PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 26631141-8 2016 UMR106 cell Fgf23 transcripts were increased by stimulation of SOCE and Ca(2+) ionophore ionomycin and decreased by Orai inhibitors 2-APB, YM58483 and SK&F96365, by Orai1 silencing, as well as by NFkappaB inhibitors wogonin, withaferin A, and CAS 545380-34-5. amicloral 151-157 fibroblast growth factor 23 Rattus norvegicus 12-17 26631141-8 2016 UMR106 cell Fgf23 transcripts were increased by stimulation of SOCE and Ca(2+) ionophore ionomycin and decreased by Orai inhibitors 2-APB, YM58483 and SK&F96365, by Orai1 silencing, as well as by NFkappaB inhibitors wogonin, withaferin A, and CAS 545380-34-5. amicloral 151-157 ORAI calcium release-activated calcium modulator 1 Rattus norvegicus 169-174 24630903-6 2014 [Ca(2+)]i and secretory responses to 2-APB at pH 6.5 were inhibited by the removal of extracellular Ca(2+) and SOC channel blockers such as SK&F96365, La(3+) and Gd(3+). amicloral 140-146 arginyl aminopeptidase Rattus norvegicus 39-42 25218985-10 2014 Only nifedipine and SK&F 96365 relaxed the arteries pre-contracted with endothelin-1. amicloral 20-26 endothelin 1 Rattus norvegicus 76-88 21767581-0 2011 SK&F 96365 induces apoptosis and autophagy by inhibiting Akt-mTOR signaling in A7r5 cells. amicloral 0-6 AKT serine/threonine kinase 1 Rattus norvegicus 61-64 23347013-5 2013 M-3M3FBS-induced Ca2 + influx was inhibited by nifedipine, econazole, SK&F96365, aristolochic acid, and GF109203X. amicloral 70-76 carbonic anhydrase 2 Homo sapiens 17-20 22212354-0 2012 Calcium influx blocked by SK&F 96365 modulates the LPS plus IFN-gamma-induced inflammatory response in murine peritoneal macrophages. amicloral 26-32 toll-like receptor 4 Mus musculus 55-58 22212354-0 2012 Calcium influx blocked by SK&F 96365 modulates the LPS plus IFN-gamma-induced inflammatory response in murine peritoneal macrophages. amicloral 26-32 interferon gamma Mus musculus 64-73 22212354-4 2012 Phagocytosis analyzing results showed that SK&F 96365 efficiently diminished the uptake of nonopsonized 1 muM yellow-green beads or pHrodo -labeled Escherichia coli bacteria both on the resting and LPS plus IFN-gamma-stimulated macrophages. amicloral 43-49 toll-like receptor 4 Mus musculus 202-205 22212354-4 2012 Phagocytosis analyzing results showed that SK&F 96365 efficiently diminished the uptake of nonopsonized 1 muM yellow-green beads or pHrodo -labeled Escherichia coli bacteria both on the resting and LPS plus IFN-gamma-stimulated macrophages. amicloral 43-49 interferon gamma Mus musculus 211-220 22212354-6 2012 The CBA analyzing results showed that SK&F 96365 pretreatment efficiently inhibited the production of LPS plus IFN-gamma-induced inflammatory cytokines of IL-6, MCP-1, TNF, INF-gamma, and IL-10. amicloral 38-44 toll-like receptor 4 Mus musculus 106-109 22212354-6 2012 The CBA analyzing results showed that SK&F 96365 pretreatment efficiently inhibited the production of LPS plus IFN-gamma-induced inflammatory cytokines of IL-6, MCP-1, TNF, INF-gamma, and IL-10. amicloral 38-44 interferon gamma Mus musculus 115-124 22212354-6 2012 The CBA analyzing results showed that SK&F 96365 pretreatment efficiently inhibited the production of LPS plus IFN-gamma-induced inflammatory cytokines of IL-6, MCP-1, TNF, INF-gamma, and IL-10. amicloral 38-44 interleukin 6 Mus musculus 159-163 22212354-6 2012 The CBA analyzing results showed that SK&F 96365 pretreatment efficiently inhibited the production of LPS plus IFN-gamma-induced inflammatory cytokines of IL-6, MCP-1, TNF, INF-gamma, and IL-10. amicloral 38-44 mast cell protease 1 Mus musculus 165-170 22212354-6 2012 The CBA analyzing results showed that SK&F 96365 pretreatment efficiently inhibited the production of LPS plus IFN-gamma-induced inflammatory cytokines of IL-6, MCP-1, TNF, INF-gamma, and IL-10. amicloral 38-44 tumor necrosis factor Mus musculus 172-175 22212354-6 2012 The CBA analyzing results showed that SK&F 96365 pretreatment efficiently inhibited the production of LPS plus IFN-gamma-induced inflammatory cytokines of IL-6, MCP-1, TNF, INF-gamma, and IL-10. amicloral 38-44 interleukin 10 Mus musculus 177-197 22212354-8 2012 Furthermore, SK&F 96365 pretreatment inhibited the LPS plus IFN-gamma-induced translocation of NF-kappaB to the nucleus, and induced a decrease in mitochondrial membrane potential (DeltaPsim) in LPS plus IFN-gamma-activated macrophages. amicloral 13-19 toll-like receptor 4 Mus musculus 55-58 22212354-8 2012 Furthermore, SK&F 96365 pretreatment inhibited the LPS plus IFN-gamma-induced translocation of NF-kappaB to the nucleus, and induced a decrease in mitochondrial membrane potential (DeltaPsim) in LPS plus IFN-gamma-activated macrophages. amicloral 13-19 interferon gamma Mus musculus 64-73 22212354-8 2012 Furthermore, SK&F 96365 pretreatment inhibited the LPS plus IFN-gamma-induced translocation of NF-kappaB to the nucleus, and induced a decrease in mitochondrial membrane potential (DeltaPsim) in LPS plus IFN-gamma-activated macrophages. amicloral 13-19 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 99-108 22212354-8 2012 Furthermore, SK&F 96365 pretreatment inhibited the LPS plus IFN-gamma-induced translocation of NF-kappaB to the nucleus, and induced a decrease in mitochondrial membrane potential (DeltaPsim) in LPS plus IFN-gamma-activated macrophages. amicloral 13-19 toll-like receptor 4 Mus musculus 199-202 22212354-8 2012 Furthermore, SK&F 96365 pretreatment inhibited the LPS plus IFN-gamma-induced translocation of NF-kappaB to the nucleus, and induced a decrease in mitochondrial membrane potential (DeltaPsim) in LPS plus IFN-gamma-activated macrophages. amicloral 13-19 interferon gamma Mus musculus 208-217 22474110-7 2012 Coadministration of SOC inhibitors SK&F96365 or Gd3+ with E2/P4 also suppressed the up-regulation of IGFBP-1 and hESC size increase. amicloral 35-41 insulin like growth factor binding protein 1 Homo sapiens 105-112 21767581-0 2011 SK&F 96365 induces apoptosis and autophagy by inhibiting Akt-mTOR signaling in A7r5 cells. amicloral 0-6 mechanistic target of rapamycin kinase Rattus norvegicus 65-69 21767581-5 2011 In addition, we found that SK&F 96365 inhibits Akt-mTOR signaling pathways, which is comparable with the efficacy of other known Akt inhibitors. amicloral 27-33 AKT serine/threonine kinase 1 Rattus norvegicus 51-54 21767581-5 2011 In addition, we found that SK&F 96365 inhibits Akt-mTOR signaling pathways, which is comparable with the efficacy of other known Akt inhibitors. amicloral 27-33 mechanistic target of rapamycin kinase Rattus norvegicus 55-59 21767581-5 2011 In addition, we found that SK&F 96365 inhibits Akt-mTOR signaling pathways, which is comparable with the efficacy of other known Akt inhibitors. amicloral 27-33 AKT serine/threonine kinase 1 Rattus norvegicus 133-136 21470712-6 2011 Upon the same stimulation, SK&F 96365 inhibited the expression of CD69 and CD25 on CD3+ T lymphocytes in a dose-dependent manner. amicloral 27-33 CD69 antigen Mus musculus 70-74 22135909-5 2011 Paroxetine-induced Ca2+ influx was inhibited by the store-operated Ca2+ channel blockers nifedipine, econazole and SK&F96365, and protein kinase C modulators. amicloral 115-121 carbonic anhydrase 2 Homo sapiens 19-22 22135909-5 2011 Paroxetine-induced Ca2+ influx was inhibited by the store-operated Ca2+ channel blockers nifedipine, econazole and SK&F96365, and protein kinase C modulators. amicloral 115-121 carbonic anhydrase 2 Homo sapiens 67-70 21770746-6 2011 This Ca(2+) influx was inhibited by phospholipase A2 inhibitor aristolochic acid, store-operated Ca(2+) channel blockers nifedipine and SK&F96365, and protein kinase C inhibitor GF109203X. amicloral 136-142 phospholipase A2 group IB Canis lupus familiaris 36-52 21470712-6 2011 Upon the same stimulation, SK&F 96365 inhibited the expression of CD69 and CD25 on CD3+ T lymphocytes in a dose-dependent manner. amicloral 27-33 interleukin 2 receptor, alpha chain Mus musculus 79-83 21470712-9 2011 Furthermore, SK&F 96365 significantly inhibited the production of proinflammatory cytokines (interferon (IFN)-gamma and tumor necrosis factor (TNF)), and the anti-inflammatory cytokine (IL-10) on both Con A- and PMA/ionomycin-activated lymphocytes. amicloral 13-19 interferon gamma Mus musculus 97-119 21470712-9 2011 Furthermore, SK&F 96365 significantly inhibited the production of proinflammatory cytokines (interferon (IFN)-gamma and tumor necrosis factor (TNF)), and the anti-inflammatory cytokine (IL-10) on both Con A- and PMA/ionomycin-activated lymphocytes. amicloral 13-19 tumor necrosis factor Mus musculus 124-145 21470712-9 2011 Furthermore, SK&F 96365 significantly inhibited the production of proinflammatory cytokines (interferon (IFN)-gamma and tumor necrosis factor (TNF)), and the anti-inflammatory cytokine (IL-10) on both Con A- and PMA/ionomycin-activated lymphocytes. amicloral 13-19 tumor necrosis factor Mus musculus 147-150 21470712-9 2011 Furthermore, SK&F 96365 significantly inhibited the production of proinflammatory cytokines (interferon (IFN)-gamma and tumor necrosis factor (TNF)), and the anti-inflammatory cytokine (IL-10) on both Con A- and PMA/ionomycin-activated lymphocytes. amicloral 13-19 interleukin 10 Mus musculus 190-195 18436303-8 2008 2-APB and SK&F 96365 were able to amplify the reduction of fMLF-stimulated Ca(2+) entry and H(2)O(2) production observed in cells transfected by TRPC3 siRNA. amicloral 10-16 transient receptor potential cation channel subfamily C member 3 Homo sapiens 149-154 21778596-6 2011 SK&F96365, a TRPC channel blocker, decreased the number of PVC and prevented VT in anesthetized Galpha(q)-TG mice (P<0.05). amicloral 0-6 guanine nucleotide binding protein, alpha q polypeptide Mus musculus 100-109 21778596-8 2011 SK&F96365 decreased the number of PVC and prevented VT in isolated Galpha(q)-TG hearts (P<0.01) even in the presence of OAG. amicloral 0-6 guanine nucleotide binding protein, alpha q polypeptide Mus musculus 71-80 20584631-6 2010 Interestingly, selective inhibition of p38 by either SB203580 or SK&F 86002 resulted in augmented IL-2 production by DN32.D3 cells after stimulation with alpha GC. amicloral 65-71 mitogen-activated protein kinase 14 Mus musculus 39-42 20584631-6 2010 Interestingly, selective inhibition of p38 by either SB203580 or SK&F 86002 resulted in augmented IL-2 production by DN32.D3 cells after stimulation with alpha GC. amicloral 65-71 interleukin 2 Mus musculus 102-106 21793331-3 2010 This Ca2+ influx was inhibited by phospholipase A2 inhibitor aristolochic acid but not by Ca2+ channel blockers such as nifedipine, nimodipine, nicardipine, diltiazem, verapamil, econazole and SK&F96365. amicloral 193-199 phospholipase A2 group IB Canis lupus familiaris 34-50 19317445-1 2009 3-(1H-Imidazol-4-yl)propylguanidine (SK&F 91486, 4) was identified as a potent partial agonist at the human histamine H(3) receptor (hH(3)R) and human histamine H(4) receptor (hH(4)R). amicloral 37-43 histamine receptor H3 Homo sapiens 112-135 19317445-1 2009 3-(1H-Imidazol-4-yl)propylguanidine (SK&F 91486, 4) was identified as a potent partial agonist at the human histamine H(3) receptor (hH(3)R) and human histamine H(4) receptor (hH(4)R). amicloral 37-43 histamine receptor H3 Homo sapiens 137-144 19317445-1 2009 3-(1H-Imidazol-4-yl)propylguanidine (SK&F 91486, 4) was identified as a potent partial agonist at the human histamine H(3) receptor (hH(3)R) and human histamine H(4) receptor (hH(4)R). amicloral 37-43 histamine receptor H4 Homo sapiens 155-178 19317445-1 2009 3-(1H-Imidazol-4-yl)propylguanidine (SK&F 91486, 4) was identified as a potent partial agonist at the human histamine H(3) receptor (hH(3)R) and human histamine H(4) receptor (hH(4)R). amicloral 37-43 histamine receptor H4 Homo sapiens 180-186 17845018-4 2007 These large inhibitors are not predicted to bind in that they protrude through the accessible surface calculated from a PNMT/7-aminosulfonyl-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) crystal structure, yet they are potent inhibitors of PNMT. amicloral 173-179 phenylethanolamine N-methyltransferase Homo sapiens 120-124 18243160-6 2008 The FcepsilonRIbeta ITAM was essential for overall calcium response upon weak FcepsilonRI stimulation (at low antigen concentration), while upon strong stimulation (at high antigen concentration) it appeared necessary selectively to an immediate calcium response that was sensitive to the dihydropyridine receptor (DHPR) antagonist nifedipine and wortmannin but not to the store-operated calcium entry (SOCE) antagonists such as 2-aminoethoxyphenyl borate and SK&F96365. amicloral 460-466 Fc epsilon receptor Ia Homo sapiens 4-15 18243160-6 2008 The FcepsilonRIbeta ITAM was essential for overall calcium response upon weak FcepsilonRI stimulation (at low antigen concentration), while upon strong stimulation (at high antigen concentration) it appeared necessary selectively to an immediate calcium response that was sensitive to the dihydropyridine receptor (DHPR) antagonist nifedipine and wortmannin but not to the store-operated calcium entry (SOCE) antagonists such as 2-aminoethoxyphenyl borate and SK&F96365. amicloral 460-466 calcium voltage-gated channel subunit alpha1 S Homo sapiens 289-313 17845018-4 2007 These large inhibitors are not predicted to bind in that they protrude through the accessible surface calculated from a PNMT/7-aminosulfonyl-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) crystal structure, yet they are potent inhibitors of PNMT. amicloral 173-179 phenylethanolamine N-methyltransferase Homo sapiens 242-246 16279783-1 2005 The X-ray structure of human phenylethanolamine N-methyltransferase (hPNMT) complexed with its product, S-adenosyl-L-homocysteine (4), and the most potent inhibitor reported to date, SK&F 64139 (7), was used to identify the residues involved in inhibitor binding. amicloral 183-189 phenylethanolamine N-methyltransferase Homo sapiens 29-67 16838106-4 2007 TRPC7-transfected HEK293 cells showed an augmentation of carbachol-induced intracellular Ca2+ transient, which was attenuated under a Ca2+-free condition or in the presence of SK&F96365 (a Ca2+-permeable channel blocker). amicloral 176-182 transient receptor potential cation channel subfamily C member 7 Homo sapiens 0-5 16838106-4 2007 TRPC7-transfected HEK293 cells showed an augmentation of carbachol-induced intracellular Ca2+ transient, which was attenuated under a Ca2+-free condition or in the presence of SK&F96365 (a Ca2+-permeable channel blocker). amicloral 176-182 carbonic anhydrase 2 Homo sapiens 89-92 16838106-6 2007 Ang II-induced apoptosis was inhibited by CV-11974 (Candesartan; Ang II type 1 [AT1] receptor blocker), SK&F96365, and FK506 (calcineurin inhibitor). amicloral 104-110 angiotensinogen Rattus norvegicus 0-6 16778360-6 2006 IL-6 mRNA induction by CA-G alpha13 was suppressed by SK&F96365 (1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole hydrochloride), an inhibitor of receptor-activated nonselective cation channels, and the expression of CA-G alpha13 increased basal Ca2+ influx. amicloral 54-60 interleukin 6 Rattus norvegicus 0-4 16778360-6 2006 IL-6 mRNA induction by CA-G alpha13 was suppressed by SK&F96365 (1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole hydrochloride), an inhibitor of receptor-activated nonselective cation channels, and the expression of CA-G alpha13 increased basal Ca2+ influx. amicloral 54-60 G protein subunit alpha 13 Rattus norvegicus 26-35 16778360-6 2006 IL-6 mRNA induction by CA-G alpha13 was suppressed by SK&F96365 (1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole hydrochloride), an inhibitor of receptor-activated nonselective cation channels, and the expression of CA-G alpha13 increased basal Ca2+ influx. amicloral 54-60 G protein subunit alpha 13 Rattus norvegicus 245-254 16519936-4 2006 Approximately 25% of the measured CaMKII autophosphorylation in DRG neurons in culture can be regulated by Ca(2+) flux from intracellular stores caused by manipulating [Ca(2+)](O), as shown by blocking refilling of store-operated Ca(2+)-channels with SK&F 96365, Ruthenium Red, and a partial block with Ni(2+). amicloral 251-257 calcium/calmodulin dependent protein kinase II gamma Homo sapiens 34-40 16622014-6 2006 Furthermore, the expression of p12(I) in Jurkat T cells using lentiviral vectors enhanced LFA-1-mediated cell adhesion, which was inhibited by the calcium chelator BAPTA-AM, the calcium channel blocker SK&F 96365, and calpeptin, an inhibitor of the calcium-dependent protease calpain. amicloral 202-208 DNA polymerase epsilon 4, accessory subunit Homo sapiens 31-34 16622014-6 2006 Furthermore, the expression of p12(I) in Jurkat T cells using lentiviral vectors enhanced LFA-1-mediated cell adhesion, which was inhibited by the calcium chelator BAPTA-AM, the calcium channel blocker SK&F 96365, and calpeptin, an inhibitor of the calcium-dependent protease calpain. amicloral 202-208 integrin subunit alpha L Homo sapiens 90-95 16539844-4 2006 A combination of DIDS (1 micromol/L) and SK&F96365 (1 micromol/L) significantly diminished ConA-induced ClC-3 mRNA expression by 64%, whereas DIDS(1 micromol/L) or SK&F96365 (1 micromol/L) alone decreased ConA-induced ClC-3 mRNA expression by only 16% and 9%, respectively. amicloral 41-47 chloride voltage-gated channel 3 Homo sapiens 108-113 16539844-4 2006 A combination of DIDS (1 micromol/L) and SK&F96365 (1 micromol/L) significantly diminished ConA-induced ClC-3 mRNA expression by 64%, whereas DIDS(1 micromol/L) or SK&F96365 (1 micromol/L) alone decreased ConA-induced ClC-3 mRNA expression by only 16% and 9%, respectively. amicloral 41-47 chloride voltage-gated channel 3 Homo sapiens 226-231 16279783-1 2005 The X-ray structure of human phenylethanolamine N-methyltransferase (hPNMT) complexed with its product, S-adenosyl-L-homocysteine (4), and the most potent inhibitor reported to date, SK&F 64139 (7), was used to identify the residues involved in inhibitor binding. amicloral 183-189 phenylethanolamine N-methyltransferase Homo sapiens 69-74 15953564-6 2005 The stimulation by bupleuran 2IIc/PG-1 of cyclin D2 expression was significantly decreased by inhibitors, PI 3-kinase (LY294002 and Wortmannin), PLCgamma (U73122), PKC (H-7), receptor-operated calcium entry inhibitor (SK&F 96365), and calcineurin (FK506). amicloral 218-224 cyclin D2 Mus musculus 42-51 15936930-5 2005 Pretreatment of the cells with calcium inhibitor SK&F96365 inhibited the LXA4-induced apoptosis, levels of [Ca2+]i, expression of calpain 10 and Smac. amicloral 49-55 calpain 10 Rattus norvegicus 134-144 15936930-5 2005 Pretreatment of the cells with calcium inhibitor SK&F96365 inhibited the LXA4-induced apoptosis, levels of [Ca2+]i, expression of calpain 10 and Smac. amicloral 49-55 diablo, IAP-binding mitochondrial protein Rattus norvegicus 149-153 15358810-10 2004 Pharmacological studies using the imidazole derivatives SK&F96365 (30 microM) and LOE 908 (10 microM) partially inhibited the ET1-evoked Ca2+ response, thus providing evidence for the presence of both store-operated Ca2+ channels and non-selective cationic channels in the human ST. amicloral 56-62 endothelin 1 Homo sapiens 130-133 15946532-5 2005 As compared with the control group, DIDS, SK&F96365 and Nifedipine could significantly reduce the PAG, Ca2+ release and Ca2+ influx in thrombin activated platelet (P < 0.05). amicloral 42-48 coagulation factor II, thrombin Homo sapiens 139-147 15946532-8 2005 The combination of NFA and SK&F96365 weakened each other"s effect on Ca2+ release (P < 0.05), while NFA and nifedipine weakened each other"s effects on PAG, Ca2+ release and Ca2+ influx in thrombin activated platelet (P < 0.05). amicloral 27-33 coagulation factor II, thrombin Homo sapiens 196-204 15358810-10 2004 Pharmacological studies using the imidazole derivatives SK&F96365 (30 microM) and LOE 908 (10 microM) partially inhibited the ET1-evoked Ca2+ response, thus providing evidence for the presence of both store-operated Ca2+ channels and non-selective cationic channels in the human ST. amicloral 56-62 carbonic anhydrase 2 Homo sapiens 141-144 12847111-7 2003 Moreover, LPA-induced increases in Ca2+ transients and/or iNOS expression in highly purified rat liver nuclei were prevented by pertussis toxin, phosphoinositide 3-kinase/Akt inhibitor wortmannin and Ca2+ chelator and channel blockers EGTA and SK&F96365, respectively. amicloral 244-250 nitric oxide synthase 2 Rattus norvegicus 58-62 12922939-8 2003 Both SK&F 96365 and LOE 908 inhibited ET-1-induced arachidonic acid release with the IC(50) values correlated to those of ET-1-induced Ca(2+) influx. amicloral 5-11 endothelin 1 Homo sapiens 42-46 12920205-5 2003 Both SK&F 96365 and LOE 908 inhibited ET-1-induced AA release with the IC50 values correlated to those of ET-1-induced Ca2+ influx. amicloral 5-11 endothelin-1 Cricetulus griseus 42-46 12920205-5 2003 Both SK&F 96365 and LOE 908 inhibited ET-1-induced AA release with the IC50 values correlated to those of ET-1-induced Ca2+ influx. amicloral 5-11 endothelin-1 Cricetulus griseus 110-114 12922939-8 2003 Both SK&F 96365 and LOE 908 inhibited ET-1-induced arachidonic acid release with the IC(50) values correlated to those of ET-1-induced Ca(2+) influx. amicloral 5-11 endothelin 1 Homo sapiens 126-130 12496270-9 2003 5) The constitutive expression of TGF-beta1 as well as up-regulation of the PA system observed in HRA cells was inhibited by preinoculation of the cells with bikunin or calcium channel blocker SK&F 96365 but not with nifedipine or verapamil, with an IC(50) of approximately 100 nm for bikunin or approximately 30 microm for SK&F 96365, respectively, as measured by enzyme-linked immunosorbent assay. amicloral 193-199 transforming growth factor beta 1 Homo sapiens 34-43 12496270-9 2003 5) The constitutive expression of TGF-beta1 as well as up-regulation of the PA system observed in HRA cells was inhibited by preinoculation of the cells with bikunin or calcium channel blocker SK&F 96365 but not with nifedipine or verapamil, with an IC(50) of approximately 100 nm for bikunin or approximately 30 microm for SK&F 96365, respectively, as measured by enzyme-linked immunosorbent assay. amicloral 193-199 alpha-1-microglobulin/bikunin precursor Homo sapiens 289-296 12496270-9 2003 5) The constitutive expression of TGF-beta1 as well as up-regulation of the PA system observed in HRA cells was inhibited by preinoculation of the cells with bikunin or calcium channel blocker SK&F 96365 but not with nifedipine or verapamil, with an IC(50) of approximately 100 nm for bikunin or approximately 30 microm for SK&F 96365, respectively, as measured by enzyme-linked immunosorbent assay. amicloral 328-334 transforming growth factor beta 1 Homo sapiens 34-43 12496270-9 2003 5) The constitutive expression of TGF-beta1 as well as up-regulation of the PA system observed in HRA cells was inhibited by preinoculation of the cells with bikunin or calcium channel blocker SK&F 96365 but not with nifedipine or verapamil, with an IC(50) of approximately 100 nm for bikunin or approximately 30 microm for SK&F 96365, respectively, as measured by enzyme-linked immunosorbent assay. amicloral 328-334 alpha-1-microglobulin/bikunin precursor Homo sapiens 158-165 12529253-7 2003 The Ca(2+) channels activated by ET-1 in wortmannin- or LY-294002-treated CHO-ET(B)R were sensitive to LOE 908 and resistant to SK&F 96365. amicloral 128-134 endothelin-1 Cricetulus griseus 33-37 12568361-6 2003 SK&F96365 blocked vasopressin-induced Ca2+ influx in a dose-dependent manner. amicloral 0-6 arginine vasopressin Rattus norvegicus 22-33 11827704-8 2002 Furthermore, p38 MAPK inhibitors SB203580 or SK&F86002 markedly reduced oxLDL-induced CXCR2 expression. amicloral 45-51 mitogen-activated protein kinase 14 Homo sapiens 13-16 12427604-1 2002 The purpose of this study was to demonstrate the involvement of Ca(2+) influx through voltage-independent Ca(2+) channels (VICCs) in endothelin-1 (ET-1)-induced transactivation of epidermal growth factor receptor protein tyrosine kinase (EGFR PTK) using the Ca(2+) channel blockers LOE-908 and SK&F-96365 in rabbit internal carotid artery vascular smooth muscle cells. amicloral 294-300 endothelin-1 Oryctolagus cuniculus 133-145 12427604-1 2002 The purpose of this study was to demonstrate the involvement of Ca(2+) influx through voltage-independent Ca(2+) channels (VICCs) in endothelin-1 (ET-1)-induced transactivation of epidermal growth factor receptor protein tyrosine kinase (EGFR PTK) using the Ca(2+) channel blockers LOE-908 and SK&F-96365 in rabbit internal carotid artery vascular smooth muscle cells. amicloral 294-300 endothelin-1 Oryctolagus cuniculus 147-151 12427604-1 2002 The purpose of this study was to demonstrate the involvement of Ca(2+) influx through voltage-independent Ca(2+) channels (VICCs) in endothelin-1 (ET-1)-induced transactivation of epidermal growth factor receptor protein tyrosine kinase (EGFR PTK) using the Ca(2+) channel blockers LOE-908 and SK&F-96365 in rabbit internal carotid artery vascular smooth muscle cells. amicloral 294-300 epidermal growth factor receptor Oryctolagus cuniculus 180-212 12198330-7 2002 Both LOE 908 and SK&F 96365 inhibit endothelin-1-induced contraction in a concentration-dependent manner, and their combination abolished it. amicloral 17-23 endothelin-1 Oryctolagus cuniculus 40-52 12183654-8 2002 SK&F 96365 and econazole but not GdCl(3) inhibited PACAP-induced CA release. amicloral 0-6 adenylate cyclase activating polypeptide 1 Bos taurus 55-60 12131556-1 2002 Endothelin-1 (ET-1) has been shown to activate three types of Ca2+ channel, namely two Ca2+-permeable nonselective cation channels (designated NSCC-1 and NSCC-2) and a store-operated Ca2+ channel (SOCC), and that these channels can be discriminated by Ca2+ channel blockers such as LOE 908 (a blocker of NSCC-1 and NSCC-2) and SK&F 96365 (a blocker of NSCC-2 and SOCC). amicloral 327-333 endothelin 1 Rattus norvegicus 0-12 12131556-1 2002 Endothelin-1 (ET-1) has been shown to activate three types of Ca2+ channel, namely two Ca2+-permeable nonselective cation channels (designated NSCC-1 and NSCC-2) and a store-operated Ca2+ channel (SOCC), and that these channels can be discriminated by Ca2+ channel blockers such as LOE 908 (a blocker of NSCC-1 and NSCC-2) and SK&F 96365 (a blocker of NSCC-2 and SOCC). amicloral 327-333 endothelin 1 Rattus norvegicus 14-18 12088864-10 2002 Both SK&F 96365, a receptor-operated Ca(2+) channel (ROC) blocker and nimodipine, an L-type Ca(2+) channel blocker, reduced BK-induced [Ca(2+)](i) increase and glucagon release. amicloral 5-11 kininogen 1 Homo sapiens 128-130 12069846-5 2002 The thapsigargin-induced activation of NF-kappaB was inhibited by the PAF synthesis inhibitor SK&F 98625 and the PAF antagonist E6123. amicloral 94-100 PCNA clamp associated factor Rattus norvegicus 70-73 12005183-3 2002 Both nifedipine and SK&F96365 inhibited 10 nM ET-1-induced [3H]-thymidine incorporation into VSMC with the maximal inhibitory concentrations of 1 and 10 microM, respectively. amicloral 20-26 endothelin 1 Rattus norvegicus 50-54 12005183-6 2002 Pretreatment of VSMC with 1 microM nifedipine completely inhibited the DIDS effect on 10 nM ET-1-induced [3H]-thymidine incorporation into VSMC and sustained increase in [Ca2+]i, whereas pretreatment with 10 microM SK&F96365 did not completely block these effects of DIDS. amicloral 215-221 endothelin 1 Rattus norvegicus 92-96 11827704-8 2002 Furthermore, p38 MAPK inhibitors SB203580 or SK&F86002 markedly reduced oxLDL-induced CXCR2 expression. amicloral 45-51 C-X-C motif chemokine receptor 2 Homo sapiens 90-95 11600432-2 2001 In both CHO-ET(A) and CHO-ET(B), ET-1 at 0.1 nM activated the Ca(2+)-permeable nonselective cation channel-1 (NSCC-1), which was sensitive to LOE-908 and resistant to SK&F-96365. amicloral 167-173 endothelin-1 Cricetulus griseus 33-37 11779582-6 2002 The SK&F 98625-induced suppression of interleukin-6 mRNA accumulation and interleukin-6 production was partially restored by addition of exogenous prostaglandin E2. amicloral 4-10 interleukin 6 Rattus norvegicus 42-55 11779582-6 2002 The SK&F 98625-induced suppression of interleukin-6 mRNA accumulation and interleukin-6 production was partially restored by addition of exogenous prostaglandin E2. amicloral 4-10 interleukin 6 Rattus norvegicus 78-91 11786495-16 2002 The ET-1-induced hyperpolarisation was insensitive to nifedipine but was attenuated by SK&F 96365 (1 - [beta-[3-(4 - methoxy - phenyl)propoxy] - 4 - methoxyphenethyl] - 1H-imidazole hydrochloride, 50 microM), an inhibitor of receptor-mediated Ca(2+) entry. amicloral 87-93 endothelin-1 Cavia porcellus 4-8 11600432-4 2001 ET-1 at 10 nM activated the same channels as 1 nM ET-1 in both cell types, but in CHO-ET(A), it additionally activated the store-operated Ca(2+) channel (SOCC), which was resistant to LOE-908 and sensitive to SK&F-96365. amicloral 209-215 endothelin-1 Cricetulus griseus 0-4 11494311-5 2001 SK&F 96365 inhibited capacitative Ca2+ entry in a dose-dependent manner (I50: 1-5 microM). amicloral 0-6 carbonic anhydrase 2 Mus musculus 38-41 11494311-11 2001 These results indicate that the inhibitory effects of SK&F 96365 and DBHQ on cell proliferation were due to the inhibition of capacitative Ca2+ entry and Ca2+ mobilization suggesting the importance of capacitative Ca2+ entry and Ca2+ mobilization in the control of EGF-induced cell cycle progression in mouse mammary epithelial cells. amicloral 54-60 carbonic anhydrase 2 Mus musculus 143-146 11494311-11 2001 These results indicate that the inhibitory effects of SK&F 96365 and DBHQ on cell proliferation were due to the inhibition of capacitative Ca2+ entry and Ca2+ mobilization suggesting the importance of capacitative Ca2+ entry and Ca2+ mobilization in the control of EGF-induced cell cycle progression in mouse mammary epithelial cells. amicloral 54-60 carbonic anhydrase 2 Mus musculus 158-161 11494311-11 2001 These results indicate that the inhibitory effects of SK&F 96365 and DBHQ on cell proliferation were due to the inhibition of capacitative Ca2+ entry and Ca2+ mobilization suggesting the importance of capacitative Ca2+ entry and Ca2+ mobilization in the control of EGF-induced cell cycle progression in mouse mammary epithelial cells. amicloral 54-60 carbonic anhydrase 2 Mus musculus 158-161 11494311-11 2001 These results indicate that the inhibitory effects of SK&F 96365 and DBHQ on cell proliferation were due to the inhibition of capacitative Ca2+ entry and Ca2+ mobilization suggesting the importance of capacitative Ca2+ entry and Ca2+ mobilization in the control of EGF-induced cell cycle progression in mouse mammary epithelial cells. amicloral 54-60 carbonic anhydrase 2 Mus musculus 158-161 11494311-11 2001 These results indicate that the inhibitory effects of SK&F 96365 and DBHQ on cell proliferation were due to the inhibition of capacitative Ca2+ entry and Ca2+ mobilization suggesting the importance of capacitative Ca2+ entry and Ca2+ mobilization in the control of EGF-induced cell cycle progression in mouse mammary epithelial cells. amicloral 54-60 epidermal growth factor Mus musculus 269-272 11522324-1 2001 Ca(2+) channels activated by endothelin-1 (ET-1) in C6 glioma cells (C6 cells) were characterized using whole-cell patch-clamps and by monitoring the intracellular free Ca(2+) concentration ([Ca(2+)](i)), when administering Ca(2+) channel blockers such as LOE 908 and SK&F 96365. amicloral 268-274 endothelin 1 Homo sapiens 29-41 11522324-1 2001 Ca(2+) channels activated by endothelin-1 (ET-1) in C6 glioma cells (C6 cells) were characterized using whole-cell patch-clamps and by monitoring the intracellular free Ca(2+) concentration ([Ca(2+)](i)), when administering Ca(2+) channel blockers such as LOE 908 and SK&F 96365. amicloral 268-274 endothelin 1 Homo sapiens 43-47 11065174-3 2000 Removal of extracellular Ca2+ as well as SK&F96365 reduced the contraction due to the PAR-1 agonist TFLLR-NH2 (TFp-NH2) by 60-80% that was similar to the extent of the inhibition by nifedipine. amicloral 41-47 coagulation factor II (thrombin) receptor Rattus norvegicus 90-95 11444496-2 2001 In cultured porcine aortic endothelial cells, the sustained increases in the intracellular Ca2+ concentration ([Ca2+]i) elicited by bradykinin and cyclopiazonic acid, which were strongly dependent on the presence of extracellular Ca2+, were suppressed by the NSCC blockers, SK&F 96365 and mefenamic acid. amicloral 274-280 kininogen 1 Homo sapiens 132-142 11444496-4 2001 In the presence of SK&F 96365 or mefenamic acid, the peak amplitude was severely reduced and the decay phase of hyperpolarization to bradykinin was greatly accelerated, which was apparently similar to the response obtained in Ca2+-free medium. amicloral 19-25 kininogen 1 Homo sapiens 137-147 11282120-6 2001 The contractile response to vasopressin was partly inhibited by nifedipine, SK&F 96365 (1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole) and niflumic acid. amicloral 76-82 arginine vasopressin Rattus norvegicus 28-39 11082111-13 2000 Ang II-induced contraction was insensitive to inhibition by nifedipine (0.1 microM), an antagonist of L-type voltage-gated Ca(2+) channels, and SK&F96365 (10 microM), which blocks non-selective cation channels, whereas that to ET-1 was inhibited by SK&F69365. amicloral 144-150 angiotensinogen Rattus norvegicus 0-6 11082111-13 2000 Ang II-induced contraction was insensitive to inhibition by nifedipine (0.1 microM), an antagonist of L-type voltage-gated Ca(2+) channels, and SK&F96365 (10 microM), which blocks non-selective cation channels, whereas that to ET-1 was inhibited by SK&F69365. amicloral 253-259 angiotensinogen Rattus norvegicus 0-6 11034409-11 2000 Both capsaicin and SK&F96365 also inhibited PAF-induced cytosolic superoxide generation in HL-60 cells differentiated by all-trans-retinoic acid. amicloral 19-25 PCNA clamp associated factor Homo sapiens 48-51 10496327-8 1999 The responses to lower concentrations of ET-1 (< or = 0.1 nM) were abolished by either SK&F 96365 or LOE 908 alone. amicloral 90-96 endothelin 1 Rattus norvegicus 41-45 11078350-4 2000 Our results show that the response to lower concentrations of ET-1 involves only one Ca2+ channel which is sensitive to SK&F 96365 and LOE 908 (NSCC-2). amicloral 120-126 endothelin 1 Rattus norvegicus 62-66 11078350-5 2000 In contrast, the response to higher concentrations of ET-1 involves two types of Ca2+ channel in addition to NSCC-2: one is sensitive to SK&F 96365 but resistant to LOE 908 (SOCC), and the other is resistant to SK&F 96365 but sensitive to LOE 908 (NSCC-1). amicloral 137-143 endothelin 1 Rattus norvegicus 54-58 11078350-5 2000 In contrast, the response to higher concentrations of ET-1 involves two types of Ca2+ channel in addition to NSCC-2: one is sensitive to SK&F 96365 but resistant to LOE 908 (SOCC), and the other is resistant to SK&F 96365 but sensitive to LOE 908 (NSCC-1). amicloral 215-221 endothelin 1 Rattus norvegicus 54-58 11078351-7 2000 In contrast, the increase caused by higher concentrations of ET-1 (> or = 1 nM) was suppressed by SK&F 96365 or LOE 908 to about 35% of controls, and abolished by combined treatment with SK&F 96365 and LOE 908. amicloral 101-107 endothelin 1 Rattus norvegicus 61-65 11078351-7 2000 In contrast, the increase caused by higher concentrations of ET-1 (> or = 1 nM) was suppressed by SK&F 96365 or LOE 908 to about 35% of controls, and abolished by combined treatment with SK&F 96365 and LOE 908. amicloral 194-200 endothelin 1 Rattus norvegicus 61-65 10619177-6 1999 These results indicate that ET-1 augments the release of catecholamines from adrenal chromaffin cells through ET(A) receptors, by activating two types of Ca2+ entry channels in addition to L-type VOCC: one (nonselective cation channel-1; NSCC-1) is sensitive to LOE 908 but resistant to SK&F 96365, whereas the other (NSCC-2) is sensitive to both LOE 908 and SK&F 96365. amicloral 287-293 endothelin 1 Bos taurus 28-32 10619177-6 1999 These results indicate that ET-1 augments the release of catecholamines from adrenal chromaffin cells through ET(A) receptors, by activating two types of Ca2+ entry channels in addition to L-type VOCC: one (nonselective cation channel-1; NSCC-1) is sensitive to LOE 908 but resistant to SK&F 96365, whereas the other (NSCC-2) is sensitive to both LOE 908 and SK&F 96365. amicloral 363-369 endothelin 1 Bos taurus 28-32 10629863-8 1999 In contrast, the increase in [Ca2+]i induced by higher concentrations of ET-1 was partially suppressed to approximately 30% of controls by either SK&F 96365 or LOE 908 alone, and it was abolished by their combination. amicloral 146-152 endothelin 1 Rattus norvegicus 73-77 10629864-6 1999 The responses to lower concentrations (< or = 0.1 nM) of ET-1 were abolished by either SK&F 96365 or LOE 908. amicloral 90-96 endothelin 1 Rattus norvegicus 60-64 10629864-8 1999 4) These results show that the contractions and increases in [Ca2+]i of rat aortic smooth muscles at lower concentrations of ET-1 involve only one Ca2+ entry channel which is sensitive to SK&F 96365 and LOE 908 (NSCC-2), whereas those at higher concentrations of ET-1 involve another Ca2+ entry channel which is sensitive to SK&F 96365 but resistant to LOE 908 (SOCC) in addition to the former channel. amicloral 188-194 endothelin 1 Rattus norvegicus 125-129 10629864-8 1999 4) These results show that the contractions and increases in [Ca2+]i of rat aortic smooth muscles at lower concentrations of ET-1 involve only one Ca2+ entry channel which is sensitive to SK&F 96365 and LOE 908 (NSCC-2), whereas those at higher concentrations of ET-1 involve another Ca2+ entry channel which is sensitive to SK&F 96365 but resistant to LOE 908 (SOCC) in addition to the former channel. amicloral 188-194 endothelin 1 Rattus norvegicus 267-271 10629864-8 1999 4) These results show that the contractions and increases in [Ca2+]i of rat aortic smooth muscles at lower concentrations of ET-1 involve only one Ca2+ entry channel which is sensitive to SK&F 96365 and LOE 908 (NSCC-2), whereas those at higher concentrations of ET-1 involve another Ca2+ entry channel which is sensitive to SK&F 96365 but resistant to LOE 908 (SOCC) in addition to the former channel. amicloral 329-335 endothelin 1 Rattus norvegicus 125-129 10496327-9 1999 In contrast, the responses to higher concentrations of ET-1 (> or = 1 nM) were suppressed by SK&F 96365 or LOE 908 to about 10% and 35% of controls, respectively, and abolished by combined treatment with SK&F 96365 and LOE 908. amicloral 96-102 endothelin 1 Rattus norvegicus 55-59 10496327-9 1999 In contrast, the responses to higher concentrations of ET-1 (> or = 1 nM) were suppressed by SK&F 96365 or LOE 908 to about 10% and 35% of controls, respectively, and abolished by combined treatment with SK&F 96365 and LOE 908. amicloral 211-217 endothelin 1 Rattus norvegicus 55-59 10496327-10 1999 These results show that the responses of rat aorta to lower concentrations of ET-1 involve only one Ca2+ channel that is sensitive to SK&F 96365 and LOE 908 (NSCC-2), whereas those to higher concentrations of ET-1 involve NSCC-1, NSCC-2 and SOCC, contributing 10%, 55% and 35%, respectively, to total Ca2+ entry. amicloral 134-140 endothelin 1 Rattus norvegicus 78-82 10448892-4 1999 SNP (10 microM), NOC-9 (10 microM) and BNP (1 microM) all increased intracellular cyclic GMP to similar levels (2- to 2.5-fold above basal) and caused significant enhancement of CGRP (10 nM)-induced cyclic AMP accumulation similar to that caused by 10 microM SK&F 94120. amicloral 259-265 natriuretic peptide B Rattus norvegicus 39-42 10448892-4 1999 SNP (10 microM), NOC-9 (10 microM) and BNP (1 microM) all increased intracellular cyclic GMP to similar levels (2- to 2.5-fold above basal) and caused significant enhancement of CGRP (10 nM)-induced cyclic AMP accumulation similar to that caused by 10 microM SK&F 94120. amicloral 259-265 calcitonin-related polypeptide alpha Rattus norvegicus 178-182 10455288-6 1999 The responses to lower concentrations (< or =0.1 nM) of ET-1 were abolished by either SK&F 96365 or LOE 908. amicloral 89-95 endothelin 1 Rattus norvegicus 59-63 10443571-4 1999 (2) Endothelin-1-induced vasoconstriction is mediated by Ca2+ influx through a non-selective cation channel sensitive to 1-[beta-[3-(4-methoxyphenyl) propoxyl]-4-methoxyphenethyl]-1H-imidazole HCl (SK & F96365). amicloral 198-205 endothelin 1 Homo sapiens 4-16 10354406-7 1999 Remarkably, 7-aminosulfonyl-3-hydroxymethyl-THIQ (12; PNMT Ki = 0.34 microM, alpha2 Ki = 1400 microM, selectivity = 4100) displayed a 23-680-fold enhanced selectivity over the parent compounds 27 (SK&F 29661; PNMT Ki = 0.55 microM, alpha2 Ki = 100 microM, selectivity = 180) and 4 (selectivity = 6.0) and is thus the most selective PNMT inhibitor yet reported. amicloral 197-203 phenylethanolamine N-methyltransferase Homo sapiens 54-58 10354406-7 1999 Remarkably, 7-aminosulfonyl-3-hydroxymethyl-THIQ (12; PNMT Ki = 0.34 microM, alpha2 Ki = 1400 microM, selectivity = 4100) displayed a 23-680-fold enhanced selectivity over the parent compounds 27 (SK&F 29661; PNMT Ki = 0.55 microM, alpha2 Ki = 100 microM, selectivity = 180) and 4 (selectivity = 6.0) and is thus the most selective PNMT inhibitor yet reported. amicloral 197-203 phenylethanolamine N-methyltransferase Homo sapiens 213-217 10354406-7 1999 Remarkably, 7-aminosulfonyl-3-hydroxymethyl-THIQ (12; PNMT Ki = 0.34 microM, alpha2 Ki = 1400 microM, selectivity = 4100) displayed a 23-680-fold enhanced selectivity over the parent compounds 27 (SK&F 29661; PNMT Ki = 0.55 microM, alpha2 Ki = 100 microM, selectivity = 180) and 4 (selectivity = 6.0) and is thus the most selective PNMT inhibitor yet reported. amicloral 197-203 phenylethanolamine N-methyltransferase Homo sapiens 213-217 10455288-8 1999 SK&F 96365 inhibited the LOE 908-resistant contractions induced by higher concentrations of ET-1 with IC50 values similar to those for contractions induced by thapsigargin or ionomycin. amicloral 0-6 endothelin 1 Rattus norvegicus 96-100 10455288-9 1999 These results show that the contractions and increases in [Ca2+]i of rat aortic smooth muscles at lower concentrations of ET-1 involve only one Ca2+ entry channel which is sensitive to SK&F 96365 and LOE 908 (NSCC-2), whereas those at higher concentrations of ET-1 involve another Ca2+ entry channel which is sensitive to SK&F 96365 but resistant to LOE 908 (SOCC) in addition to the former channel. amicloral 185-191 endothelin 1 Rattus norvegicus 122-126 10455288-9 1999 These results show that the contractions and increases in [Ca2+]i of rat aortic smooth muscles at lower concentrations of ET-1 involve only one Ca2+ entry channel which is sensitive to SK&F 96365 and LOE 908 (NSCC-2), whereas those at higher concentrations of ET-1 involve another Ca2+ entry channel which is sensitive to SK&F 96365 but resistant to LOE 908 (SOCC) in addition to the former channel. amicloral 185-191 endothelin 1 Rattus norvegicus 264-268 10463102-7 1999 SK&F 96365 had a stimulatory effect on PAF-induced [Ca2+]i rise and on fMLP-induced O2- production, this phenomenon was not observed with extracellular Ca2+ removal or chelation. amicloral 0-6 PCNA clamp associated factor Homo sapiens 43-46 10463102-7 1999 SK&F 96365 had a stimulatory effect on PAF-induced [Ca2+]i rise and on fMLP-induced O2- production, this phenomenon was not observed with extracellular Ca2+ removal or chelation. amicloral 0-6 formyl peptide receptor 1 Homo sapiens 75-79 10204997-13 1999 The sustained increases by lower and higher [ET-1] were abolished by removal of extracellular Ca2+, and they were suppressed by LOE 908 to 0 and 35%, respectively, with the LOE 908-resistant part being abolished by SK&F 96365. amicloral 215-221 endothelin 1 Rattus norvegicus 45-49 9873525-1 1998 A series of amidine substituted phenyl-, benzyl-, and phenethylimidazoles based on the known H3 agonist SK&F 91606 (4) has been synthesized and tested as ligands for the histamine H3 receptor. amicloral 104-110 histamine receptor H3 Homo sapiens 174-195 9795163-10 1998 SK&F 96365 inhibited VIP-induced secretion completely and rises in [Ca2+]i by 75%. amicloral 0-6 vasoactive intestinal peptide Rattus norvegicus 25-28 9776313-1 1998 SK&F 96365 (1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenylethyl]-1H-imi dazole hydrochloride) stimulated the accumulation of [3H]inositol monophosphates ([3H]IP1) in human U373 MG astrocytoma cells prelabelled with [3H]inositol (EC50 15 +/- 1 microM, Hill coefficient 3.8 +/- 0.4). amicloral 0-6 inhibitor of nuclear factor kappa B kinase regulatory subunit gamma Homo sapiens 168-171 9776313-2 1998 SK&F 96365-induced accumulation of [3H]IP1 increased linearly with time, but there was no initial rapid formation of [3H]IP3. amicloral 0-6 inhibitor of nuclear factor kappa B kinase regulatory subunit gamma Homo sapiens 43-46 9776313-4 1998 SK&F 96365-induced accumulation of [3H]IP1 in U373 MG cells increased as extracellular Ca2+ was increased from nominally zero to 4 mM, but there was no evidence that SK&F 96365 induced any marked entry of Ca2+ into cells; only an inhibition of store-refilling-induced Ca2+ entry was apparent. amicloral 0-6 inhibitor of nuclear factor kappa B kinase regulatory subunit gamma Homo sapiens 43-46 9809851-9 1998 The significant increases in sniffing, grooming and intense grooming and the significant decrease in stillness induced by the DA D1 agonist, SK&F 38393 [(+/-)-1-phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrochloride], were not altered by concomitant pre-treatment with NDL-249. amicloral 141-147 defender against cell death 1 Rattus norvegicus 126-131 9834082-2 1998 Here, we report that inhibitors of the p38 mitogen-activated kinase (p38 MAPK), SK&F 86002 or the more selective inhibitor, SB 203580, reduce the levels of soluble CD23 formed by IL-4-stimulated human monocytes or the human monocytic cell line, U937. amicloral 80-86 mitogen-activated protein kinase 14 Homo sapiens 39-42 9834082-2 1998 Here, we report that inhibitors of the p38 mitogen-activated kinase (p38 MAPK), SK&F 86002 or the more selective inhibitor, SB 203580, reduce the levels of soluble CD23 formed by IL-4-stimulated human monocytes or the human monocytic cell line, U937. amicloral 80-86 Fc epsilon receptor II Homo sapiens 168-172 9834082-2 1998 Here, we report that inhibitors of the p38 mitogen-activated kinase (p38 MAPK), SK&F 86002 or the more selective inhibitor, SB 203580, reduce the levels of soluble CD23 formed by IL-4-stimulated human monocytes or the human monocytic cell line, U937. amicloral 80-86 interleukin 4 Homo sapiens 183-187 9834082-4 1998 Further, evaluation of surface intact CD23 (iCD23) by flow cytometry demonstrated that SK&F 86002 and SB 203580 reduced the surface expression of iCD23 in a concentration-dependent fashion, while batimastat increased the surface expression of iCD23. amicloral 87-93 Fc epsilon receptor II Homo sapiens 38-42 9723969-14 1998 The current at lower [ET-1] was resistant to SK&F 96365 but was abolished by replacement of Ca2+ in the bath solution with Mn2+. amicloral 45-51 endothelin 1 Rattus norvegicus 22-26 9723969-15 1998 The current at higher [ET-1] was abolished by the replacement plus SK&F 96365. amicloral 67-73 endothelin 1 Rattus norvegicus 23-27 9723969-17 1998 In a bath solution containing only Ca2+ as a movable cation, ET-1 evoked currents: the current at lower [ET-1] was sensitive to Mn2+, whereas that at higher [ET-1] was partly sensitive to SK&F 96365. amicloral 188-194 endothelin 1 Rattus norvegicus 61-65 9600332-0 1998 Inhibition of tumor necrosis factor-alpha production by SK&F 98625, a CoA-independent transacylase inhibitor, in cultured rat peritoneal macrophages. amicloral 56-62 tumor necrosis factor Rattus norvegicus 14-41 9716353-13 1998 Finally, increasing doses of alnespirone or 8-OH-DPAT weakly increased sniffing induced by apomorphine (0.75 mg/kg, s.c.) in mice and decreased grooming induced by the dopamine D1 receptor agonist SK&F 39393 ((+/-)-1-phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol, 1.87 mg/kg, s.c.), whereas buspirone decreased both apomorphine-induced sniffing and SK&F 39393-induced grooming. amicloral 197-203 dopamine receptor D1 Mus musculus 168-188 9716360-5 1998 HCl(SK&F 96365) suppressed the endothelin-1-induced contraction and increase in [Ca2+]i to the level similar to that after removal of extracellular Ca2+. amicloral 4-10 endothelin 1 Homo sapiens 35-47 9600332-2 1998 In the presence of SK&F 98625, a CoA-independent transacylase inhibitor, the thapsigargin-induced TNF-alpha production was inhibited dose-dependently. amicloral 19-25 tumor necrosis factor Rattus norvegicus 102-111 9600332-3 1998 Platelet-activating factor (PAF) and prostaglandin E2 (PGE2) production were also inhibited by SK&F 98625. amicloral 95-101 PCNA clamp associated factor Rattus norvegicus 0-26 9600332-3 1998 Platelet-activating factor (PAF) and prostaglandin E2 (PGE2) production were also inhibited by SK&F 98625. amicloral 95-101 PCNA clamp associated factor Rattus norvegicus 28-31 9600332-4 1998 The SK&F 98625-induced inhibition of TNF-alpha production was not prevented by addition of PGE2. amicloral 4-10 tumor necrosis factor Rattus norvegicus 41-50 9600332-6 1998 The inhibition by SK&F 98625 of thapsigargin-induced TNF-alpha production might be partly due to the inhibition of PAF production. amicloral 18-24 tumor necrosis factor Rattus norvegicus 57-66 9600332-6 1998 The inhibition by SK&F 98625 of thapsigargin-induced TNF-alpha production might be partly due to the inhibition of PAF production. amicloral 18-24 PCNA clamp associated factor Rattus norvegicus 119-122 9698043-6 1998 It indicated that SK&F 108566 is a high affinity competitive antagonist at AT1 receptors in the proximal tubule. amicloral 18-24 angiotensin II receptor, type 1a Rattus norvegicus 79-82 9406590-0 1997 Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. amicloral 125-131 phenylethanolamine N-methyltransferase Homo sapiens 162-200 9406590-1 1997 7-(Aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661, 1) is a potent inhibitor of the enzyme phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28). amicloral 50-56 phenylethanolamine N-methyltransferase Homo sapiens 105-143 9406590-1 1997 7-(Aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661, 1) is a potent inhibitor of the enzyme phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28). amicloral 50-56 phenylethanolamine N-methyltransferase Homo sapiens 145-149 9406818-4 1997 Removal of extracellular Ca2+ or addition of Ca2+-entry blocker La3+ or SK&F 96365 inhibited Ca(i) oscillations, suggesting that Ca(i) oscillations in ras-transfected HaCaT keratinocytes were dependent on Ca2+ influx across the plasma membrane. amicloral 72-78 carbonic anhydrase 1 Homo sapiens 97-102 9406818-4 1997 Removal of extracellular Ca2+ or addition of Ca2+-entry blocker La3+ or SK&F 96365 inhibited Ca(i) oscillations, suggesting that Ca(i) oscillations in ras-transfected HaCaT keratinocytes were dependent on Ca2+ influx across the plasma membrane. amicloral 72-78 carbonic anhydrase 1 Homo sapiens 133-138 9309381-2 1997 IL6 is another cytokine important in the mechanisms of bone resorption and could be a target for the actions of SK&F 86002. amicloral 112-118 interleukin 6 Homo sapiens 0-3 9259410-4 1997 PC-6/SN2-5 cells were resistant to SN-38 (32-fold) and SK&F 104864 (topotecan; 14-fold), but barely resistant to CPT-11 (3-fold) and DX-8951f (2-fold). amicloral 55-61 proprotein convertase subtilisin/kexin type 5 Homo sapiens 0-4 9276129-11 1997 Pretreatment of cells with SK&F 96365 resulted in an inhibition of greater than 60% of the BK response. amicloral 27-33 kininogen 1 Canis lupus familiaris 95-97 9144511-3 1997 Using freshly elutriated human monocytes, we examined the effect on PGHS-2 expression of certain cytokine-suppressive anti-inflammatory drugs such as SK&F 86002. amicloral 150-156 prostaglandin-endoperoxide synthase 2 Homo sapiens 68-74 9144511-5 1997 SK&F 86002 dose-dependently inhibited this STZ-induced expression of PGHS-2 protein, which correlated with a decrease in prostaglandin E2 and thromboxane A2 production. amicloral 0-6 prostaglandin-endoperoxide synthase 2 Homo sapiens 73-79 9144511-6 1997 However, suppression of PGHS-2 expression is not the result of suppressed cytokine production, because SK&F 86002 suppressed PGHS-2 expression initiated by IL-1beta and TNF-alpha, in addition to other stimuli. amicloral 103-109 prostaglandin-endoperoxide synthase 2 Homo sapiens 24-30 9144511-6 1997 However, suppression of PGHS-2 expression is not the result of suppressed cytokine production, because SK&F 86002 suppressed PGHS-2 expression initiated by IL-1beta and TNF-alpha, in addition to other stimuli. amicloral 103-109 prostaglandin-endoperoxide synthase 2 Homo sapiens 129-135 9144511-6 1997 However, suppression of PGHS-2 expression is not the result of suppressed cytokine production, because SK&F 86002 suppressed PGHS-2 expression initiated by IL-1beta and TNF-alpha, in addition to other stimuli. amicloral 103-109 interleukin 1 beta Homo sapiens 160-168 9144511-6 1997 However, suppression of PGHS-2 expression is not the result of suppressed cytokine production, because SK&F 86002 suppressed PGHS-2 expression initiated by IL-1beta and TNF-alpha, in addition to other stimuli. amicloral 103-109 tumor necrosis factor Homo sapiens 173-182 9144511-9 1997 These results indicate a new and potentially important anti-inflammatory property of SK&F 86002, namely the specific suppression of PGHS-2 induction. amicloral 85-91 prostaglandin-endoperoxide synthase 2 Homo sapiens 136-142 9113376-17 1997 The ET-1-induced current was reversibly and completely inhibited by 30 microM SK&F 96365 or 500 microM Cd2+. amicloral 78-84 endothelin 1 Rattus norvegicus 4-8 9150842-5 1997 Results from clinical studies using receptor antagonists, such as LY-171883, SK&F-104353, ICI-204219, ONO-1078, MK-751, MK-0679, demonstrate beneficial effects, with improvement in symptoms and forced expiratory volume in one second (FEV1), and a reduction in the use of beta 2-adrenergic relief medication. amicloral 77-83 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 275-281 9335411-5 1997 Mefenamic acid and SK&F 96365 inhibited the ET-1-induced contraction with 50% inhibitory concentration (IC50) values of 10(-4) M and 2 x 10(-5) M, respectively, and abolished it at 10(-3) M and 10(-4) M. By contrast, nifedipine, mefenamic acid, or SK&F 96365 had little effect on the contraction by a high concentration of ET-1. amicloral 19-25 endothelin-1 Oryctolagus cuniculus 48-52 9335411-5 1997 Mefenamic acid and SK&F 96365 inhibited the ET-1-induced contraction with 50% inhibitory concentration (IC50) values of 10(-4) M and 2 x 10(-5) M, respectively, and abolished it at 10(-3) M and 10(-4) M. By contrast, nifedipine, mefenamic acid, or SK&F 96365 had little effect on the contraction by a high concentration of ET-1. amicloral 19-25 endothelin-1 Oryctolagus cuniculus 331-335 9335411-5 1997 Mefenamic acid and SK&F 96365 inhibited the ET-1-induced contraction with 50% inhibitory concentration (IC50) values of 10(-4) M and 2 x 10(-5) M, respectively, and abolished it at 10(-3) M and 10(-4) M. By contrast, nifedipine, mefenamic acid, or SK&F 96365 had little effect on the contraction by a high concentration of ET-1. amicloral 252-258 endothelin-1 Oryctolagus cuniculus 48-52 9298542-11 1997 The relaxant effects induced by SK&F 94120 and rolipram were inhibited by Rp-8-Br-cyclic GMPS with no significant effect of H-89. amicloral 32-38 guanine monophosphate synthase Rattus norvegicus 93-97 9309381-4 1997 Both indomethacin (5 x 10(-8)-5 x 10(-6) M) and SK&F 86002 (5 x 10(-7)-10(-5) M) markedly inhibited the IL6 release and totally inhibited resorption at all concentrations tested. amicloral 48-54 interleukin 6 Homo sapiens 108-111 9309381-6 1997 In human osteoblastic cells (SaOS2) both basal and TNF alpha-stimulated IL6 production were inhibited in a concentration-related manner by SK&F 86002 but not by indomethacin. amicloral 139-145 interleukin 6 Homo sapiens 72-75 9309381-7 1997 The effect of SK&F 86002 was greatest in 6 h cultures where relatively low levels of IL6 are produced and progressively less in 24 and 48 h cultures which produce higher levels of IL6. amicloral 14-20 interleukin 6 Homo sapiens 89-92 9309381-7 1997 The effect of SK&F 86002 was greatest in 6 h cultures where relatively low levels of IL6 are produced and progressively less in 24 and 48 h cultures which produce higher levels of IL6. amicloral 14-20 interleukin 6 Homo sapiens 184-187 9309381-9 1997 Therefore, SK&F 86002 may inhibit IL6 production in osteoblastic cells via a more direct mechanism, possibly involving inhibition of the p38 MAP kinase, the mechanism proposed for its inhibition of IL 1 beta and TNF alpha release. amicloral 11-17 interleukin 6 Homo sapiens 38-41 9309381-9 1997 Therefore, SK&F 86002 may inhibit IL6 production in osteoblastic cells via a more direct mechanism, possibly involving inhibition of the p38 MAP kinase, the mechanism proposed for its inhibition of IL 1 beta and TNF alpha release. amicloral 11-17 mitogen-activated protein kinase 14 Homo sapiens 141-144 9309381-9 1997 Therefore, SK&F 86002 may inhibit IL6 production in osteoblastic cells via a more direct mechanism, possibly involving inhibition of the p38 MAP kinase, the mechanism proposed for its inhibition of IL 1 beta and TNF alpha release. amicloral 11-17 interleukin 1 beta Homo sapiens 202-211 8946652-9 1996 SK&F 86002 blocked the LPS-induced increase in myeloperoxidase activity, indicating a reduction in pulmonary neutrophil infiltration, but had no effect on systemic leukopenia. amicloral 0-6 myeloperoxidase Sus scrofa 51-66 8985595-6 1996 Pretreatment with SK&F 96365 prevented thapsigargin from increasing [Ca2+]i, NO production and vWF secretion. amicloral 18-24 von Willebrand factor Homo sapiens 99-102 8946652-10 1996 Pretreatment with SK&F 86002 significantly attenuated LPS-induced increases in plasma thromboxane B2 and tumor necrosis factor-alpha. amicloral 18-24 tumor necrosis factor Sus scrofa 83-136 7632163-8 1995 The action of fenamates resembled that of the inhibitor of receptor-mediated calcium entry, SK&F 96365, especially when A23187, fMLP or PMA were used to stimulate the cells. amicloral 92-98 formyl peptide receptor 1 Homo sapiens 132-136 8773410-9 1996 This route of Ca2+ entry is also sensitive to blockade by SK&F 96365. amicloral 58-64 carbonic anhydrase 2 Canis lupus familiaris 14-17 8991541-2 1996 In this study, we describe the effects of SK&F108636 on highly enriched Lin-Sca1+ hematopoietic stem cells. amicloral 42-48 caspase 3 Mus musculus 80-84 8991541-5 1996 SK&F108636 significantly inhibited proliferation of high proliferative potential (HPP)-CFC in semisolid agar cultures stimulated by stem cell factor + interleukin 3 (IL-3) + IL-1, but had no effect in cultures stimulated with M-CSF + IL-3 + IL-1. amicloral 0-6 colony stimulating factor 1 (macrophage) Mus musculus 230-235 8991541-5 1996 SK&F108636 significantly inhibited proliferation of high proliferative potential (HPP)-CFC in semisolid agar cultures stimulated by stem cell factor + interleukin 3 (IL-3) + IL-1, but had no effect in cultures stimulated with M-CSF + IL-3 + IL-1. amicloral 0-6 interleukin 3 Mus musculus 170-174 8991541-5 1996 SK&F108636 significantly inhibited proliferation of high proliferative potential (HPP)-CFC in semisolid agar cultures stimulated by stem cell factor + interleukin 3 (IL-3) + IL-1, but had no effect in cultures stimulated with M-CSF + IL-3 + IL-1. amicloral 0-6 interleukin 1 complex Mus musculus 245-249 8991541-6 1996 SK&F108636 was shown to act directly on the stem cells since SK&F108636 inhibited proliferation of Lin-Sca1+ cells in single cell assays. amicloral 0-6 caspase 3 Mus musculus 111-115 8991541-6 1996 SK&F108636 was shown to act directly on the stem cells since SK&F108636 inhibited proliferation of Lin-Sca1+ cells in single cell assays. amicloral 65-71 caspase 3 Mus musculus 111-115 8991541-7 1996 Administration of SK&F108636 to lethally irradiated mice transplanted with 2000 Lin-Sca1+ cells significantly inhibited proliferation/differentiation of cells developing into colony forming units-spleen (CFU-S) (preCFU-S) and the reconstitution of HPP-CFC and GM-CFC. amicloral 18-24 caspase 3 Mus musculus 88-92 7503756-10 1995 These data indicate that the duration of action of SK&F 97574 is longer than that of the histamine H2 receptor antagonists such as cimetidine, but shorter than that of covalent (H+/K+)-inhibitors such as omeprazole. amicloral 51-57 histamine receptor H 2 Rattus norvegicus 93-114 8894140-7 1996 SK&F 96365, an inhibitor of receptor-operated Ca2+ entry, significantly inhibited the choline formation induced by FCS. amicloral 0-6 carbonic anhydrase 2 Mus musculus 50-53 8702797-5 1996 Of these two chemokines, only Gro-alpha induced an influx of calcium in neutrophils as judged by the sensitivity of the mobilization of calcium to the extracellular calcium chelator EGTA and to the nonselective divalent cation channel inhibitor SK&F 96365, as well as by manganese quenching experiments. amicloral 245-251 C-X-C motif chemokine ligand 1 Homo sapiens 30-39 8864528-4 1996 In lysates prepared from both subsets, SK&F 95654 (PDE3 inhibitor) and rolipram (PDE4 inhibitor) suppressed cyclic AMP hydrolysis indicating the presence of PDE3 and PDE4 isoenzymes in these cells. amicloral 39-45 phosphodiesterase 4A Homo sapiens 170-174 8864528-14 1996 Although inactive alone, SK&F 95654 potentiated the ability of rolipram to suppress PHA- and anti-CD3-induced T-cell proliferation, and PHA-induced IL-2 release. amicloral 25-31 interleukin 2 Homo sapiens 152-156 9812726-0 1996 SK&F 105494, a V2-vasopressin receptor antagonist, blocks oxytocin receptors in porcine myometrium. amicloral 0-6 oxytocin/neurophysin I prepropeptide Homo sapiens 62-70 9812726-1 1996 AIM: To study the effects of SK & F 105494 (SK & F), a V2-vasopressin receptor antagonist, on lypressin (Lyp)- and oxytocin (Oxy)-induced increases in myometrial contractility. amicloral 29-36 oxytocin/neurophysin I prepropeptide Homo sapiens 133-136 9812726-5 1996 SK & F 30-300 nmol.L-1 antagonized the contractile effects of Lyp and Oxy in a concentration-dependent manner. amicloral 0-7 oxytocin/neurophysin I prepropeptide Homo sapiens 74-77 9812726-6 1996 When the concentration-dependent inhibition of [3H] Oxy binding by SK & F was compared with Lyp and L-366948 [(cyclo-(L-Pro-D-2-naphthyl-Ala-L-lle-D-pipecolic acid-L-pipecolic acid-D-His)], a potent antagonist specific for Oxy receptors, the Ki values for SK & F, Lyp, and L-366948 were 1.73 +/- 0.32, 14.36 +/- 1.73, and 1.79 +/- 0.35 nmol.L-1, respectively. amicloral 67-74 oxytocin/neurophysin I prepropeptide Homo sapiens 52-55 9812726-7 1996 CONCLUSION: SK & F has a potent Oxy receptor blocking activity in addition to its known V2-receptor blocking activity. amicloral 12-19 oxytocin/neurophysin I prepropeptide Homo sapiens 36-39 7498963-6 1995 Depletion of extracellular Ca2+ or addition of Ca2+ channel blockers (nifedipine, verapamil, SK&F 96365) attenuated ET-1-mediated 6-keto-PGF1 alpha synthesis, while a Ca2+ channel agonist, S(-)-Bay K 8644, potentiated this effect of ET-1. amicloral 93-99 endothelin 1 Rattus norvegicus 120-124 7498963-6 1995 Depletion of extracellular Ca2+ or addition of Ca2+ channel blockers (nifedipine, verapamil, SK&F 96365) attenuated ET-1-mediated 6-keto-PGF1 alpha synthesis, while a Ca2+ channel agonist, S(-)-Bay K 8644, potentiated this effect of ET-1. amicloral 93-99 endothelin 1 Rattus norvegicus 237-241 7883027-1 1994 When acetylcholinesterase was inhibited by neostigmine, SK&F 96365 (1-(beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl)-1H-imidazole hydrochloride) at 10 microM caused no effect on the amplitude of single endplate potentials (e.p.p.s) but shortened the decay time in mouse phrenic nerve-diaphragm preparations. amicloral 56-62 acetylcholinesterase Mus musculus 5-25 7539326-4 1995 Pretreatment with the PDE IV inhibitors rolipram or Ro 20-1724 or the nonselective PDE inhibitor theophylline 1 h before intratracheal injection of IL-5 significantly reduced the number of eosinophils in the BAL fluid at 48 h. In contrast, the selective PDE III inhibitors milrinone and SK&F 94-836 and the PDE I/V inhibitor zaprinast did not inhibit the airway eosinophil infiltration induced by IL-5. amicloral 287-293 interleukin 5 Homo sapiens 148-152 7773223-4 1995 Both the marrow GM-CFC progenitor cell population and Mac-1 positive cells in blood were shown to recover faster in recipients of SK&F107647 treated donors. amicloral 130-136 integrin alpha M Mus musculus 54-59 7583362-3 1995 Levels of TNF protein were lowered by SK&F 86002 under conditions where TNF mRNA accumulation was unaffected, suggesting a post-transcriptional action. amicloral 38-44 tumor necrosis factor Homo sapiens 10-13 7583362-3 1995 Levels of TNF protein were lowered by SK&F 86002 under conditions where TNF mRNA accumulation was unaffected, suggesting a post-transcriptional action. amicloral 38-44 tumor necrosis factor Homo sapiens 76-79 7583362-5 1995 The kinetics of SK&F 86002 inhibition of TNF protein synthesis coincided with those of anisomycin, not with actinomycin, suggesting an effect of SK&F 86002 on TNF mRNA translation. amicloral 16-22 tumor necrosis factor Homo sapiens 45-48 7583362-5 1995 The kinetics of SK&F 86002 inhibition of TNF protein synthesis coincided with those of anisomycin, not with actinomycin, suggesting an effect of SK&F 86002 on TNF mRNA translation. amicloral 149-155 tumor necrosis factor Homo sapiens 167-170 7583362-8 1995 Treatment with lipopolysaccharide plus SK&F 86002 led to a marked accumulation of TNF mRNA in the 43S complex-containing fractions and a concomitant reduction of polysome-associated TNF message. amicloral 39-45 tumor necrosis factor Homo sapiens 86-89 7583362-8 1995 Treatment with lipopolysaccharide plus SK&F 86002 led to a marked accumulation of TNF mRNA in the 43S complex-containing fractions and a concomitant reduction of polysome-associated TNF message. amicloral 39-45 tumor necrosis factor Homo sapiens 186-189 7947609-5 1994 Autacoids released by histamine-stimulated endothelial cells caused the phosphorylation of rap1B and VASP in platelets, which was only partly inhibited by either indomethacin or NG-monomethyl-L-arginine but was almost completely suppressed by SK&F 96365. amicloral 243-249 RAP1B, member of RAS oncogene family Homo sapiens 91-96 7947609-7 1994 The results demonstrate that blockade of receptor-mediated calcium entry by SK&F 96365 markedly reduced the release of biologically active prostacyclin and EDRF from endothelial cells. amicloral 76-82 alpha hemoglobin stabilizing protein Homo sapiens 160-164 7858878-0 1994 Inhibition by SK&F 96365 of Ca2+ current, IL-2 production and activation in T lymphocytes. amicloral 14-20 interleukin 2 Homo sapiens 46-50 7858878-9 1994 The ability of SK&F 96365 to inhibit IL-2 synthesis and cell proliferation suggests that a new class of related Ca2+ channel blockers can be developed as immunosuppressive agents. amicloral 15-21 interleukin 2 Homo sapiens 41-45 7521569-2 1994 Mediators released from mast cells in immune animals challenged with beta-lactoglobulin evoked an increase in short-circuit current that was reduced by SK&F 102922, a peptidoleukotriene antagonist. amicloral 152-158 beta-lactoglobulin Bos taurus 69-87 7705461-7 1994 Both endothelin-1- and endothelin-3-induced 45Ca2+ uptake were inhibited by receptor operated Ca2+ channel blocker SK&F 96365, whereas they were insensitive to dihydropyridine derivatives nifedipine and nitrendipine. amicloral 115-121 endothelin 1 Rattus norvegicus 5-17 7705461-7 1994 Both endothelin-1- and endothelin-3-induced 45Ca2+ uptake were inhibited by receptor operated Ca2+ channel blocker SK&F 96365, whereas they were insensitive to dihydropyridine derivatives nifedipine and nitrendipine. amicloral 115-121 endothelin 3 Rattus norvegicus 23-35 7705461-8 1994 The release of arachidonic acid from rat brain endothelial cells observed in response to endothelin-1 was inhibited by ryanodine or SK&F 96365, implicating participation of both intra- and extra- cellular components of Ca2+ signaling in activating endothelial secretion of vasoactive substances. amicloral 132-138 endothelin 1 Rattus norvegicus 89-101 7980964-3 1994 In the present study, SK&F 86002 inhibited fetal rat long bone (FRLB) resorption induced by parathyroid hormone (PTH), 1,25-dihydroxy-vitamin D3, tumor necrosis factor alpha, and Escherichia coli lipopolysaccharide in a dose-dependent (IC50 of 0.5-1 microM) and reversible manner. amicloral 22-28 parathyroid hormone Rattus norvegicus 96-115 7980964-3 1994 In the present study, SK&F 86002 inhibited fetal rat long bone (FRLB) resorption induced by parathyroid hormone (PTH), 1,25-dihydroxy-vitamin D3, tumor necrosis factor alpha, and Escherichia coli lipopolysaccharide in a dose-dependent (IC50 of 0.5-1 microM) and reversible manner. amicloral 22-28 tumor necrosis factor Rattus norvegicus 150-177 8063786-11 1994 As an independent verification of specificity, a marked reduction in MMP-2 gelatinase activity by zymogram was shown after treatment of A2058 cells with SK&F 96365, an unrelated inhibitor of receptor-operated calcium influx. amicloral 153-159 matrix metallopeptidase 2 Homo sapiens 69-74 8057281-3 1994 We have shown that known GABA uptake inhibitors such as SK&F 89976-A, CI-966, and Tiagabine exhibit high affinity and selectivity for GAT-1. amicloral 56-62 solute carrier family 6 member 1 Homo sapiens 138-143 8072241-4 1994 In a second series of experiments, a selective 5-lipoxygenase (5-LO) inhibitor, SK&F 107649, was used to investigate the involvement of 5-LO products in the pathophysiology of anti-GBM antibody-induced glomerulonephritis. amicloral 80-86 arachidonate 5-lipoxygenase Rattus norvegicus 47-61 7851497-0 1994 Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. amicloral 11-17 solute carrier family 6 member 1 Homo sapiens 95-100 7965744-4 1994 AII-stimulated endothelin (ET)-1 gene expression was antagonized by SK&F 108566 (50% at 1 microM), but not by selective AT2 receptor antagonists. amicloral 68-74 angiotensinogen Rattus norvegicus 0-3 7965744-5 1994 Similarly, AII stimulated the release of immunoreactive ET (irET) from cultured VSM cells that was antagonized by 1 microM SK&F 108566 (72%) and DuP 753 (66%), but not by AT2 receptor antagonists. amicloral 123-129 angiotensinogen Rattus norvegicus 11-14 7965744-7 1994 AII (1-100 nM) markedly (6- to 10-fold) stimulated mitogen-activated protein kinase, an enzyme believed to be involved in the pathway for cell proliferation, and this stimulation was blocked (50-75%) by SK&F 108566 (1 nM-1 microM). amicloral 203-209 angiotensinogen Rattus norvegicus 0-3 7980964-2 1994 SK&F 86002 [5-(4-pyridyl)-6(4-fluorophenyl)-2,3-dihydroimidazo(2,1-b) thiazole], a potent cytokine-suppressive anti-inflammatory agent, has been shown to inhibit cyclooxygenase (CO) and 5-lipoxygenase (LO) activity and to inhibit the production of cytokines both in vitro and in vivo. amicloral 0-6 arachidonate 5-lipoxygenase Rattus norvegicus 190-204 8038206-2 1994 Gd3+ and SK&F 96365 inhibited Ca2+ and Mn2+ inflow stimulated by vasopressin, angiotensin II or phenylephrine. amicloral 9-15 arginine vasopressin Homo sapiens 69-80 8038206-2 1994 Gd3+ and SK&F 96365 inhibited Ca2+ and Mn2+ inflow stimulated by vasopressin, angiotensin II or phenylephrine. amicloral 9-15 angiotensinogen Homo sapiens 82-96 8038206-3 1994 The concentrations of Gd3+ and SK&F 96365 which gave half-maximal inhibition of vasopressin-stimulated Ca2+ inflow were 2 x 10(-7) M and 16 x 10(-6) M, respectively. amicloral 31-37 arginine vasopressin Homo sapiens 84-95 7974388-5 1994 SK&F 106760 inhibited biotinylated fibrinogen binding to purified human GPIIb/IIIa immobilized on plastic microtitre plates with a Ki of 477 +/- 57 pM. amicloral 0-6 fibrinogen beta chain Homo sapiens 39-49 7974388-5 1994 SK&F 106760 inhibited biotinylated fibrinogen binding to purified human GPIIb/IIIa immobilized on plastic microtitre plates with a Ki of 477 +/- 57 pM. amicloral 0-6 integrin subunit alpha 2b Homo sapiens 76-81 7974388-9 1994 SK&F 106760 produced insurmountable inhibition of adenosine diphosphate-induced platelet aggregation in the presence of constant fibrinogen concentrations, but produced competitive inhibition of the concentration-response curve to fibrinogen in adenosine diphosphate-activated platelets with a Kb of 8.0 +/- 1.0 nM. amicloral 0-6 fibrinogen beta chain Homo sapiens 235-245 7915128-1 1994 SK&F 87516 is a potent DA1 receptor agonist with demonstrated renal vasodilator activity. amicloral 0-6 RT1 class II, locus Da Rattus norvegicus 27-30 8183249-8 1994 SK&F104856 was found to be 6-fold more potent at the alpha 1a/d receptor subtype than at alpha 1b- or alpha 1c-adrenergic receptors. amicloral 0-6 calcium voltage-gated channel subunit alpha1 A Homo sapiens 57-65 8012704-10 1994 Concentrations of SK&F 103829 causing greater than threshold constrictions enhanced vasoconstrictor responses of sympathetic nerve stimulation, noradrenaline, angiotensin II, methoxamine and alpha, beta-methylene ATP in the mesenteric arterial bed. amicloral 18-24 angiotensinogen Rattus norvegicus 163-200 8012704-13 1994 Ketanserin prevented both the constrictor effect of SK&F 103829 and the SK&F 103829-evoked potentiation of the responses to noradrenaline and angiotensin II in the mesenteric arterial bed. amicloral 76-82 angiotensinogen Rattus norvegicus 150-164 7915128-2 1994 SK&F 87516 is the 6-fluoro analog of another DA1 agonist/renal vasodilator agent, fenoldopam. amicloral 0-6 RT1 class II, locus Da Rattus norvegicus 49-52 8149896-0 1994 Disposition of growth hormone-releasing peptide (SK&F 110679) in rat and dog following intravenous or subcutaneous administration. amicloral 49-55 ghrelin and obestatin prepropeptide Rattus norvegicus 15-47 8035652-6 1994 The secondary phase of aggregation produced by human laminin in "responsive" individuals was abolished by aspirin, SQ 29,548, a selective thromboxane antagonist, and SK&F 106760, an RGD-derived platelet fibrinogen receptor (GPIIb/IIIa) antagonist. amicloral 166-172 integrin subunit alpha 2b Homo sapiens 228-233 8264564-7 1993 The idea that CYP2B1 was involved in the one-electron reduction of ADR in PB microsomes and in reconstituted systems of purified CYP2B1 and purified NADPH-CYP reductase (RED) under anaerobic conditions could be concluded from inhibition studies using SK&F 525-A and antibodies (KO1) against CYP2B enzymes. amicloral 251-257 cytochrome P450, family 2, subfamily b, polypeptide 1 Rattus norvegicus 14-20 7507780-5 1993 The combination of the peptidoleukotriene receptor antagonist, SK&F 104353 (10 microM) and the H1-histamine receptor antagonist, mepyramine (10 microM), which abolishes antigen-induced contraction in guinea-pig trachea, was without effect on ET-1 concentration-response curves. amicloral 63-69 endothelin-1 Cavia porcellus 246-250 8516808-6 1993 SK&F 105685 therapy diminished the immunohistological features of acute rejection, with the cellular infiltrate suppressed and the induction of IL-2/transferrin receptors, and elaboration of IL-2/IFN-gamma essentially abolished, as compared with the grafts in untreated hosts. amicloral 0-6 interleukin 2 Rattus norvegicus 148-152 8402579-1 1993 SK&F 96365, a reported receptor-operated Ca2+ channel blocker, inhibited the growth of U-373 MG human astrocytoma and SK-N-MC human neuroblastoma cell lines in a dose-dependent manner. amicloral 0-6 carbonic anhydrase 2 Homo sapiens 45-48 8402579-4 1993 These results suggest that SK&F 96365 is a potent inhibitor of brain tumor cell growth and that its effect may be mediated by the inhibition of agonist-induced intracellular Ca2+ mobilization. amicloral 27-33 carbonic anhydrase 2 Homo sapiens 178-181 8516808-6 1993 SK&F 105685 therapy diminished the immunohistological features of acute rejection, with the cellular infiltrate suppressed and the induction of IL-2/transferrin receptors, and elaboration of IL-2/IFN-gamma essentially abolished, as compared with the grafts in untreated hosts. amicloral 0-6 interleukin 2 Rattus norvegicus 195-199 8516808-6 1993 SK&F 105685 therapy diminished the immunohistological features of acute rejection, with the cellular infiltrate suppressed and the induction of IL-2/transferrin receptors, and elaboration of IL-2/IFN-gamma essentially abolished, as compared with the grafts in untreated hosts. amicloral 0-6 interferon gamma Rattus norvegicus 200-209 8435086-17 1993 Finally, use of fura-2 and SK&F 96365 to manipulate the fMLP-stimulated rise in [Ca2+]i showed that when fMLP was able to evoke its normal rise in [Ca2+]i (to a peak of 700-900 nM), O2-. amicloral 27-33 formyl peptide receptor 1 Homo sapiens 60-64 8097163-2 1993 This compound induced the same intense grooming behaviour identified previously as a characteristic response to typical dopamine D1 receptor agonists such as SK&F 77434 that stimulate adenylyl cyclase; it also induced vacuous chewing. amicloral 158-164 dopamine receptor D1 Homo sapiens 120-140 8435086-17 1993 Finally, use of fura-2 and SK&F 96365 to manipulate the fMLP-stimulated rise in [Ca2+]i showed that when fMLP was able to evoke its normal rise in [Ca2+]i (to a peak of 700-900 nM), O2-. amicloral 27-33 formyl peptide receptor 1 Homo sapiens 109-113 7682199-0 1993 Inhibition of CD44, CD45 and LFA-3 mediated cytokine release from human monocytes by SK&F 86002 and pentoxifylline. amicloral 85-91 CD44 molecule (Indian blood group) Homo sapiens 14-18 7682199-0 1993 Inhibition of CD44, CD45 and LFA-3 mediated cytokine release from human monocytes by SK&F 86002 and pentoxifylline. amicloral 85-91 protein tyrosine phosphatase receptor type C Homo sapiens 20-24 7682199-0 1993 Inhibition of CD44, CD45 and LFA-3 mediated cytokine release from human monocytes by SK&F 86002 and pentoxifylline. amicloral 85-91 CD58 molecule Homo sapiens 29-34 7682199-1 1993 Compounds from two distinct pharmacological classes namely, SK&F 86002 and pentoxifylline, were examined for their effects on TNF alpha and IL-1 beta release by human monocytes stimulated with LPS or monoclonal antibodies to three cell surface glycoproteins, CD44, CD45 and LFA-3 (LFA-3 is also known as CD58). amicloral 60-66 tumor necrosis factor Homo sapiens 130-139 7682199-1 1993 Compounds from two distinct pharmacological classes namely, SK&F 86002 and pentoxifylline, were examined for their effects on TNF alpha and IL-1 beta release by human monocytes stimulated with LPS or monoclonal antibodies to three cell surface glycoproteins, CD44, CD45 and LFA-3 (LFA-3 is also known as CD58). amicloral 60-66 interleukin 1 beta Homo sapiens 144-153 7682199-2 1993 SK&F 86002, an inhibitor of 5-LO and CO in arachidonic acid metabolism, inhibited LPS-induced release of TNF alpha and IL-1 beta with an IC50 of 1 microM. amicloral 0-6 tumor necrosis factor Homo sapiens 109-118 7682199-2 1993 SK&F 86002, an inhibitor of 5-LO and CO in arachidonic acid metabolism, inhibited LPS-induced release of TNF alpha and IL-1 beta with an IC50 of 1 microM. amicloral 0-6 interleukin 1 beta Homo sapiens 123-132 7682199-6 1993 These results suggest that (a) LPS induced cytokine release shares a common step with the physiologically relevant stimuli (involving cross-linking of cell surface receptors), and that this pathway is sensitive to inhibition by SK&F 86002 and, (b) SK&F 86002 is more potent than pentoxifylline in inhibiting TNF alpha and IL-1 beta release induced by both stimuli. amicloral 228-234 tumor necrosis factor Homo sapiens 316-325 7682199-6 1993 These results suggest that (a) LPS induced cytokine release shares a common step with the physiologically relevant stimuli (involving cross-linking of cell surface receptors), and that this pathway is sensitive to inhibition by SK&F 86002 and, (b) SK&F 86002 is more potent than pentoxifylline in inhibiting TNF alpha and IL-1 beta release induced by both stimuli. amicloral 228-234 interleukin 1 beta Homo sapiens 330-339 7682199-6 1993 These results suggest that (a) LPS induced cytokine release shares a common step with the physiologically relevant stimuli (involving cross-linking of cell surface receptors), and that this pathway is sensitive to inhibition by SK&F 86002 and, (b) SK&F 86002 is more potent than pentoxifylline in inhibiting TNF alpha and IL-1 beta release induced by both stimuli. amicloral 252-258 tumor necrosis factor Homo sapiens 316-325 7682199-6 1993 These results suggest that (a) LPS induced cytokine release shares a common step with the physiologically relevant stimuli (involving cross-linking of cell surface receptors), and that this pathway is sensitive to inhibition by SK&F 86002 and, (b) SK&F 86002 is more potent than pentoxifylline in inhibiting TNF alpha and IL-1 beta release induced by both stimuli. amicloral 252-258 interleukin 1 beta Homo sapiens 330-339 8273586-2 1993 In vitro, SK&F 86002 inhibited LPS stimulated TNF-alpha production by the RAW 264.7 cell line and by oil elicited peritoneal macrophages with an IC50 of 5 microM. amicloral 10-16 tumor necrosis factor Mus musculus 50-59 8273586-5 1993 Following oral administration, SK&F 86002 and its analogs reduced serum TNF-alpha levels by > 80% and afforded 100% protection from lethality. amicloral 31-37 tumor necrosis factor Mus musculus 76-85 8273589-1 1993 The mechanism by which SK&F 86002 and other pyridinyl imidazoles inhibit the production of IL-1 and TNF from LPS-stimulated human monocytes was examined. amicloral 23-29 interleukin 1 beta Homo sapiens 95-99 8273589-1 1993 The mechanism by which SK&F 86002 and other pyridinyl imidazoles inhibit the production of IL-1 and TNF from LPS-stimulated human monocytes was examined. amicloral 23-29 tumor necrosis factor Homo sapiens 104-107 8273589-2 1993 Inhibition of IL-1 and TNF production was found to depend on the time of addition of SK&F 86002, with diminishing effect when added more than 2 h after LPS stimulation. amicloral 85-91 interleukin 1 beta Homo sapiens 14-26 8273589-3 1993 Analysis of Western blots confirmed that both intracellular IL-1 beta and extracellular TNF were significantly reduced in response to SK&F 86002, but these reductions were not paralleled by changes in IL-1 and TNF mRNA. amicloral 134-140 interleukin 1 beta Homo sapiens 60-69 8273589-3 1993 Analysis of Western blots confirmed that both intracellular IL-1 beta and extracellular TNF were significantly reduced in response to SK&F 86002, but these reductions were not paralleled by changes in IL-1 and TNF mRNA. amicloral 134-140 tumor necrosis factor Homo sapiens 88-91 8273589-3 1993 Analysis of Western blots confirmed that both intracellular IL-1 beta and extracellular TNF were significantly reduced in response to SK&F 86002, but these reductions were not paralleled by changes in IL-1 and TNF mRNA. amicloral 134-140 interleukin 1 beta Homo sapiens 60-64 8273589-4 1993 35S methionine pulse and pulse-chase studies on IL-1 biosynthesis suggest that significant inhibition by SK&F 86002 and related compounds occurs at the translational level. amicloral 105-111 interleukin 1 beta Homo sapiens 48-52 1281979-10 1992 SK&F 96365 inhibited fMLP- and ATP-stimulated currents with a half-maximal effect at about 3 microM. amicloral 0-6 formyl peptide receptor 1 Homo sapiens 25-29 8275798-4 1993 In contrast, SK&F 96365, which is an inhibitor of receptor-operated calcium channel, blocked the PAF-elicited Ca(2+)-response dose-dependently. amicloral 13-19 patchy fur Mus musculus 101-104 8013267-7 1993 The CSAID (exemplified by SK&F 86002, SK&F 105809 and SK&F 104351), strongly inhibited TNF alpha production in this model system (ED50s of 32, 48, and 34 mg/kg p.o., respectively). amicloral 26-32 tumor necrosis factor Mus musculus 99-108 1281979-18 1992 SK&F 96365 inhibited fMLP-induced beta-glucuronidase release and O2- production in the presence of both Ca2+ and Na+, and in the presence of Ca2+ or Na+ alone. amicloral 0-6 formyl peptide receptor 1 Homo sapiens 25-29 1281979-18 1992 SK&F 96365 inhibited fMLP-induced beta-glucuronidase release and O2- production in the presence of both Ca2+ and Na+, and in the presence of Ca2+ or Na+ alone. amicloral 0-6 glucuronidase beta Homo sapiens 38-56 1326953-4 1992 In contrast, SK&F 96365 a purported receptor operated calcium channel (ROCC) inhibitor, and its parent compound SC 32849, attenuated LTB4 induced [Ca++]i. amicloral 13-19 prostaglandin reductase 1 Cavia porcellus 137-141 1422592-2 1992 SK&F 95654 inhibited the guanosine 3":5"-cyclic monophosphate (cyclic GMP)-inhibited phosphodiesterase (cGI-PDE) with an IC50 value of 0.7 microM. amicloral 0-6 phosphodiesterase 3A Homo sapiens 108-115 1422592-4 1992 The R-enantiomer of SK&F 95654 (IC50 = 0.35 microM) was a more potent inhibitor of cGI-PDE than was the S-enantiomer (IC50 = 5.3 microM). amicloral 20-26 phosphodiesterase 3A Homo sapiens 87-94 1422592-12 1992 SK&F 95654 caused a potent inhibition of U46619-induced aggregation in both a human washed platelet suspension (WPS) (IC50 = 70 nM) and in human platelet-rich plasma (PRP) (IC50 = 60 nM), indicating that the compound shows negligible plasma binding. amicloral 0-6 proline rich protein 2-like 1 Rattus norvegicus 171-174 1422592-15 1992 The similarity of this ratio to that obtained on the cGI-PDE suggests that SK&F 95654 inhibits platelet aggregation via its effects on cGI-PDE. amicloral 75-81 phosphodiesterase 3A Homo sapiens 53-60 1422592-15 1992 The similarity of this ratio to that obtained on the cGI-PDE suggests that SK&F 95654 inhibits platelet aggregation via its effects on cGI-PDE. amicloral 75-81 phosphodiesterase 3A Homo sapiens 139-146 1422592-18 1992 Collagen-induced aggregation of rat PRP was also inhibited by SK&F 95654 (ICso = 65 nM). amicloral 62-68 proline rich protein 2-like 1 Rattus norvegicus 36-39 1330154-14 1992 Preincubation of the cells with EGTA, verapamil, or the receptor-operated calcium channel antagonist, SK&F 96365, reduced vasopressin-stimulated [3H]-PtdBuOH accumulation by approximately 30%, suggesting that influx of calcium has a significant role to play in the regulation of vasopressinstimulated PLD activity. amicloral 102-108 arginine vasopressin Homo sapiens 126-137 1330154-14 1992 Preincubation of the cells with EGTA, verapamil, or the receptor-operated calcium channel antagonist, SK&F 96365, reduced vasopressin-stimulated [3H]-PtdBuOH accumulation by approximately 30%, suggesting that influx of calcium has a significant role to play in the regulation of vasopressinstimulated PLD activity. amicloral 102-108 glycosylphosphatidylinositol specific phospholipase D1 Homo sapiens 305-308 1510680-5 1992 Thus biosynthesis and release of EDRF from human umbilical vein endothelial cells significantly depend on agonist-induced Ca2+ entry involving receptor-operated Ca(2+)-permeable channels which can be blocked by SK&F 96365. amicloral 211-217 alpha hemoglobin stabilizing protein Homo sapiens 33-37 1446388-3 1992 We report here that in vitro SK&F 105561 also blocks the production of tumor necrosis factor (TNF) from human monocytes (IC50 0.8-3 microM). amicloral 29-35 tumor necrosis factor Homo sapiens 75-96 1446388-3 1992 We report here that in vitro SK&F 105561 also blocks the production of tumor necrosis factor (TNF) from human monocytes (IC50 0.8-3 microM). amicloral 29-35 tumor necrosis factor Homo sapiens 98-101 1355296-1 1992 The effects of dynorphin A(1-13) on the D1 dopamine agonist SK&F 38393- and the D2 dopamine agonist RU 24213-induced behavioral alterations in the mouse were determined by using multidimensional behavioral analyses based upon a capacitance system. amicloral 60-66 prodynorphin Mus musculus 15-31 1356721-10 1992 These data indicate that M3a and M3b are nonglycosidic isomers of M2 that were formed by a nonenzymic reaction involving migration of the aglycone (SK&F 102922) from C-1 to C-2, C-3, or C-4 of glucuronic acid. amicloral 148-154 complement C2 Cavia porcellus 170-185 1635591-2 1992 SK&F 108566 produced dose-dependent decreases in blood pressure in renin-dependent hypertensive rats. amicloral 0-6 renin Rattus norvegicus 71-76 1348448-0 1992 Effect of P-glycoprotein expression on the accumulation and cytotoxicity of topotecan (SK&F 104864), a new camptothecin analogue. amicloral 87-93 ATP binding cassette subfamily B member 1 Homo sapiens 10-24 1591653-1 1992 The purpose of this study was to determine if a structurally novel dual inhibitor of arachidonic acid metabolism, SK & F 86002, would inhibit the endotoxin-induced production of tumor necrosis factor (TNF) activity by equine peritoneal macrophages. amicloral 114-121 tumor necrosis factor Equus caballus 182-203 1591653-1 1992 The purpose of this study was to determine if a structurally novel dual inhibitor of arachidonic acid metabolism, SK & F 86002, would inhibit the endotoxin-induced production of tumor necrosis factor (TNF) activity by equine peritoneal macrophages. amicloral 114-121 tumor necrosis factor Equus caballus 205-208 1591653-7 1992 Coincubation of macrophages with SK & F 86002 significantly decreased the subsequent supernatant TNF activity. amicloral 33-40 tumor necrosis factor Equus caballus 101-104 1591653-8 1992 Concentrations of SK & F 86002 from 10(-7) to 10(-4) molar effectively reduced TNF production when added to macrophages 0 and 0.5 h prior to endotoxin. amicloral 18-25 tumor necrosis factor Equus caballus 83-86 1591653-9 1992 After 2 h of preincubation, SK & F 86002 significantly reduced supernatant TNF activity at 10(-5) and 10(-4) M concentrations. amicloral 28-35 tumor necrosis factor Equus caballus 79-82 1560388-2 1992 We therefore investigated the effect of inhibition of the renin-angiotensin system by SK&F 108566, a novel, nonpeptide angiotensin II (AII) receptor antagonist, or by enalapril, an angiotensin converting enzyme inhibitor, on glycine-induced hyperfiltration. amicloral 86-92 renin Rattus norvegicus 58-63 1312215-13 1992 SK&F 96365 at 30 microM inhibited MTX-induced insulin release by 75%, whereas nifedipine, even at 30 microM, inhibited release by only 10%. amicloral 0-6 insulin Homo sapiens 50-57 2050194-6 1991 PCP, (+)-SK&F 10047 and (+/-)-pentazocine probably enhance neurogenic contractions in rat vas deferens primarily by inhibition of the neuronal uptake of noradrenaline. amicloral 5-15 arginine vasopressin Rattus norvegicus 94-97 1683559-2 1991 Ropinirole, SK&F 101468 has been characterized preclinically as a specific dopamine D2-receptor agonist. amicloral 12-18 dopamine receptor D2 Homo sapiens 79-99 1907824-0 1991 Pharmacology of the pyrroloimidazole, SK&F 105809--I. Inhibition of inflammatory cytokine production and of 5-lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. amicloral 38-44 arachidonate 5-lipoxygenase Homo sapiens 112-126 1907825-8 1991 The impact of inhibition of both 5-lipoxygenase (5-LO) and CO was seen with platelet-activating factor-induced vascular permeability which was inhibited markedly by SK&F 105809. amicloral 165-171 arachidonate 5-lipoxygenase Mus musculus 33-47 1292522-5 1992 However, SK&F 95587 reduced mesenteric vasoconstrictor responses to PGD2. amicloral 9-15 prostaglandin D2 synthase Homo sapiens 72-76 1292522-6 1992 Results of the present study indicate that SK&F 95587 blocks TX-receptor-mediated responses in the hindquarters circulation of the cat in a competitive and selective manner and reduces mesenteric vascular responses to the TXA2 mimics, as well as PGD2. amicloral 43-49 prostaglandin D2 synthase Homo sapiens 250-254 1309870-0 1992 Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&F 108566. amicloral 87-93 angiotensinogen Rattus norvegicus 51-65 1309870-9 1992 administration of SK&F 108566 (0.01-0.3 mg/kg) produced dose-dependent parallel shifts in the AII pressor dose-response curve. amicloral 18-24 angiotensinogen Rattus norvegicus 98-101 1309870-10 1992 Administration of SK&F 108566 (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). amicloral 18-24 angiotensinogen Rattus norvegicus 181-184 1309870-13 1992 The data demonstrate that SK&F 108566 is a potent, highly selective, competitive nonpeptide AII antagonist. amicloral 26-32 angiotensinogen Rattus norvegicus 96-99 1684820-6 1991 Administration of the vasopressin receptor antagonist, SK&F 105494, to either dogs or cynomolgus monkeys demonstrated that antagonism of the vasopressin V2 receptor could result in a brisk water diuresis in both species. amicloral 55-61 arginine vasopressin Rattus norvegicus 22-33 1684820-6 1991 Administration of the vasopressin receptor antagonist, SK&F 105494, to either dogs or cynomolgus monkeys demonstrated that antagonism of the vasopressin V2 receptor could result in a brisk water diuresis in both species. amicloral 55-61 arginine vasopressin Rattus norvegicus 145-156 2059205-0 1991 SK&F 96365, a receptor-mediated calcium entry inhibitor, inhibits calcium responses to endothelin-1 in NG108-15 cells. amicloral 0-6 endothelin 1 Mus musculus 91-103 2059205-2 1991 Since SK&F 96365 has recently been reported to inhibit receptor-mediated Ca2+ entry in other systems, we examined its effect on intracellular Ca2+ responses to endothelin-1, measured with the fluorescent Ca2+ indicator fura-2, in NG108-15 cells. amicloral 6-12 endothelin 1 Mus musculus 164-176 2263673-1 1990 The acute and chronic effects of a potent and selective dopamine beta-hydroxylase inhibitor, SK&F 102698 [1-(3,5-difluorobenzyl)imidazole-2-thiol], on systemic hemodynamic variables were assessed in chronically instrumented spontaneously hypertensive and normotensive Wistar rats. amicloral 93-99 dopamine beta-hydroxylase Rattus norvegicus 56-81 1663380-7 1991 In pigs pretreated with SK & F104353 the MAP and RABF were transiently improved (P less than 0.05), and the decrease in arterial PO2 was delayed. amicloral 24-31 PO2 Sus scrofa 133-136 1775514-0 1991 Effect of the dopamine beta-hydroxylase inhibitor, SK&F 102698, on blood pressure in the 1-kidney, 1-clip hypertensive dog. amicloral 51-57 dopamine beta-hydroxylase Canis lupus familiaris 14-39 1775514-1 1991 The acute and chronic effects of a potent selective dopamine beta-hydroxylase inhibitor, SK&F 102698, were assessed in chronically instrumented 1-kidney, 1-clip Goldblatt hypertensive dogs. amicloral 89-95 dopamine beta-hydroxylase Canis lupus familiaris 52-77 1663268-1 1991 This study characterized the induction of the rat hepatic cytochrome P-450-dependent mixed function oxidase system by SK&F 86002 [6-(4"-fluorophenyl)-5-(4"-pyridyl)-2,3-dihydroimidazo-(2,1-b)thia zole], an inhibitor of both the cyclooxygenase and 5-lipoxygenase pathways of arachidonic acid metabolism. amicloral 118-124 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 58-74 1663268-1 1991 This study characterized the induction of the rat hepatic cytochrome P-450-dependent mixed function oxidase system by SK&F 86002 [6-(4"-fluorophenyl)-5-(4"-pyridyl)-2,3-dihydroimidazo-(2,1-b)thia zole], an inhibitor of both the cyclooxygenase and 5-lipoxygenase pathways of arachidonic acid metabolism. amicloral 118-124 arachidonate 5-lipoxygenase Rattus norvegicus 251-265 2081508-8 1990 Pretreatment with an aerosol of the specific LTD4 receptor antagonist SK&F 104353-Z2 produced a dose-dependent inhibition of the changes in both the airway resistance and GFV. amicloral 70-76 cysteinyl leukotriene receptor 1 Cavia porcellus 45-58 2173565-5 1990 producing 50% inhibition) for inhibition of RMCE by SK&F 96365 in platelets stimulated with ADP or thrombin was 8.5 microM or 11.7 microM respectively; these concentrations of SK&F 96365 did not affect internal Ca2+ release. amicloral 52-58 prothrombin Oryctolagus cuniculus 103-111 1982058-1 1990 Fenoldopam (SK&F 82526) is a potent and selective dopamine DA-1 agonist with demonstrated renal vasodilator and antihypertensive activities in experimental animals and humans. amicloral 12-18 immunoglobulin heavy diversity 4-11 (non-functional) Homo sapiens 63-67 1982058-6 1990 The renal and systemic vasodilator properties of SK&F R-82526 are antagonized in a competitive fashion by the DA-1 antagonist, SK&F R-83566, but not the DA-2 antagonist, domperidone. amicloral 49-55 immunoglobulin heavy diversity 4-11 (non-functional) Homo sapiens 114-118 1982058-6 1990 The renal and systemic vasodilator properties of SK&F R-82526 are antagonized in a competitive fashion by the DA-1 antagonist, SK&F R-83566, but not the DA-2 antagonist, domperidone. amicloral 131-137 immunoglobulin heavy diversity 4-11 (non-functional) Homo sapiens 114-118 1982058-8 1990 Thus, the mechanism of SK&F R-82526-associated vasodilation, like that previously established for fenoldopam, is via stimulation of postganglionic DA-1 receptors. amicloral 23-29 immunoglobulin heavy diversity 4-11 (non-functional) Homo sapiens 151-155 2083145-0 1990 Calmodulin discriminates between the two enantiomers of the receptor-operated calcium channel blocker SK&F 96365: a study using 1H-NMR and chiral HPLC. amicloral 102-108 calmodulin 1 Homo sapiens 0-10 2083145-1 1990 1H nuclear magnetic resonance at 360 MHz shows that SK&F 96365 (1-(beta-[3-(p-methoxyphenyl)-propyloxy]-p-methoxyphenethyl)-1H- imidazole hydrochloride), an antagonist of mammalian receptor-operated calcium channels, interacts with the calcium-binding regulatory protein calmodulin (CaM). amicloral 52-58 calmodulin 1 Homo sapiens 275-285 2083145-1 1990 1H nuclear magnetic resonance at 360 MHz shows that SK&F 96365 (1-(beta-[3-(p-methoxyphenyl)-propyloxy]-p-methoxyphenethyl)-1H- imidazole hydrochloride), an antagonist of mammalian receptor-operated calcium channels, interacts with the calcium-binding regulatory protein calmodulin (CaM). amicloral 52-58 calmodulin 1 Homo sapiens 287-290 2405151-11 1990 The pressor effects of ET-1 were reduced by diltiazem, nitrendipine, verapamil or cromakalim and unchanged after BW 755c, desipramine, enalapril, indomethacin, methysergide, phentolamine or SK&F 100273. amicloral 190-196 endothelin 1 Rattus norvegicus 23-27 2306207-9 1990 Similarly, blockade of the early phase of Ca2+ entry by SK&F 96365 further delays the second phase. amicloral 56-62 carbonic anhydrase 2 Homo sapiens 42-45 2153809-2 1990 SK&F 94120 (1-10 microM) potentiated relaxation induced by isoproterenol, vasoactive intestinal peptide (VIP) and electrical field stimulation (EFS) in the presence of atropine and propranolol but had no effect on relaxation induced by sodium nitroprusside. amicloral 0-6 VIP peptides Cavia porcellus 109-112 1688665-1 1990 SK&F 101926, a synthetic peptide, is a potent antagonist of vasopressin at both the V2 and the V1 receptors. amicloral 0-6 arginine vasopressin Rattus norvegicus 64-75 2577500-3 1989 There was also a sustained and significant 80% rise in median 24-h integrated plasma-gastrin concentration during dosing with SK&F 94482 (364 pmol h/L) when compared with placebo (202 pmol h/L; P = 0.003). amicloral 126-132 gastrin Homo sapiens 85-92 2559032-7 1989 The 5-lipoxygenase inhibitors, SK&F 86002, SK&F 104493, and phenidone inhibited LTB4 production in vivo as well as inflammatory cell infiltration induced by arachidonic acid. amicloral 31-37 arachidonate 5-lipoxygenase Mus musculus 4-18 2574051-2 1989 SK&F 101468, a non phenolic indolone derivative, has been characterised preclinically as a novel, potent and specific dopamine D2-receptor agonist. amicloral 0-6 dopamine receptor D2 Homo sapiens 122-142 2571297-8 1989 SK&F 83566-C, a selective DA1 dopaminergic receptor antagonist, prevented the induction of FM and dopamine-induced hemorrhagic lesions of large caliber arteries. amicloral 0-6 RT1 class II, locus Da Rattus norvegicus 30-33 2571511-0 1989 The alpha 2-adrenoceptor antagonist SK&F 104078 has high affinity for 5-HT1A and 5-HT2 receptors. amicloral 36-42 5-hydroxytryptamine receptor 1A Rattus norvegicus 74-86 2571511-1 1989 The affinity of SK&F 104078, a putative selective postjunctional alpha 2-adrenoceptor antagonist, was determined at 5-HT1A and 5-HT2 receptors in rat brain. amicloral 16-22 5-hydroxytryptamine receptor 1A Rattus norvegicus 120-132 2570079-0 1989 Application of thermospray liquid chromatography-mass spectrometry and liquid chromatography-tandem mass spectrometry for the identification of cynomolgus monkey and human metabolites of SK & F 101468, a dopamine D2 receptor agonist. amicloral 187-194 dopamine receptor D2 Homo sapiens 208-228 2543692-1 1989 Growth hormone-releasing peptide (GHRP, SK&F 110679) is a hexapeptide (His-DTrp-Ala-Trp-DPhe-LysNH2) that selectively stimulates the release of growth hormone (GH) but not other pituitary hormones in vitro and in vivo in a variety of animal species. amicloral 40-46 ghrelin and obestatin prepropeptide Homo sapiens 0-32 2543692-1 1989 Growth hormone-releasing peptide (GHRP, SK&F 110679) is a hexapeptide (His-DTrp-Ala-Trp-DPhe-LysNH2) that selectively stimulates the release of growth hormone (GH) but not other pituitary hormones in vitro and in vivo in a variety of animal species. amicloral 40-46 ghrelin and obestatin prepropeptide Homo sapiens 34-38 2543692-1 1989 Growth hormone-releasing peptide (GHRP, SK&F 110679) is a hexapeptide (His-DTrp-Ala-Trp-DPhe-LysNH2) that selectively stimulates the release of growth hormone (GH) but not other pituitary hormones in vitro and in vivo in a variety of animal species. amicloral 40-46 growth hormone 1 Homo sapiens 148-162 2559032-7 1989 The 5-lipoxygenase inhibitors, SK&F 86002, SK&F 104493, and phenidone inhibited LTB4 production in vivo as well as inflammatory cell infiltration induced by arachidonic acid. amicloral 47-53 arachidonate 5-lipoxygenase Mus musculus 4-18 2678952-2 1989 SK&F 86002, a dual inhibitor of the arachidonate metabolism, has been shown to inhibit LPS induced IL-1 production in human monocytes. amicloral 0-6 interleukin 1 alpha Homo sapiens 103-107 2678952-4 1989 The IC50 of SK&F 86002 for the TNF production was 5-8 microM, and greater than 20 microM for the other three cytokines. amicloral 12-18 tumor necrosis factor Homo sapiens 35-38 2678952-6 1989 Taken together these data indicate that the inhibitory effect of SK&F 86002 on IL-1 production is selective and the production of cytokines in drug treated monocytes can be differentially affected. amicloral 65-71 interleukin 1 alpha Homo sapiens 83-87 2801311-0 1989 Inhibitory effect of SK&F 86002 on monocyte IL-1 production. amicloral 21-27 interleukin 1 alpha Homo sapiens 48-52 2801311-2 1989 SK&F 86002-A2 was shown to be a potent inhibitor of IL-1 production with a 50% inhibitory concentration (IC50) of 1.3 +/- 0.5 microM. amicloral 0-6 interleukin 1 alpha Homo sapiens 56-60 2801311-6 1989 Thus, SK&F 86002 may serve as a useful reagent in the understanding of the synthetic, processing and/or secretory pathways of interleukin-1, and may provide important insight into the treatment of disease states where aberrant IL-1 production is implicated. amicloral 6-12 interleukin 1 alpha Homo sapiens 231-235 2524585-0 1989 Cyclooxygenase inhibition unmasks the full antidiuretic agonist activity of the vasopressin antagonist, SK&F 101926, in dogs. amicloral 104-110 prostaglandin-endoperoxide synthase 1 Canis lupus familiaris 0-14 2524585-0 1989 Cyclooxygenase inhibition unmasks the full antidiuretic agonist activity of the vasopressin antagonist, SK&F 101926, in dogs. amicloral 104-110 arginine vasopressin Rattus norvegicus 80-91 2566992-4 1989 Two mixed DA D1/D2 antagonists (cis(Z)-flupentixol and zuclopenthixol) inhibited the effects of both SK&F 38393 and pergolide on the spinal reflex, while the neuroleptically inactive isomer of clopenthixol (trans(E)-clopenthixol) was also inactive in this context. amicloral 101-107 defender against cell death 1 Rattus norvegicus 10-15 2522994-2 1989 A new animal model for vasopressin activity has been developed in dogs that duplicates the clinical agonist findings exhibited with SK&F 101926. amicloral 132-138 arginine vasopressin Homo sapiens 23-34 2568682-7 1989 The presence of DA1 receptors was confirmed in isolated perfused mesenteric arteries by standard pharmacologic techniques; stimulation by FM resulted in vasodilation which was inhibited by the DA1 receptor antagonist SK&F 83566-C. amicloral 217-223 RT1 class II, locus Da Rattus norvegicus 16-19 2492908-8 1989 The administration of SK&F 86002 to P. acnes/LPS-treated mice decreased serum levels of tumor necrosis factor (TNF), which was not observed following naproxen or indomethacin treatment. amicloral 22-28 tumor necrosis factor Mus musculus 92-113 2492908-8 1989 The administration of SK&F 86002 to P. acnes/LPS-treated mice decreased serum levels of tumor necrosis factor (TNF), which was not observed following naproxen or indomethacin treatment. amicloral 22-28 tumor necrosis factor Mus musculus 115-118 2560662-15 1989 The 5-lipoxygenase/cyclooxygenase inhibitors, SK & F 86002 and BW 775C, also attenuated the endotoxin-induced increase in hematocrit, whereas indomethacin, heparin, daltroban, or the selective V1 vasopressin receptor antagonist [d(CH2)5Tyr(Me)]AVP did not significantly affect the endotoxin-induced hemoconcentration. amicloral 46-53 arachidonate 5-lipoxygenase Rattus norvegicus 4-18 2469790-0 1989 SK&F 93574, a histamine H2-receptor antagonist, releases histamine in the dog. amicloral 0-6 histamine receptor H2 Canis lupus familiaris 18-39 2568682-7 1989 The presence of DA1 receptors was confirmed in isolated perfused mesenteric arteries by standard pharmacologic techniques; stimulation by FM resulted in vasodilation which was inhibited by the DA1 receptor antagonist SK&F 83566-C. amicloral 217-223 RT1 class II, locus Da Rattus norvegicus 193-196 3142488-4 1988 Treatment with SK&F 86002, SK&F 104351, phenidone, or dexamethasone significantly reduced disease severity, as judged by clinical score (55%, 72%, 41%, and 45% inhibition, respectively) and SAP levels (62%, 94%, 52%, and 94% inhibition, respectively) in arthritic mice. amicloral 15-21 amyloid P component, serum Mus musculus 198-201 3142488-4 1988 Treatment with SK&F 86002, SK&F 104351, phenidone, or dexamethasone significantly reduced disease severity, as judged by clinical score (55%, 72%, 41%, and 45% inhibition, respectively) and SAP levels (62%, 94%, 52%, and 94% inhibition, respectively) in arthritic mice. amicloral 31-37 amyloid P component, serum Mus musculus 198-201 3572812-2 1987 SK&F 102698 [1-(3,5-difluorobenzyl)imidazole-2-thiol] is the prototype molecule of this class of substituted 1-benzylimidazole-2-thiols and is one of the most potent inhibitors of DBH yet described. amicloral 0-6 dopamine beta-hydroxylase Rattus norvegicus 184-187 2898333-1 1988 The pharmacokinetics of SK&F recombinant two-chain tissue-type plasminogen activator (tPA) following intravenous (iv) infusion were characterized in anesthetized, open chested mongrel dogs in which artificial intracoronary thrombi were formed. amicloral 24-30 tissue-type plasminogen activator Canis lupus familiaris 90-93 2828915-9 1988 Lysine vasopressin, the selective V2 agonist dDAVP, and the V1-selective agonist SK&F 105349 were at least 10- to 100-fold less potent than oxytocin and exhibited only partial agonist activity. amicloral 81-87 oxytocin/neurophysin I prepropeptide Sus scrofa 144-152 2894879-0 1988 Zolantidine (SK&F 95282) is a potent selective brain-penetrating histamine H2-receptor antagonist. amicloral 13-19 histamine receptor H 2 Rattus norvegicus 69-90 3148560-0 1988 Inhibition of monocyte IL-1 production by the anti-inflammatory compound, SK&F 86002. amicloral 74-80 interleukin 1 alpha Homo sapiens 23-27 3148560-2 1988 SK&F 86002, a novel dihydroimidazo thiazoline which inhibits both 5-lipoxygenase- and cyclooxygenase-mediated arachidonate metabolism was shown to be a potent inhibitor of IL-1 production by LPS-stimulated human monocytes. amicloral 0-6 arachidonate 5-lipoxygenase Homo sapiens 70-84 3148560-2 1988 SK&F 86002, a novel dihydroimidazo thiazoline which inhibits both 5-lipoxygenase- and cyclooxygenase-mediated arachidonate metabolism was shown to be a potent inhibitor of IL-1 production by LPS-stimulated human monocytes. amicloral 0-6 interleukin 1 alpha Homo sapiens 176-180 3148560-7 1988 The inhibition of IL-1 production by SK&F 86002 adds another facet of drug action contributing to its spectrum of anti-inflammatory activities. amicloral 37-43 interleukin 1 alpha Homo sapiens 18-22 2963185-1 1988 The dopamine D-1 agonist SK&F 38393 (10 mg/kg) the D-2 agonist (-)-NPA (0.04 mg/kg) and d-amphetamine (1.0 mg/kg) were established as discriminative stimuli versus saline in rats. amicloral 25-31 solute carrier family 3 member 1 Rattus norvegicus 55-58 2522994-3 1989 In this model we have discovered that substitution of a cis-4"-methyl group on the Pmp moiety at residue 1 of vasopressin antagonists results in substantially reduced agonist activity compared to the unsubstituted molecule (SK&F 101926). amicloral 224-230 arginine vasopressin Homo sapiens 110-121 3050029-0 1988 Further characterization of the cardiovascular effects of the dopamine beta-hydroxylase inhibitor SK&F 102698 in conscious hypertensive rats. amicloral 98-104 dopamine beta-hydroxylase Rattus norvegicus 62-87 3050029-1 1988 The dopamine beta-hydroxylase inhibitor SK&F 102698 was characterized by studying its cardiovascular effects in hypertensive rats. amicloral 40-46 dopamine beta-hydroxylase Rattus norvegicus 4-29 3050029-6 1988 The antihypertensive mechanism of action of dopamine beta-hydroxylase inhibition was probed with the selective DA1-receptor antagonist SCH 23390, which produced an attenuation of the antihypertensive effects of SK&F 102698. amicloral 211-217 dopamine beta-hydroxylase Rattus norvegicus 44-69 3050029-13 1988 These data indicate that inhibition of dopamine beta-hydroxylase with SK&F 102698 results in both peripherally and centrally mediated cardiovascular effects and suggest that central dopamine receptors contribute to the control of systemic blood pressure in hypertensive models associated with an increased sympathetic outflow. amicloral 70-76 dopamine beta-hydroxylase Rattus norvegicus 39-64 3388423-1 1988 The purpose of this study was to determine whether a 30-day administration of SK&F 86002-A2, an inhibitor of cyclooxygenase and 5-lipoxygenase pathways of arachidonate metabolism, adversely affected reproductive cycles, ovarian structure, and/or pituitary/ovarian hormone secretion. amicloral 78-84 arachidonate 5-lipoxygenase Rattus norvegicus 132-146 3385645-0 1988 Effects of the novel dopamine beta-hydroxylase inhibitor SK&F 102698 on catecholamines and blood pressure in spontaneously hypertensive rats. amicloral 57-63 dopamine beta-hydroxylase Rattus norvegicus 21-46 3385645-1 1988 The novel dopamine beta-hydroxylase (D beta H) inhibitor SK&F 102698 was characterized in vitro with soluble enzyme from bovine adrenal medulla and in vivo by measuring the dopamine/norepinephrine (DA/NE) ratio in the mesenteric artery, heart and brains of spontaneously hypertensive rats (SHR). amicloral 57-63 dopamine beta-hydroxylase Bos taurus 10-35 3361442-1 1988 The vasopressin analog desGly(CH2)5D-Tyr(Et)VAVP (SK&F 101926) is a potent antagonist of the antidiuretic action of vasopressin in rats, dogs, and squirrel monkeys, demonstrating minimal agonist activity in these species. amicloral 50-56 arginine vasopressin Rattus norvegicus 4-15 3361442-1 1988 The vasopressin analog desGly(CH2)5D-Tyr(Et)VAVP (SK&F 101926) is a potent antagonist of the antidiuretic action of vasopressin in rats, dogs, and squirrel monkeys, demonstrating minimal agonist activity in these species. amicloral 50-56 arginine vasopressin Rattus norvegicus 120-131 2837395-9 1988 The ability of SK&F 104353 to block LTD4-induced activation of PKC further suggests that stimulation of PKC might be an important intermediate step in the signal transduction mechanism of the LTD4 receptor in RBL-1 cells. amicloral 15-21 RB transcriptional corepressor like 1 Rattus norvegicus 213-218 2963816-3 1988 These responses to vasopressin were inhibited by the V1-specific antagonist SK&F 100273, indicating that these were receptor-mediated phenomena. amicloral 76-82 arginine vasopressin Rattus norvegicus 19-30 2906470-3 1988 Furthermore, toxicologic problems of unsurmountable and/or or long-acting histamine H2-receptor antagonists (tiotidine, loxtidine, and SK&F 93479) are discussed. amicloral 135-141 histamine receptor H2 Homo sapiens 74-95 2823821-3 1987 In addition, SK&F 86002 inhibited the generation of dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE) by a high speed supernatant fraction of RBL-1 cells (IC50 10 microM). amicloral 13-19 RB transcriptional corepressor like 1 Homo sapiens 180-185 2823821-4 1987 Cellular production of 5-lipoxygenase products was inhibited by SK&F 86002 as measured by leukotriene B4 (LTB4) generation from human neutrophils (IC50 20 microM), leukotriene C4 (LTC4) generation by human monocytes (IC50 20 microM), and 5-HETE production by RBL-1 cells (IC50 40 microM). amicloral 64-70 arachidonate 5-lipoxygenase Homo sapiens 23-37 2823821-4 1987 Cellular production of 5-lipoxygenase products was inhibited by SK&F 86002 as measured by leukotriene B4 (LTB4) generation from human neutrophils (IC50 20 microM), leukotriene C4 (LTC4) generation by human monocytes (IC50 20 microM), and 5-HETE production by RBL-1 cells (IC50 40 microM). amicloral 64-70 RB transcriptional corepressor like 1 Homo sapiens 263-268 3039684-2 1987 SK&F 88046 inhibited platelet aggregation and secretion induced by AA, U46619, EP171 and thrombin at low (0.05 U/ml) but not at a high (1 U/ml) concentrations. amicloral 0-6 coagulation factor II, thrombin Homo sapiens 93-101 3572812-7 1987 SK&F 102698 inhibited DBH in vivo as demonstrated by its ability to increase vascular levels of dopamine (DA) while concomitantly decreasing vascular levels of norepinephrine (NE), thus increasing the overall DA/NE ratio. amicloral 0-6 dopamine beta-hydroxylase Rattus norvegicus 26-29 2882972-8 1987 These studies indicate that the omega- and (omega-1)-hydroxylations of SK&F 102,081 are probably carried out by different isozymes of hepatic cytochrome P-450 in the rat. amicloral 71-77 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 146-162 2963185-13 1988 It is concluded that the cues induced by SK&F 38393 and (-)-NPA are mediated by separate D-1 and D-2 sites, whereas both sites contribute to the effect of d-amphetamine. amicloral 41-47 solute carrier family 3 member 1 Rattus norvegicus 101-104 2951585-2 1987 We chose to radiolabel SK&F 101926 because this vasopressin analog is a potent antagonist of vascular V1 and renal V2 vasopressin receptors in all species studied. amicloral 23-29 arginine vasopressin Rattus norvegicus 52-63 2886338-1 1987 Temelastine (SK&F 93944) is a novel histamine H1-receptor antagonist with a high degree of protein binding and predominant hepatic elimination. amicloral 13-19 histamine receptor H1 Homo sapiens 40-61 2949991-6 1987 The maximal effects of SK & F 38393 plus quinpirole were effectively blocked by either a D-1 antagonist (SCH 23390) or a D-2 antagonist (YM 09151-2) confirming the close relation between D-1 and D-2 receptor sites in the brain. amicloral 23-30 solute carrier family 3 member 1 Rattus norvegicus 125-128 2949991-6 1987 The maximal effects of SK & F 38393 plus quinpirole were effectively blocked by either a D-1 antagonist (SCH 23390) or a D-2 antagonist (YM 09151-2) confirming the close relation between D-1 and D-2 receptor sites in the brain. amicloral 23-30 solute carrier family 3 member 1 Rattus norvegicus 199-202 2887313-2 1987 Fenoldopam (SK&F 82526) is a potent agonist at DA1 receptors, with much less agonist activity at the DA2 subtype or at alpha and beta adrenoceptors. amicloral 12-18 RT1 class II, locus Da Rattus norvegicus 51-54 2887313-4 1987 SK&F 85174, the N-allyl derivative of fenoldopam, retains potent DA1 agonist activity but also has moderately potent agonist activity at the DA2 receptor. amicloral 0-6 RT1 class II, locus Da Rattus norvegicus 69-72 2875234-9 1986 Thus, SK&F 93944 is a highly potent, selective histamine H1-receptor antagonist which is efficacious vs. pharmacologic and antigen-induced bronchoconstriction. amicloral 6-12 histamine receptor H1 Canis lupus familiaris 51-72 3490631-0 1986 Stereotyped behaviour in response to the selective D-2 dopamine receptor agonist RU 24213 is enhanced by pretreatment with the selective D-1 agonist SK&F 38393. amicloral 149-155 dopamine receptor D2 Homo sapiens 51-72 2879585-10 1986 SK&F 93944 may have an advantage over classical histamine H1-receptor antagonists in that it is likely to be devoid of untoward effects on the central nervous system. amicloral 0-6 histamine H1 receptor Cavia porcellus 52-73 2873965-3 1986 This stimulation was blocked by the selective DA1 receptor antagonist SK&F 83566, but not by the beta-receptor antagonist propranolol. amicloral 70-76 immunoglobulin heavy diversity 4-11 (non-functional) Homo sapiens 46-49 3594004-3 1986 When SK&F 64 139 was administered (40 mg/kg, ip) to male rats or to female rats during diestrus or proestrus, plasma prolactin levels were not different from those of control groups. amicloral 5-11 prolactin Rattus norvegicus 121-130 3594004-4 1986 Lactating and ovariectomized rats, however, responded to the same SK&F 64 139 dose with an increase in plasma prolactin levels: 210.02 +/- 22.72 vs 378.66 +/- 42.57 (mean +/- SEM) for control of lactating rats, and 4.35 +/- 0.52 vs 6.21 +/- 0.60 ng/ml for control ovariectomized rat. amicloral 66-72 prolactin Rattus norvegicus 114-123 2434770-5 1986 A selective vasopressin pressor (V1) antagonist (SK&F 100273) was inactive as a diuretic agent in these tests. amicloral 49-55 arginine vasopressin Rattus norvegicus 12-23 2434770-6 1986 SK&F 101926 antagonized, in a competitive fashion, exogenous vasopressin-stimulated antidiuresis in conscious water-loaded rats. amicloral 0-6 arginine vasopressin Rattus norvegicus 65-76 6352246-7 1983 However, selective EPI synthesis inhibition with SK&F 64139 only partially prevented this increase in LHRH. amicloral 49-55 gonadotropin releasing hormone 1 Rattus norvegicus 106-110 6152747-0 1984 Pathology of the forestomach in rats treated for 1 year with a new histamine H2-receptor antagonist, SK&F 93479 trihydrochloride. amicloral 101-107 histamine receptor H 2 Rattus norvegicus 67-88 2860689-0 1985 Differential involvement of dopamine D-1 and D-2 receptors in the circling behaviour induced by apomorphine, SK & F 38393, pergolide and LY 171555 in 6-hydroxydopamine-lesioned rats. amicloral 109-116 solute carrier family 3 member 1 Rattus norvegicus 0-48 6151803-5 1984 These findings suggest that SK&F 93479 lacks non-specific antiarrhythmic activity and that its protective effects against coronary artery ligation may be mediated by its histamine H2-receptor antagonizing action. amicloral 28-34 histamine receptor H 2 Rattus norvegicus 174-195 6147403-2 1984 Two centrally active PNMT inhibitors (SK&F 64139 and LY134046) were administered over a 6-day treatment period to cause prolonged reductions in epinephrine formation. amicloral 38-44 phenylethanolamine N-methyltransferase Homo sapiens 21-25 6144180-0 1984 Repeated pentagastrin-stimulated gastric acid secretory tests carried out in the evaluation of the pharmacodynamics of a new histamine H2-receptor antagonist, SK&F 93479. amicloral 159-165 histamine receptor H2 Homo sapiens 125-146 6144180-1 1984 Single doses of 10 mg or 20 mg intravenously or 25 mg or 40 mg orally of a new histamine H2-receptor antagonist, SK&F 93479, have been administered to 31 patients with peptic ulcer disease. amicloral 113-119 histamine receptor H2 Homo sapiens 79-100 6195482-5 1983 Although SK&F 64139 is a potent inhibitor of phenylethanolamine N-methyltransferase (PNMT), the time course of blood pressure reduction is not consistent with PNMT inhibition as a mechanism for its antihypertensive action. amicloral 9-15 phenylethanolamine-N-methyltransferase Rattus norvegicus 49-87 6195482-5 1983 Although SK&F 64139 is a potent inhibitor of phenylethanolamine N-methyltransferase (PNMT), the time course of blood pressure reduction is not consistent with PNMT inhibition as a mechanism for its antihypertensive action. amicloral 9-15 phenylethanolamine-N-methyltransferase Rattus norvegicus 89-93 6132343-11 1982 In pithed rats the pressor responses to both methoxamine and clonidine were antagonized by SK & F 64139 suggesting blockade of vascular alpha 1-and alpha 2-adrenoceptors by the PNMT inhibitor. amicloral 91-98 phenylethanolamine-N-methyltransferase Rattus norvegicus 181-185 6838886-4 1983 Phenylethanolamine-N-methyltransferase inhibitors S-adenosyl-homocysteine and SK & F 64139 can block this photoactivated cross-linkage. amicloral 78-85 phenylethanolamine N-methyltransferase Homo sapiens 0-38 6752375-9 1982 RNa rats treated with SK&F 64139 were found to have decreased phenylethanolamine N-methyltransferase activity by an average 80% in selected brain stem nuclei when compared with nontreated rats. amicloral 22-28 phenylethanolamine-N-methyltransferase Rattus norvegicus 66-104 6223952-0 1982 Short-term toxicological studies with impromidine (SK&F 92676): a specific histamine H2-receptor agonist. amicloral 51-57 histamine receptor H2 Canis lupus familiaris 79-100 6125896-1 1982 SK&F 29661 (1,2,3,4-tetrahydro-7-isoquinoline-sulfonamide) is a potent and selective in vitro and in vivo inhibitor of adrenal phenylethanolamine N-methyltransferase (PNMT; EC 2.1.1.28). amicloral 0-6 phenylethanolamine-N-methyltransferase Rattus norvegicus 131-169 6125896-1 1982 SK&F 29661 (1,2,3,4-tetrahydro-7-isoquinoline-sulfonamide) is a potent and selective in vitro and in vivo inhibitor of adrenal phenylethanolamine N-methyltransferase (PNMT; EC 2.1.1.28). amicloral 0-6 phenylethanolamine-N-methyltransferase Rattus norvegicus 171-175 7202481-1 1980 After 7 day dosing with SK & F 64139, an inhibitor of adrenal and CNS PNMT, a stoichiometric relationship is observed between epinephrine decrease and norepinephrine increase in adrenal tissue. amicloral 24-31 phenylethanolamine-N-methyltransferase Rattus norvegicus 74-78 7252985-3 1981 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (SK&F 64139) is a potent inhibitor of phenylethanolamine N-methyltransferase (IC50 = 10 muM) that may have therapeutic utility in man. amicloral 45-51 phenylethanolamine N-methyltransferase Homo sapiens 86-124 7252985-3 1981 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (SK&F 64139) is a potent inhibitor of phenylethanolamine N-methyltransferase (IC50 = 10 muM) that may have therapeutic utility in man. amicloral 45-51 latexin Homo sapiens 136-139 6119751-2 1981 The parent compound, SK&F 64139, inhibits PNMT in the nanomolar range and also has moderate affinity as an alpha 2-adrenoceptor antagonist. amicloral 21-27 phenylethanolamine N-methyltransferase Homo sapiens 46-50 6119751-6 1981 It was also possible to substantially enhance the PNMT inhibitory activity of a highly polar compound (SK&UF 29661) without decreasing its receptor specificity, although the resulting analogue contains an additional lipophilic chloro substituent and does, unlike SK&F 29661, penetrate into the CNS. amicloral 103-109 phenylethanolamine N-methyltransferase Homo sapiens 50-54 6108034-1 1980 We have compared the effects of cimetidine and SK&F 92994, a new more potent histamine H2 receptor antagonist, on serum prolactin, and also assessed the effect of the H2 receptor agonist impromidine on the response to cimetidine. amicloral 47-53 prolactin Homo sapiens 124-133 6109637-0 1980 The blockade of alpha 2-adrenoceptors by the PNMT inhibitaor SK&F 64139. amicloral 61-67 phenylethanolamine-N-methyltransferase Rattus norvegicus 45-49 7432557-3 1980 The former but not the latter enzyme is markedly inhibited by micromolar concentrations of the PNMT antagonist, SK & F 64139. amicloral 112-119 phenylethanolamine N-methyltransferase Homo sapiens 95-99 445951-1 1979 DCTQ (SK&F 64139) is a potent inhibitor of both adrenal and central nervous system (CNS) phenylethanolamine N-methyltransferase (PNMT). amicloral 6-12 phenylethanolamine N-methyltransferase Homo sapiens 93-131 445951-1 1979 DCTQ (SK&F 64139) is a potent inhibitor of both adrenal and central nervous system (CNS) phenylethanolamine N-methyltransferase (PNMT). amicloral 6-12 phenylethanolamine N-methyltransferase Homo sapiens 133-137 444372-0 1979 Impromidine (SK&F 92676)--a potent and highly selective histamine H2-receptor agonist in man [proceedings]. amicloral 13-19 histamine receptor H2 Homo sapiens 60-81 215747-0 1979 Studies on SK&F 29661, an organ-specific inhibitor of phenylethanolamine N-methyltransferase. amicloral 11-17 phenylethanolamine-N-methyltransferase Rattus norvegicus 58-96 683413-7 1978 Kinetic studies showed that the type of inhibition of PNMT from rat brain and rat adrenals by SK&F 7698 was the same as described for PNMT from rabbit adrenals. amicloral 94-100 phenylethanolamine-N-methyltransferase Rattus norvegicus 54-58 683413-7 1978 Kinetic studies showed that the type of inhibition of PNMT from rat brain and rat adrenals by SK&F 7698 was the same as described for PNMT from rabbit adrenals. amicloral 94-100 phenylethanolamine-N-methyltransferase Rattus norvegicus 138-142 7202481-3 1980 SK & F 64139 was found to possess significant adrenal MAO inhibitory activity, but SK & F 29661 does not. amicloral 0-7 monoamine oxidase A Rattus norvegicus 58-61 7408955-2 1980 The bradycardia, which is abolished by vagotomy and partially antagonized by atropine, was significantly prolonged by pretreatment with SK&F 64139, a potent in vivo inhibitor of peripheral and central (CNS) phenylethanolamine N-methyltransferase (PNMT). amicloral 136-142 phenylethanolamine-N-methyltransferase Rattus norvegicus 211-249 7408955-2 1980 The bradycardia, which is abolished by vagotomy and partially antagonized by atropine, was significantly prolonged by pretreatment with SK&F 64139, a potent in vivo inhibitor of peripheral and central (CNS) phenylethanolamine N-methyltransferase (PNMT). amicloral 136-142 phenylethanolamine-N-methyltransferase Rattus norvegicus 251-255 7408955-4 1980 These data suggest that the effects of SK&F 64139 are a result of inhibition of central PNMT and that epinephrine may function as a central neurotransmitter mediating cardiovascular responses to hemorrhage, at least under the conditions of these studies. amicloral 39-45 phenylethanolamine-N-methyltransferase Rattus norvegicus 92-96 6153165-0 1980 Gastric secretory studies in humans with impromidine (SK&F 92676)--a specific histamine H2 receptor agonist. amicloral 54-60 histamine receptor H2 Homo sapiens 82-103 406652-0 1977 The effect of phenylethanolamine n-methyltransferase concentration and species difference on the inhibitory potency of SK&F 64139. amicloral 119-125 phenylethanolamine N-methyltransferase Homo sapiens 14-52 406652-1 1977 We have found that the potency of SK&F 64139 in inhibiting rabbit adrenal phenylethanolamine N-methyltransferase (PNMT) is a function of protein concentration when high concentrations of the latter are employed. amicloral 34-40 phenylethanolamine N-methyltransferase Oryctolagus cuniculus 78-116 406652-1 1977 We have found that the potency of SK&F 64139 in inhibiting rabbit adrenal phenylethanolamine N-methyltransferase (PNMT) is a function of protein concentration when high concentrations of the latter are employed. amicloral 34-40 phenylethanolamine N-methyltransferase Oryctolagus cuniculus 118-122 406652-5 1977 These data provide evidence that the PNMT receptor sites for SK&F 64139 do not differ substantially from species to species and suggest the general utility of this drug as an inhibitor of adrenal epinephrine biosynthesis. amicloral 61-67 phenylethanolamine N-methyltransferase Homo sapiens 37-41 876399-1 1977 SK&F 64139, an inhibitor of adrenal phenylethanolamine N-methyltransferase (PNMT), was found to significantly decrease 2-deoxy-D-glucose (2-DG) induced epinephrine excretion in the conscious rat under conditions where the former agent was administered chromically at 50 and 200 mg/kg/day over a 12-day period and 2-DG was administered after 3, 7 and 11 days of treatment. amicloral 0-6 phenylethanolamine-N-methyltransferase Rattus norvegicus 40-78 876399-1 1977 SK&F 64139, an inhibitor of adrenal phenylethanolamine N-methyltransferase (PNMT), was found to significantly decrease 2-deoxy-D-glucose (2-DG) induced epinephrine excretion in the conscious rat under conditions where the former agent was administered chromically at 50 and 200 mg/kg/day over a 12-day period and 2-DG was administered after 3, 7 and 11 days of treatment. amicloral 0-6 phenylethanolamine-N-methyltransferase Rattus norvegicus 80-84 590238-8 1977 A potent and selective competitive inhibitor, SK&F 64139, when added to tissue cultures, prevented increase of PNMT activity by prolonged stimulation. amicloral 46-52 phenylethanolamine-N-methyltransferase Rattus norvegicus 115-119 1047087-3 1976 Cefamandole and SK&F 59962 were highly active against both large and small inocula of staphylococci and were resistant to staphylococcal beta-lactamase. amicloral 16-22 beta-lactamase Staphylococcus aureus 141-155 825786-1 1976 Chronic administration of SK&F 64139, an inhibitor of phenylethanolamine N-methyltransferase (PNMT), initially resulted in a lowered adrenal epinephrine content in both the rat and squirrel monkey adrenal gland. amicloral 26-32 phenylethanolamine-N-methyltransferase Rattus norvegicus 58-96 825786-1 1976 Chronic administration of SK&F 64139, an inhibitor of phenylethanolamine N-methyltransferase (PNMT), initially resulted in a lowered adrenal epinephrine content in both the rat and squirrel monkey adrenal gland. amicloral 26-32 phenylethanolamine-N-methyltransferase Rattus norvegicus 98-102 6786-1 1976 SK&F 64139 is a potent, reversible inhibitor of phenylethanolamine N-methyltransferase; its IC50 concentration in our standard assay system was 1 X 10(-7) M. Kinetically, the compound is a competitive inhibitor with respect to norepinephrine but is uncompetitive when S-adenosylmethionine is the variable substrate. amicloral 0-6 phenylethanolamine-N-methyltransferase Rattus norvegicus 52-90