26 15993898-7 2005 Both NEP(-/-) mice and NEP(+/+) mice pretreated with the NEP antagonist phosphoramidon (10 mg/kg s.c.) had significant elevations of lung MPO and worsened lung histology compared to NEP(+/+) mice given elastase alone. phosphoramidon 72-86 membrane metallo endopeptidase Mus musculus 23-26 15993898-7 2005 Both NEP(-/-) mice and NEP(+/+) mice pretreated with the NEP antagonist phosphoramidon (10 mg/kg s.c.) had significant elevations of lung MPO and worsened lung histology compared to NEP(+/+) mice given elastase alone. phosphoramidon 72-86 myeloperoxidase Mus musculus 138-141 15993898-7 2005 Both NEP(-/-) mice and NEP(+/+) mice pretreated with the NEP antagonist phosphoramidon (10 mg/kg s.c.) had significant elevations of lung MPO and worsened lung histology compared to NEP(+/+) mice given elastase alone. phosphoramidon 72-86 membrane metallo endopeptidase Mus musculus 23-26 15151517-9 2004 The effects of big ET-1([1-38]) and phosphoramidon suggest the presence of endogenous ECE activity in the skin. phosphoramidon 36-50 endothelin converting enzyme 1 Homo sapiens 86-89 15969636-7 2005 Phosphoramidon, thiorphan, acidification, and phenanthroline inhibited PM ECE activity; the cytosolic ECE activity was not affected by phenanthroline but was inhibited by the others. phosphoramidon 0-14 endothelin converting enzyme 1 Homo sapiens 74-77 15969636-9 2005 Pepstatin, a potent inhibitor of cathepsins, and phosphoramidon, a potent inhibitor of ECE, inhibited the cytosolic conversion of Big ET-1 peptide by 46% and 35%, respectively, whereas the combination of both inhibited the cytosolic activity by 93%. phosphoramidon 49-63 endothelin converting enzyme 1 Homo sapiens 87-90 15969636-9 2005 Pepstatin, a potent inhibitor of cathepsins, and phosphoramidon, a potent inhibitor of ECE, inhibited the cytosolic conversion of Big ET-1 peptide by 46% and 35%, respectively, whereas the combination of both inhibited the cytosolic activity by 93%. phosphoramidon 49-63 endothelin 1 Homo sapiens 134-138 15764737-4 2005 Treatment with 10 microM phosphoramidon (NEP inhibitor) or 10 microM amastatin (APM inhibitor) potentiated DAKD-elicited responses, whereas 1 microM captopril (ACE inhibitor) had no significant effects. phosphoramidon 25-39 membrane metalloendopeptidase Homo sapiens 41-44 16280098-4 2005 Pretreatment with phosphoramidon, an inhibitor of ECE-1 activity, not only led to a decline in ECE-1 and ET-1 generation, but also produced a dose-dependent reduction in the mucosal level of leptin and the extent of mucosal damage caused by indomethacin. phosphoramidon 18-32 endothelin converting enzyme 1 Rattus norvegicus 50-55 16280098-4 2005 Pretreatment with phosphoramidon, an inhibitor of ECE-1 activity, not only led to a decline in ECE-1 and ET-1 generation, but also produced a dose-dependent reduction in the mucosal level of leptin and the extent of mucosal damage caused by indomethacin. phosphoramidon 18-32 endothelin converting enzyme 1 Rattus norvegicus 95-100 16280098-4 2005 Pretreatment with phosphoramidon, an inhibitor of ECE-1 activity, not only led to a decline in ECE-1 and ET-1 generation, but also produced a dose-dependent reduction in the mucosal level of leptin and the extent of mucosal damage caused by indomethacin. phosphoramidon 18-32 endothelin 1 Rattus norvegicus 105-109 16280098-4 2005 Pretreatment with phosphoramidon, an inhibitor of ECE-1 activity, not only led to a decline in ECE-1 and ET-1 generation, but also produced a dose-dependent reduction in the mucosal level of leptin and the extent of mucosal damage caused by indomethacin. phosphoramidon 18-32 leptin Rattus norvegicus 191-197 16280098-5 2005 This effect of phosphoramidon, however, was subject to suppression by the exogenous ET-1 administration. phosphoramidon 15-29 endothelin 1 Rattus norvegicus 84-88 16117692-10 2005 The retinal PM Big ET-1 converting activity was inhibited by phosphoramidon, thiorphan, and acidification. phosphoramidon 61-75 endothelin 1 Bos taurus 19-23 16021085-3 2005 STUDY DESIGN: Forearm blood flow was measured by venous occlusion plethysmography during intra-arterial infusion of phosphoramidon, an endothelin-converting enzyme inhibitor, for 60 minutes, which was followed by co-infusion with endothelin-1 for 30 minutes. phosphoramidon 116-130 endothelin 1 Homo sapiens 230-242 15956117-4 2005 Phosphoramidon, a dual neutral endopeptidase and endothelin-converting enzyme inhibitor, blocked both pressor responses to endothelin-1 (1-31) and big endothelin-1 but not those afforded by endothelin-1. phosphoramidon 0-14 endothelin-1 Oryctolagus cuniculus 123-135 15956117-4 2005 Phosphoramidon, a dual neutral endopeptidase and endothelin-converting enzyme inhibitor, blocked both pressor responses to endothelin-1 (1-31) and big endothelin-1 but not those afforded by endothelin-1. phosphoramidon 0-14 endothelin-1 Oryctolagus cuniculus 151-163 15956117-4 2005 Phosphoramidon, a dual neutral endopeptidase and endothelin-converting enzyme inhibitor, blocked both pressor responses to endothelin-1 (1-31) and big endothelin-1 but not those afforded by endothelin-1. phosphoramidon 0-14 endothelin-1 Oryctolagus cuniculus 151-163 15956117-7 2005 Furthermore, injection of big endothelin-1 concomitantly with phosphoramidon induced an increase in endothelin-1 (1-31) plasma levels. phosphoramidon 62-76 endothelin-1 Oryctolagus cuniculus 30-42 15956117-7 2005 Furthermore, injection of big endothelin-1 concomitantly with phosphoramidon induced an increase in endothelin-1 (1-31) plasma levels. phosphoramidon 62-76 endothelin-1 Oryctolagus cuniculus 100-112 15956117-8 2005 Finally, intracardiac-administered endothelin-1 (1-31) induced an increase of endothelin-1 plasma levels, which are markedly reduced by phosphoramidon and thiorphan but not by CGS 35066. phosphoramidon 136-150 endothelin-1 Oryctolagus cuniculus 35-47 15956117-8 2005 Finally, intracardiac-administered endothelin-1 (1-31) induced an increase of endothelin-1 plasma levels, which are markedly reduced by phosphoramidon and thiorphan but not by CGS 35066. phosphoramidon 136-150 endothelin-1 Oryctolagus cuniculus 78-90 15177934-6 2004 The NT-induced stimulation of EGFR/ERK/Akt phosphorylation and DNA synthesis was inhibited by EGFR-tyrosine kinase inhibitors (AG1478, PD153035), metallo-endopeptidase inhibitor phosphoramidon and by heparin, but not by neutralizing anti-EGF antibody. phosphoramidon 178-192 epidermal growth factor receptor Homo sapiens 30-34 15177934-6 2004 The NT-induced stimulation of EGFR/ERK/Akt phosphorylation and DNA synthesis was inhibited by EGFR-tyrosine kinase inhibitors (AG1478, PD153035), metallo-endopeptidase inhibitor phosphoramidon and by heparin, but not by neutralizing anti-EGF antibody. phosphoramidon 178-192 mitogen-activated protein kinase 1 Homo sapiens 35-38 15177934-6 2004 The NT-induced stimulation of EGFR/ERK/Akt phosphorylation and DNA synthesis was inhibited by EGFR-tyrosine kinase inhibitors (AG1478, PD153035), metallo-endopeptidase inhibitor phosphoramidon and by heparin, but not by neutralizing anti-EGF antibody. phosphoramidon 178-192 AKT serine/threonine kinase 1 Homo sapiens 39-42 15177934-6 2004 The NT-induced stimulation of EGFR/ERK/Akt phosphorylation and DNA synthesis was inhibited by EGFR-tyrosine kinase inhibitors (AG1478, PD153035), metallo-endopeptidase inhibitor phosphoramidon and by heparin, but not by neutralizing anti-EGF antibody. phosphoramidon 178-192 epidermal growth factor receptor Homo sapiens 94-98 15172962-13 2004 Big ET-1 also contracted the ductus sphincter but differed from ET-1 for its lesser potency and inhibition by phosphoramidon (50 microm). phosphoramidon 110-124 EDN1 Ovis aries 4-8 14659804-4 2003 Force and [Na(+)](i) increase were abolished by inhibition of the Na(+)/H(+) exchanger (NHE) with the inhibitor HOE642, blockade of endothelin receptors with the nonselective antagonist TAK044 and by inhibition of the endothelin-converting enzyme with phosphoramidon. phosphoramidon 252-266 solute carrier family 9 member C1 Homo sapiens 88-91 15148521-3 2004 Degradation of SP was inhibited by a metal chelator, o-phenanthroline, and also by specific inhibitors of endopeptidase-24.11, thiorphan and phosphoramidon. phosphoramidon 141-155 tachykinin 1 Mus musculus 15-17 14972450-6 2004 Cell number was reduced by 54.4 per cent of the control by culture with 10(-6)m GnRH for 24 h. However, phosphoramidon, a NEP specific inhibitor, inhibited antiproliferative effect of GnRH and reverted to the control level. phosphoramidon 104-118 gonadotropin releasing hormone 1 Homo sapiens 80-84 14972450-6 2004 Cell number was reduced by 54.4 per cent of the control by culture with 10(-6)m GnRH for 24 h. However, phosphoramidon, a NEP specific inhibitor, inhibited antiproliferative effect of GnRH and reverted to the control level. phosphoramidon 104-118 membrane metalloendopeptidase Homo sapiens 122-125 14972450-6 2004 Cell number was reduced by 54.4 per cent of the control by culture with 10(-6)m GnRH for 24 h. However, phosphoramidon, a NEP specific inhibitor, inhibited antiproliferative effect of GnRH and reverted to the control level. phosphoramidon 104-118 gonadotropin releasing hormone 1 Homo sapiens 184-188 12827039-0 2003 The effects of phosphoramidon on the expression of human endothelin-converting enzyme-1 (ECE-1) isoforms. phosphoramidon 15-29 endothelin converting enzyme 1 Homo sapiens 57-87 15804063-7 2003 Phosphoramidon can protect the myocardial injury in rats and its mechanism may be to inhibit ECE and reduce the endothelins production. phosphoramidon 0-14 endothelin converting enzyme 1 Rattus norvegicus 93-96 14500390-7 2003 Cytotoxicity of CPI-0004Na was inhibited by phosphoramidon, a known inhibitor of CD10 enzymatic activity. phosphoramidon 44-58 membrane metalloendopeptidase Homo sapiens 81-85 12885426-6 2003 Investigations were also performed to determine whether the administration of phosphoramidon, an endothelin-converting enzyme (ECE) inhibitor, and BQ-123, an endothelin receptor ET(A) antagonist, suppresses angiogenesis and VEGF expression. phosphoramidon 78-92 vascular endothelial growth factor A Rattus norvegicus 224-228 14501953-1 2003 We tested the hypothesis that metalloendopeptidase inhibition using phosphoramidon during induction of endotoxemia 24 h later would down-regulate the protein expression of myocardial inducible nitric oxide synthase (iNOS) and phosphorylation of p38-mitogen-activated protein kinase (p38-MAPK). phosphoramidon 68-82 thimet oligopeptidase 1 Rattus norvegicus 30-50 14501953-1 2003 We tested the hypothesis that metalloendopeptidase inhibition using phosphoramidon during induction of endotoxemia 24 h later would down-regulate the protein expression of myocardial inducible nitric oxide synthase (iNOS) and phosphorylation of p38-mitogen-activated protein kinase (p38-MAPK). phosphoramidon 68-82 nitric oxide synthase 2 Rattus norvegicus 183-214 14501953-1 2003 We tested the hypothesis that metalloendopeptidase inhibition using phosphoramidon during induction of endotoxemia 24 h later would down-regulate the protein expression of myocardial inducible nitric oxide synthase (iNOS) and phosphorylation of p38-mitogen-activated protein kinase (p38-MAPK). phosphoramidon 68-82 nitric oxide synthase 2 Rattus norvegicus 216-220 14501953-1 2003 We tested the hypothesis that metalloendopeptidase inhibition using phosphoramidon during induction of endotoxemia 24 h later would down-regulate the protein expression of myocardial inducible nitric oxide synthase (iNOS) and phosphorylation of p38-mitogen-activated protein kinase (p38-MAPK). phosphoramidon 68-82 mitogen activated protein kinase 14 Rattus norvegicus 245-281 14501953-1 2003 We tested the hypothesis that metalloendopeptidase inhibition using phosphoramidon during induction of endotoxemia 24 h later would down-regulate the protein expression of myocardial inducible nitric oxide synthase (iNOS) and phosphorylation of p38-mitogen-activated protein kinase (p38-MAPK). phosphoramidon 68-82 mitogen activated protein kinase 14 Rattus norvegicus 283-291 14501953-8 2003 This LPS-induced left ventricular ET-1 elevation at 24 h was significantly reduced by phosphoramidon. phosphoramidon 86-100 endothelin 1 Rattus norvegicus 34-38 14501953-11 2003 Also, LPS-induced upregulated protein expression of myocardial-inducible nitric oxide synthase and increased levels of nitric oxide byproducts at 24 h were blocked by phosphoramidon. phosphoramidon 167-181 nitric oxide synthase 2 Rattus norvegicus 63-94 14501953-12 2003 Phosphoramidon inhibited LPS-induced down-regulated expression of myocardial endothelial nitric oxide synthase and upregulated p38-MAPK phosphorylation. phosphoramidon 0-14 mitogen activated protein kinase 14 Rattus norvegicus 127-130 12827039-0 2003 The effects of phosphoramidon on the expression of human endothelin-converting enzyme-1 (ECE-1) isoforms. phosphoramidon 15-29 endothelin converting enzyme 1 Homo sapiens 89-94 12827039-2 2003 This process is inhibited by phosphoramidon through binding to the catalytic domain of ECE-1. phosphoramidon 29-43 endothelin converting enzyme 1 Homo sapiens 87-92 12827039-5 2003 It is not known, however, whether phosphoramidon has similar effects on the expression of other ECE-1 isoforms. phosphoramidon 34-48 endothelin converting enzyme 1 Homo sapiens 96-101 12827039-10 2003 Taken together, our results demonstrate that phosphoramidon differentially affects the expression of three human ECE-1 isoforms. phosphoramidon 45-59 endothelin converting enzyme 1 Homo sapiens 113-118 12962299-5 2003 Application of 10(-4)-M phosphoramidon resulted in a statistically significant decrease in big ET-1-induced contraction in E+ and E- segments; 10(-5)-M and 10(-6)-M [22D-Val]big ET-1 [16-38] in E- segments produced no statistically significant effect. phosphoramidon 24-38 endothelin 1 Rattus norvegicus 95-99 12962299-5 2003 Application of 10(-4)-M phosphoramidon resulted in a statistically significant decrease in big ET-1-induced contraction in E+ and E- segments; 10(-5)-M and 10(-6)-M [22D-Val]big ET-1 [16-38] in E- segments produced no statistically significant effect. phosphoramidon 24-38 endothelin 1 Rattus norvegicus 178-182 12654643-2 2003 Incubation of SP-A with P. aeruginosa organisms from several clinical isolates resulted in concentration- and temperature-dependent degradation of SP-A that was inhibited by a metalloproteinase inhibitor, phosphoramidon. phosphoramidon 205-219 surfactant protein A1 Homo sapiens 14-18 12654643-2 2003 Incubation of SP-A with P. aeruginosa organisms from several clinical isolates resulted in concentration- and temperature-dependent degradation of SP-A that was inhibited by a metalloproteinase inhibitor, phosphoramidon. phosphoramidon 205-219 surfactant protein A1 Homo sapiens 147-151 12541324-5 2003 The enzyme was acted upon by the NEP inhibitors phosphoramidon (IC(50), 0.64 microM) and thiorphan (IC(50), 1.23 microM), and the detergent-solubilized enzyme had an Mr of approximately 300,000 and a neutral pH optimum. phosphoramidon 48-62 membrane metalloendopeptidase Homo sapiens 33-36 12392915-9 2002 Phosphoramidon-treated CD1 mice survived the acute infection. phosphoramidon 0-14 CD1 antigen complex Mus musculus 23-26 12434178-7 2002 This ECE-activity could be inhibited by Captopril and Phosporamidon, suggesting a potency for prevention and therapy of cerebral vasospasm. phosphoramidon 54-67 endothelin converting enzyme 1 Rattus norvegicus 5-8 12499645-5 2002 The MAPK activation was also inhibited by the endothelin receptor antagonist cyclo(D-alpha-aspartyl-L-prolyl-D-valyl-L-leucyl-D-tryptophyl) (BQ123) and by the endothelin-converting enzyme inhibitor phosphoramidon. phosphoramidon 198-212 mitogen activated protein kinase 3 Rattus norvegicus 4-8 12431739-7 2002 Complete inhibition of the endopeptidic hydrolysis of the LomTK-1 by a disc homogenate required a combination of captopril and the neprilysin inhibitor, phosphoramidon, providing biochemical evidence for a neprilysin-like peptidase, in addition to Ance, in imaginal discs of D. melanogaster. phosphoramidon 153-167 Neprilysin-like 11 Drosophila melanogaster 131-141 12431739-7 2002 Complete inhibition of the endopeptidic hydrolysis of the LomTK-1 by a disc homogenate required a combination of captopril and the neprilysin inhibitor, phosphoramidon, providing biochemical evidence for a neprilysin-like peptidase, in addition to Ance, in imaginal discs of D. melanogaster. phosphoramidon 153-167 Neprilysin-like 11 Drosophila melanogaster 206-216 12477147-10 2002 ECE-1 inhibitors, phosphoramidon and FR-901533, inhibited vascular ECE-1 activity by more than 80%. phosphoramidon 18-32 endothelin converting enzyme 1 Homo sapiens 0-5 12393059-1 2002 Previous in vitro studies showed that the degradation of [Met(5)]enkephalin-Arg-Gly-Leu by cerebral membrane preparations is almost completely prevented by a mixture of three peptidase inhibitors: amastatin, captopril and phosphoramidon. phosphoramidon 222-236 proenkephalin Rattus norvegicus 65-75 12220742-3 2002 NMB cells express neutral endopeptidase (NEP) activity that can be specifically inhibited by phosphoramidon (PA). phosphoramidon 93-107 membrane metalloendopeptidase Homo sapiens 18-39 12220742-3 2002 NMB cells express neutral endopeptidase (NEP) activity that can be specifically inhibited by phosphoramidon (PA). phosphoramidon 93-107 membrane metalloendopeptidase Homo sapiens 41-44 12220742-3 2002 NMB cells express neutral endopeptidase (NEP) activity that can be specifically inhibited by phosphoramidon (PA). phosphoramidon 109-111 membrane metalloendopeptidase Homo sapiens 18-39 12220742-3 2002 NMB cells express neutral endopeptidase (NEP) activity that can be specifically inhibited by phosphoramidon (PA). phosphoramidon 109-111 membrane metalloendopeptidase Homo sapiens 41-44 12220742-4 2002 Our data now show that phosphoramidon treatment increases the efficacy of VIP-stimulated neuroblastoma proliferation. phosphoramidon 23-37 vasoactive intestinal peptide Homo sapiens 74-77 12477147-10 2002 ECE-1 inhibitors, phosphoramidon and FR-901533, inhibited vascular ECE-1 activity by more than 80%. phosphoramidon 18-32 endothelin converting enzyme 1 Homo sapiens 67-72 12208785-5 2002 NEP inhibition with phosphoramidon did not affect the bradykinin concentration-response curve (CRC), nor did combined NEP/ACE inhibition with omapatrilat exert a further leftward shift on top of the approximately 10 fold leftward shift of the bradykinin CRC observed with ACE inhibition alone. phosphoramidon 20-34 membrane metalloendopeptidase Homo sapiens 0-3 12363040-5 2002 Inhibition of NEP/CD10 by the NEP inhibitor phosphoramidon or by an anti-CD10 monoclonal antibody significantly increased apoptosis induction. phosphoramidon 44-58 membrane metalloendopeptidase Homo sapiens 14-17 12363040-5 2002 Inhibition of NEP/CD10 by the NEP inhibitor phosphoramidon or by an anti-CD10 monoclonal antibody significantly increased apoptosis induction. phosphoramidon 44-58 membrane metalloendopeptidase Homo sapiens 18-22 12363040-5 2002 Inhibition of NEP/CD10 by the NEP inhibitor phosphoramidon or by an anti-CD10 monoclonal antibody significantly increased apoptosis induction. phosphoramidon 44-58 membrane metalloendopeptidase Homo sapiens 30-33 12099999-9 2002 This increase is attributed to the higher conversion rate of big ET-1 to ET-1 because the ET-converting enzyme (ECE) inhibitor phosphoramidon, at a concentration of 10(-6) mol/L, causes an inhibition in the response to big ET-1 by 52.6% in normal kidneys, whereas this inhibition with the same concentration of phosphoramidon was found to be significantly decreased in kidneys isolated from GLY-pretreated rabbits. phosphoramidon 127-141 endothelin-1 Oryctolagus cuniculus 65-77 12099999-9 2002 This increase is attributed to the higher conversion rate of big ET-1 to ET-1 because the ET-converting enzyme (ECE) inhibitor phosphoramidon, at a concentration of 10(-6) mol/L, causes an inhibition in the response to big ET-1 by 52.6% in normal kidneys, whereas this inhibition with the same concentration of phosphoramidon was found to be significantly decreased in kidneys isolated from GLY-pretreated rabbits. phosphoramidon 127-141 endothelin-1 Oryctolagus cuniculus 65-69 12099999-9 2002 This increase is attributed to the higher conversion rate of big ET-1 to ET-1 because the ET-converting enzyme (ECE) inhibitor phosphoramidon, at a concentration of 10(-6) mol/L, causes an inhibition in the response to big ET-1 by 52.6% in normal kidneys, whereas this inhibition with the same concentration of phosphoramidon was found to be significantly decreased in kidneys isolated from GLY-pretreated rabbits. phosphoramidon 311-325 endothelin-1 Oryctolagus cuniculus 65-77 12099999-9 2002 This increase is attributed to the higher conversion rate of big ET-1 to ET-1 because the ET-converting enzyme (ECE) inhibitor phosphoramidon, at a concentration of 10(-6) mol/L, causes an inhibition in the response to big ET-1 by 52.6% in normal kidneys, whereas this inhibition with the same concentration of phosphoramidon was found to be significantly decreased in kidneys isolated from GLY-pretreated rabbits. phosphoramidon 311-325 endothelin-1 Oryctolagus cuniculus 65-69 12193062-9 2002 Cleavage of bradykinin by PgPepO occurs at the Pro(7)-Phe(8) bond and is inhibited by the NEP and ECE-1 inhibitor phosphoramidon in a pH-dependent fashion (IC(50) =10 microM at pH 7.0) but not by thiorphan, an NEP-specific inhibitor. phosphoramidon 114-128 endothelin converting enzyme 1 Homo sapiens 98-103 12193101-11 2002 In another experiment phosphoramidon treatment was also tested in CD1 mice, which have a high mortality during the acute phase of infection with 5 x 10(4) trypomastigotes of the Brazil strain. phosphoramidon 22-36 CD1 antigen complex Mus musculus 66-69 12182783-9 2002 Preincubation with phosphoramidon (10(-4) mol/L) resulted in a small yet significant inhibition of the contraction induced by big ET-1. phosphoramidon 19-33 endothelin 1 Homo sapiens 130-134 11882619-5 2002 NEP inhibitor phosphoramidon (100 nmol/L), or omapatrilat, which inhibits both NEP and ACE, did not potentiate bradykinin in CHO/B(2) cells. phosphoramidon 14-28 membrane metalloendopeptidase Homo sapiens 0-3 12110606-7 2002 Phosphoramidon (5 and 10 mg kg(-1)) reduced both pressor and PIP effects of ET-1(1-31). phosphoramidon 0-14 prolactin-inducible protein homolog Cavia porcellus 61-64 11897392-7 2002 Phosphoramidon inhibited both these cleavages, but with markedly different potencies, indicating the presence in the fly brain of two NEP-like enzymes with different substrate and inhibitor specificity. phosphoramidon 0-14 Neprilysin-like 11 Drosophila melanogaster 134-137 11909608-4 2002 Phosphoramidon, an inhibitor of neutral endopeptidase 24.11 (neprilysin, CD10), was ineffective at 10 microM, but at 100 microM, significant increase in the maximum response was achieved by neurokinin A in detrusor strips with and without mucosa. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 32-59 11909608-4 2002 Phosphoramidon, an inhibitor of neutral endopeptidase 24.11 (neprilysin, CD10), was ineffective at 10 microM, but at 100 microM, significant increase in the maximum response was achieved by neurokinin A in detrusor strips with and without mucosa. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 61-71 11909608-4 2002 Phosphoramidon, an inhibitor of neutral endopeptidase 24.11 (neprilysin, CD10), was ineffective at 10 microM, but at 100 microM, significant increase in the maximum response was achieved by neurokinin A in detrusor strips with and without mucosa. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 73-77 11909608-4 2002 Phosphoramidon, an inhibitor of neutral endopeptidase 24.11 (neprilysin, CD10), was ineffective at 10 microM, but at 100 microM, significant increase in the maximum response was achieved by neurokinin A in detrusor strips with and without mucosa. phosphoramidon 0-14 tachykinin precursor 1 Homo sapiens 190-202 11818328-5 2002 Serum-stimulated proliferation was attenuated by inhibiting either endogenous ET-1 release with phosphoramidon (10(-5) mol/L) or its action with PD145065 (10(-5) mol/L). phosphoramidon 96-110 endothelin 1 Homo sapiens 78-82 12137746-5 2002 Phosphoramidon, a potent inhibitor of NEP, reduced the liberated amino acids to about a half, suggesting that NEP is a responsible enzyme for GnRH degradation. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 38-41 12137746-5 2002 Phosphoramidon, a potent inhibitor of NEP, reduced the liberated amino acids to about a half, suggesting that NEP is a responsible enzyme for GnRH degradation. phosphoramidon 0-14 membrane metalloendopeptidase Homo sapiens 110-113 12137746-5 2002 Phosphoramidon, a potent inhibitor of NEP, reduced the liberated amino acids to about a half, suggesting that NEP is a responsible enzyme for GnRH degradation. phosphoramidon 0-14 gonadotropin releasing hormone 1 Homo sapiens 142-146 12021551-6 2002 In contrast, the expression of neutral endopeptidase (NEP), a cell surface peptide with hydrolyzing activity of SP, was increased in fibroblasts stimulated with SP after 24 h. The administration of NEP inhibitor (phosphoramidon) to the fibroblasts induced higher SP production. phosphoramidon 213-227 membrane metalloendopeptidase Homo sapiens 31-52 12021551-6 2002 In contrast, the expression of neutral endopeptidase (NEP), a cell surface peptide with hydrolyzing activity of SP, was increased in fibroblasts stimulated with SP after 24 h. The administration of NEP inhibitor (phosphoramidon) to the fibroblasts induced higher SP production. phosphoramidon 213-227 membrane metalloendopeptidase Homo sapiens 54-57 12021551-6 2002 In contrast, the expression of neutral endopeptidase (NEP), a cell surface peptide with hydrolyzing activity of SP, was increased in fibroblasts stimulated with SP after 24 h. The administration of NEP inhibitor (phosphoramidon) to the fibroblasts induced higher SP production. phosphoramidon 213-227 tachykinin precursor 1 Homo sapiens 112-114 12021551-6 2002 In contrast, the expression of neutral endopeptidase (NEP), a cell surface peptide with hydrolyzing activity of SP, was increased in fibroblasts stimulated with SP after 24 h. The administration of NEP inhibitor (phosphoramidon) to the fibroblasts induced higher SP production. phosphoramidon 213-227 tachykinin precursor 1 Homo sapiens 161-163 12021551-6 2002 In contrast, the expression of neutral endopeptidase (NEP), a cell surface peptide with hydrolyzing activity of SP, was increased in fibroblasts stimulated with SP after 24 h. The administration of NEP inhibitor (phosphoramidon) to the fibroblasts induced higher SP production. phosphoramidon 213-227 membrane metalloendopeptidase Homo sapiens 198-201 12021551-6 2002 In contrast, the expression of neutral endopeptidase (NEP), a cell surface peptide with hydrolyzing activity of SP, was increased in fibroblasts stimulated with SP after 24 h. The administration of NEP inhibitor (phosphoramidon) to the fibroblasts induced higher SP production. phosphoramidon 213-227 tachykinin precursor 1 Homo sapiens 161-163 11882619-8 2002 Arachidonic acid release by bradykinin from CHO/NEP-B(2) cells was also augmented by 100 nmol/L phosphoramidon or omapatrilat about 3-fold, and again, the inhibitors resensitized the desensitized B(2) receptor. phosphoramidon 96-110 kininogen 1 Homo sapiens 28-38 11882619-8 2002 Arachidonic acid release by bradykinin from CHO/NEP-B(2) cells was also augmented by 100 nmol/L phosphoramidon or omapatrilat about 3-fold, and again, the inhibitors resensitized the desensitized B(2) receptor. phosphoramidon 96-110 membrane metalloendopeptidase Homo sapiens 48-51 11882619-8 2002 Arachidonic acid release by bradykinin from CHO/NEP-B(2) cells was also augmented by 100 nmol/L phosphoramidon or omapatrilat about 3-fold, and again, the inhibitors resensitized the desensitized B(2) receptor. phosphoramidon 96-110 bradykinin receptor B2 Homo sapiens 196-209 11561101-10 2001 Phosphoramidon (10 mg/kg), an endothelin converting enzyme inhibitor, markedly blunted U46619-induced changes on CBF and MBF (p < 0.05). phosphoramidon 0-14 CCAAT/enhancer binding protein zeta Rattus norvegicus 113-124 11764001-6 2001 ), an NK2 receptor antagonist, significantly inhibited the phosphoramidon-induced enhancement of BK-induced bronchoconstriction, although FK888 (3 mg kg(-1), i.v. phosphoramidon 59-73 substance-K receptor Cavia porcellus 6-18 11687727-2 2001 Posthemorrhagic vasospasm can be counteracted by the administration of phosphoramidon, which blocks the endothelin converting enzyme (ECE) responsible for the conversion of big endothelin into a fully active ET1 peptide. phosphoramidon 71-85 endothelin converting enzyme 1 Rattus norvegicus 104-132 11687727-2 2001 Posthemorrhagic vasospasm can be counteracted by the administration of phosphoramidon, which blocks the endothelin converting enzyme (ECE) responsible for the conversion of big endothelin into a fully active ET1 peptide. phosphoramidon 71-85 endothelin converting enzyme 1 Rattus norvegicus 134-137 11687727-2 2001 Posthemorrhagic vasospasm can be counteracted by the administration of phosphoramidon, which blocks the endothelin converting enzyme (ECE) responsible for the conversion of big endothelin into a fully active ET1 peptide. phosphoramidon 71-85 endothelin 1 Rattus norvegicus 208-211 11687727-6 2001 The ECE inhibitor phosphoramidon was administered in a dose of 40 nmol in 50 microl of cerebrospinal fluid three times: 20 min before SAH, 60 min after SAH, and 24 hours after SAH. phosphoramidon 18-32 endothelin converting enzyme 1 Rattus norvegicus 4-7 11747295-5 2001 This NEP-induced degradation was completely inhibited by the NEP inhibitors thiorphan and phosphoramidon. phosphoramidon 90-104 membrane metalloendopeptidase Homo sapiens 5-8 11747295-5 2001 This NEP-induced degradation was completely inhibited by the NEP inhibitors thiorphan and phosphoramidon. phosphoramidon 90-104 membrane metalloendopeptidase Homo sapiens 61-64 11440542-8 2001 The level of hCG secretion from the FSK-treated cells was further enhanced when the cells were treated in the presence of the NEP inhibitor phosphoramidon. phosphoramidon 140-154 hypertrichosis 2 (generalised, congenital) Homo sapiens 13-16 11740152-5 2001 The specific involvement of ET-1 in the angiogenic effect mediated by CHO-ET-1 was demonstrated by the reduction or abolition of neovascularized CHO-ET-1 nodules by (1) bosentan, a mixed antagonist of ET(A)/ET(B) receptors, (2) an ET(A) receptor antagonist (Ru69986) and (3) phosporamidon, an inhibitor of endothelin-converting enzyme-1 (ECE-1). phosphoramidon 275-288 endothelin-1 Cricetulus griseus 28-32 11740152-5 2001 The specific involvement of ET-1 in the angiogenic effect mediated by CHO-ET-1 was demonstrated by the reduction or abolition of neovascularized CHO-ET-1 nodules by (1) bosentan, a mixed antagonist of ET(A)/ET(B) receptors, (2) an ET(A) receptor antagonist (Ru69986) and (3) phosporamidon, an inhibitor of endothelin-converting enzyme-1 (ECE-1). phosphoramidon 275-288 endothelin-1 Cricetulus griseus 74-78 11740152-5 2001 The specific involvement of ET-1 in the angiogenic effect mediated by CHO-ET-1 was demonstrated by the reduction or abolition of neovascularized CHO-ET-1 nodules by (1) bosentan, a mixed antagonist of ET(A)/ET(B) receptors, (2) an ET(A) receptor antagonist (Ru69986) and (3) phosporamidon, an inhibitor of endothelin-converting enzyme-1 (ECE-1). phosphoramidon 275-288 endothelin-1 Cricetulus griseus 74-78 11337485-7 2001 Furthermore, we show that overexpression of ECE-1 in Chinese hamster ovary cells, which lack endogenous ECE activity, reduces extracellular Abeta concentration by up to 90% and that this effect is completely reversed by treatment of the cells with phosphoramidon. phosphoramidon 248-262 endothelin-converting enzyme 1 Cricetulus griseus 44-49 11404259-6 2001 Coincubation with phosphoramidon augmented the effect of 10(-9) and 10(-8) M bradykinin. phosphoramidon 18-32 kininogen 1 Homo sapiens 77-87 11472982-6 2001 Addition of an ET-A receptor antagonist (BQ123) or an inhibitor of ET-1 synthesis (phosphoramidon) reduced the proliferation induced by serum, confirming an autocrine role for ET-1. phosphoramidon 83-97 endothelin 1 Homo sapiens 67-71 11447035-7 2001 Conversely, pretreatment of wild-type mice with the NEP inhibitor phosphoramidon exacerbated enteritis. phosphoramidon 66-80 membrane metallo endopeptidase Mus musculus 52-55 11466223-7 2001 Uterine NK(2)R mRNA levels remain stable during the course of pregnancy and at Day 1 postpartum; and the contractions elicited by activating selectively the NK(2) receptor in the presence of the neutral endopeptidase inhibitor phosphoramidon (1 microM) were similar in early, mid, or late pregnancy. phosphoramidon 227-241 tachykinin receptor 2 Rattus norvegicus 157-171 11558680-6 2001 Phosphoramidon, a neutral endopeptidase inhibitor, shifted the apparent potency of ANP to values equivalent to that of BNP, suggesting these kidney cell/slices rapidly degrade ANP but not BNP. phosphoramidon 0-14 natriuretic peptide type A Mus musculus 83-86 11558680-6 2001 Phosphoramidon, a neutral endopeptidase inhibitor, shifted the apparent potency of ANP to values equivalent to that of BNP, suggesting these kidney cell/slices rapidly degrade ANP but not BNP. phosphoramidon 0-14 natriuretic peptide type A Mus musculus 176-179 11440542-8 2001 The level of hCG secretion from the FSK-treated cells was further enhanced when the cells were treated in the presence of the NEP inhibitor phosphoramidon. phosphoramidon 140-154 membrane metalloendopeptidase Homo sapiens 126-129 11278416-0 2001 Neprilysin degrades both amyloid beta peptides 1-40 and 1-42 most rapidly and efficiently among thiorphan- and phosphoramidon-sensitive endopeptidases. phosphoramidon 111-125 membrane metalloendopeptidase Homo sapiens 0-10 11278416-1 2001 To identify the amyloid beta peptide (Abeta) 1-42-degrading enzyme whose activity is inhibited by thiorphan and phosphoramidon in vivo, we searched for neprilysin (NEP) homologues and cloned neprilysin-like peptidase (NEPLP) alpha, NEPLP beta, and NEPLP gamma cDNAs. phosphoramidon 112-126 membrane metalloendopeptidase Homo sapiens 164-167 11278416-2 2001 We expressed NEP, phosphate-regulating gene with homologies to endopeptidases on the X chromosome (PEX), NEPLPs, and damage-induced neuronal endopeptidase (DINE) in 293 cells as 95- to 125-kDa proteins and found that the enzymatic activities of PEX, NEPLP alpha, and NEPLP beta, as well as those of NEP and DINE, were sensitive to thiorphan and phosphoramidon. phosphoramidon 345-359 membrane metalloendopeptidase Homo sapiens 13-16 11278416-5 2001 These data suggest that, among the endopeptidases whose activities are sensitive to thiorphan and phosphoramidon, NEP is the most potent Abeta-degrading enzyme in vivo. phosphoramidon 98-112 membrane metalloendopeptidase Homo sapiens 114-117 11459133-0 2001 Endothelium-dependent relaxation in response to low concentrations of bradykinin is enhanced by phosphoramidon, bosentan and BQ-123 in bovine coronary arteries in vitro. phosphoramidon 96-110 kininogen 1 Bos taurus 70-80 11438756-5 2001 The naturally derived metalloproteinase inhibitor phosphoramidon was docked in the active site of this model and comparisons with the respective NEP complex were made. phosphoramidon 50-64 membrane metalloendopeptidase Homo sapiens 145-148