PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 20533894-5 2010 WHAT THE READER WILL GAIN: Chemically diverse non-peptide NK1 receptor antagonists have been identified since the discovery of CP-96,345 by Pfizer in 1991. CP96 127-132 tachykinin receptor 1 Homo sapiens 58-61 20940324-5 2011 This inhibitory effect upon cytotoxicity was partially prevented by the NK1R antagonist CP96,345. CP96 88-92 tachykinin receptor 1 Homo sapiens 72-76 22040127-6 2012 SP treatment increased PPTA and NK1R expression in isolated pancreatic acinar cells, which was abolished by pretreatment of a selective NK1R antagonist, CP96,345. CP96 153-157 tachykinin 1 Mus musculus 0-2 22040127-6 2012 SP treatment increased PPTA and NK1R expression in isolated pancreatic acinar cells, which was abolished by pretreatment of a selective NK1R antagonist, CP96,345. CP96 153-157 tachykinin 1 Mus musculus 23-27 22040127-6 2012 SP treatment increased PPTA and NK1R expression in isolated pancreatic acinar cells, which was abolished by pretreatment of a selective NK1R antagonist, CP96,345. CP96 153-157 tachykinin receptor 1 Mus musculus 32-36 22040127-6 2012 SP treatment increased PPTA and NK1R expression in isolated pancreatic acinar cells, which was abolished by pretreatment of a selective NK1R antagonist, CP96,345. CP96 153-157 tachykinin receptor 1 Mus musculus 136-140 18053315-6 2007 The administration of an NK-1 receptor antagonist, CP-96,345, significantly reduced the BF-increase response to SS in AI rats, but its inactive enantiomer, CP-96,344, had no effect. CP96 51-56 tachykinin receptor 1 Rattus norvegicus 25-38 18602450-9 2008 Hepatic sympathetic denervation and CP96,345 (neurokinin 1 receptor antagonist), not SR48968 (neurokinin 2 receptor antagonist), significantly inhibited AUBD, CRD and AUBD+CRD induced hepatic vasoconstriction. CP96 36-40 tachykinin receptor 1 Rattus norvegicus 46-67 17218475-1 2007 We investigated the effect of a specific neurokinin-1 receptor (NK1R) antagonist, CP-96,345, on the regulation of the expression of adhesion molecules ICAM-1, VCAM-1, E-selectin, and P-selectin as well as leukocyte recruitment during acute pancreatitis (AP). CP96 82-87 tachykinin receptor 1 Mus musculus 41-62 17218475-1 2007 We investigated the effect of a specific neurokinin-1 receptor (NK1R) antagonist, CP-96,345, on the regulation of the expression of adhesion molecules ICAM-1, VCAM-1, E-selectin, and P-selectin as well as leukocyte recruitment during acute pancreatitis (AP). CP96 82-87 tachykinin receptor 1 Mus musculus 64-68 17218475-1 2007 We investigated the effect of a specific neurokinin-1 receptor (NK1R) antagonist, CP-96,345, on the regulation of the expression of adhesion molecules ICAM-1, VCAM-1, E-selectin, and P-selectin as well as leukocyte recruitment during acute pancreatitis (AP). CP96 82-87 intercellular adhesion molecule 1 Mus musculus 151-157 17218475-1 2007 We investigated the effect of a specific neurokinin-1 receptor (NK1R) antagonist, CP-96,345, on the regulation of the expression of adhesion molecules ICAM-1, VCAM-1, E-selectin, and P-selectin as well as leukocyte recruitment during acute pancreatitis (AP). CP96 82-87 vascular cell adhesion molecule 1 Mus musculus 159-165 17218475-1 2007 We investigated the effect of a specific neurokinin-1 receptor (NK1R) antagonist, CP-96,345, on the regulation of the expression of adhesion molecules ICAM-1, VCAM-1, E-selectin, and P-selectin as well as leukocyte recruitment during acute pancreatitis (AP). CP96 82-87 selectin, platelet Mus musculus 183-193 17218475-6 2007 Treatment with CP-96,345 effectively reduced the mRNA expression of P-selectin and E-selectin but not ICAM-1 and VCAM-1. CP96 15-20 selectin, platelet Mus musculus 68-78 17218475-6 2007 Treatment with CP-96,345 effectively reduced the mRNA expression of P-selectin and E-selectin but not ICAM-1 and VCAM-1. CP96 15-20 selectin, endothelial cell Mus musculus 83-93 16873893-9 2007 The suppression effect of CP-96,345 on MCP-1, MIP-1alpha, and MIP-2 expression was concordantly demonstrated by immunohistochemistry, which, additionally, suggested that chemokine immunoreactivity was localized to acinar cells and the infiltrating leukocytes in the pancreas and alveolar macrophages, epithelial cells, and endothelial cells in the lungs. CP96 26-31 chemokine (C-C motif) ligand 3 Mus musculus 46-56 18040825-3 2007 We have previously shown that CP-96,345, a neurokinin-1 receptor (NK-1R) antagonist, inhibits HIV-1 infection of macrophages in vitro by downregulating CCR5 expression (Lai JP, Ho WZ, Zhan GX, Yi Y, Collman RG, Douglas SD 2001). CP96 30-35 tachykinin receptor 1 Homo sapiens 66-71 18040825-3 2007 We have previously shown that CP-96,345, a neurokinin-1 receptor (NK-1R) antagonist, inhibits HIV-1 infection of macrophages in vitro by downregulating CCR5 expression (Lai JP, Ho WZ, Zhan GX, Yi Y, Collman RG, Douglas SD 2001). CP96 30-35 C-C motif chemokine receptor 5 Homo sapiens 152-156 16873893-8 2007 Either prophylactic or therapeutic treatment with a potent selective NK-1R antagonist CP-96,345 significantly suppressed caerulein-induced increase in MCP-1, MIP-1alpha, and MIP-2 expression but had no apparent effect on RANTES expression. CP96 86-91 tachykinin receptor 1 Mus musculus 69-74 16873893-9 2007 The suppression effect of CP-96,345 on MCP-1, MIP-1alpha, and MIP-2 expression was concordantly demonstrated by immunohistochemistry, which, additionally, suggested that chemokine immunoreactivity was localized to acinar cells and the infiltrating leukocytes in the pancreas and alveolar macrophages, epithelial cells, and endothelial cells in the lungs. CP96 26-31 chemokine (C-X-C motif) ligand 2 Mus musculus 62-67 16873893-8 2007 Either prophylactic or therapeutic treatment with a potent selective NK-1R antagonist CP-96,345 significantly suppressed caerulein-induced increase in MCP-1, MIP-1alpha, and MIP-2 expression but had no apparent effect on RANTES expression. CP96 86-91 chemokine (C-C motif) ligand 2 Mus musculus 151-156 16369913-4 2006 Treatment with the NK1R antagonist, CP96,345, results in protection against caerulein-induced acute pancreatitis in mice. CP96 36-40 tachykinin receptor 1 Mus musculus 19-23 16873893-8 2007 Either prophylactic or therapeutic treatment with a potent selective NK-1R antagonist CP-96,345 significantly suppressed caerulein-induced increase in MCP-1, MIP-1alpha, and MIP-2 expression but had no apparent effect on RANTES expression. CP96 86-91 chemokine (C-C motif) ligand 3 Mus musculus 158-168 16873893-8 2007 Either prophylactic or therapeutic treatment with a potent selective NK-1R antagonist CP-96,345 significantly suppressed caerulein-induced increase in MCP-1, MIP-1alpha, and MIP-2 expression but had no apparent effect on RANTES expression. CP96 86-91 chemokine (C-X-C motif) ligand 2 Mus musculus 174-179 16873893-9 2007 The suppression effect of CP-96,345 on MCP-1, MIP-1alpha, and MIP-2 expression was concordantly demonstrated by immunohistochemistry, which, additionally, suggested that chemokine immunoreactivity was localized to acinar cells and the infiltrating leukocytes in the pancreas and alveolar macrophages, epithelial cells, and endothelial cells in the lungs. CP96 26-31 chemokine (C-C motif) ligand 2 Mus musculus 39-44 17071590-6 2006 The substance P receptor antagonist, CP-96,345, not only blocked AW- or PW-induced endogenous substance P expression but also abrogated AW- or PW-induced HIV replication in T cells. CP96 37-42 tachykinin precursor 1 Homo sapiens 4-15 17071590-6 2006 The substance P receptor antagonist, CP-96,345, not only blocked AW- or PW-induced endogenous substance P expression but also abrogated AW- or PW-induced HIV replication in T cells. CP96 37-42 tachykinin precursor 1 Homo sapiens 94-105 16904192-5 2006 Treatment with the NK-1R antagonist CP-96,345 dramatically reduced clinical and histological signs of EAE if administered before disease onset. CP96 36-41 tachykinin receptor 1 Homo sapiens 19-24 16904192-6 2006 The protective effect of CP96,345 treatment was related to a reduced expression of the adhesion molecules ICAM-1 and VCAM-1 on CNS endothelia. CP96 25-29 intercellular adhesion molecule 1 Homo sapiens 106-112 16904192-6 2006 The protective effect of CP96,345 treatment was related to a reduced expression of the adhesion molecules ICAM-1 and VCAM-1 on CNS endothelia. CP96 25-29 vascular cell adhesion molecule 1 Homo sapiens 117-123 16904192-9 2006 In summary, our findings suggest that the protective effect of CP96,345 treatment is mediated by stabilization of the blood-brain barrier and suppression of Th1 immunity. CP96 63-67 negative elongation factor complex member C/D Homo sapiens 157-160 12458047-5 2002 SP-induced MIP-1beta expression is abrogated by the specific NK-1R antagonist (CP-96,345). CP96 79-84 C-C motif chemokine ligand 4 Homo sapiens 11-20 15390113-6 2004 CP-96,345, a specific non-peptide NK-1R antagonist, inhibited SP-induced rise of [Ca(2+)](i) in the astroglioma cells. CP96 0-5 tachykinin receptor 1 Homo sapiens 34-39 14743438-0 2004 A non-peptide substance P antagonist (CP-96,345) inhibits morphine-induced NF-kappa B promoter activation in human NT2-N neurons. CP96 38-43 tachykinin precursor 1 Homo sapiens 14-25 14743438-0 2004 A non-peptide substance P antagonist (CP-96,345) inhibits morphine-induced NF-kappa B promoter activation in human NT2-N neurons. CP96 38-43 nuclear factor kappa B subunit 1 Homo sapiens 75-85 14743438-5 2004 The induced activation of NF-kappaB promoter by morphine or DAMGO was abolished not only by naltrexone (a opioid receptor antagonist) and CTAP (a selective, competitive mu-opioid receptor antagonist), but also by CP-96,345, a non-peptide SP receptor antagonist. CP96 213-218 nuclear factor kappa B subunit 1 Homo sapiens 26-35 14743438-5 2004 The induced activation of NF-kappaB promoter by morphine or DAMGO was abolished not only by naltrexone (a opioid receptor antagonist) and CTAP (a selective, competitive mu-opioid receptor antagonist), but also by CP-96,345, a non-peptide SP receptor antagonist. CP96 213-218 opioid receptor mu 1 Homo sapiens 169-187 14622931-0 2003 Tritiation of nonpeptide substance P antagonist CP-96,345 and its azido analogue. CP96 48-53 tachykinin precursor 1 Homo sapiens 25-36 12458047-5 2002 SP-induced MIP-1beta expression is abrogated by the specific NK-1R antagonist (CP-96,345). CP96 79-84 tachykinin receptor 1 Homo sapiens 61-66 12383866-7 2002 In contrast, the specific nonpeptide NK(1) receptor antagonist CP-96,345 clearly abolished the effect of substance P and [D-Pro(2), D-Trp(7,9)]SP on MAPK activity. CP96 63-68 tachykinin receptor 1 Homo sapiens 37-51 12383866-7 2002 In contrast, the specific nonpeptide NK(1) receptor antagonist CP-96,345 clearly abolished the effect of substance P and [D-Pro(2), D-Trp(7,9)]SP on MAPK activity. CP96 63-68 tachykinin precursor 1 Homo sapiens 105-116 12383866-7 2002 In contrast, the specific nonpeptide NK(1) receptor antagonist CP-96,345 clearly abolished the effect of substance P and [D-Pro(2), D-Trp(7,9)]SP on MAPK activity. CP96 63-68 tachykinin precursor 1 Homo sapiens 143-145 10817615-2 2000 The present study aimed to determine the effect of the selective non-peptide rat neurokinin-1 (NK1) receptor antagonists WIN 51,708 and CP-96,345 on the firing activity of rat dorsal raphe serotonin (5-HT) and locus coeruleus noradrenaline (NA) neurons. CP96 136-141 tachykinin receptor 1 Rattus norvegicus 81-108 11877343-14 2002 A high dose of SP increased the permeability in a manner reversible by the NK(1) receptor antagonist, CP-96,345. CP96 102-107 substance-P receptor Cavia porcellus 75-89 11274418-0 2001 Substance P antagonist (CP-96,345) inhibits HIV-1 replication in human mononuclear phagocytes. CP96 24-29 tachykinin precursor 1 Homo sapiens 0-11 11274418-4 2001 SP enhanced HIV replication in human blood-isolated mononuclear phagocytes, whereas the nonpeptide SP antagonist (CP-96,345) potently inhibited HIV infectivity of these cells in a concentration-dependent fashion. CP96 114-119 tachykinin precursor 1 Homo sapiens 99-101 11274418-7 2001 Both CP-96,345 and anti-SP antibody inhibited SP-enhanced HIV replication in monocyte-derived macrophages (MDM). CP96 5-10 tachykinin precursor 1 Homo sapiens 46-48 11274418-8 2001 Among HIV strains tested (both prototype and primary isolates), only the R5 strains (Bal, ADA, BL-6, and CSF-6) that use the CCR5 coreceptor for entry into MDM were significantly inhibited by CP-96,345; in contrast, the X4 strain (UG024), which uses CXCR4 as its coreceptor, was not inhibited. CP96 192-197 C-C motif chemokine receptor 5 Homo sapiens 125-129 11274418-8 2001 Among HIV strains tested (both prototype and primary isolates), only the R5 strains (Bal, ADA, BL-6, and CSF-6) that use the CCR5 coreceptor for entry into MDM were significantly inhibited by CP-96,345; in contrast, the X4 strain (UG024), which uses CXCR4 as its coreceptor, was not inhibited. CP96 192-197 C-X-C motif chemokine receptor 4 Homo sapiens 250-255 11274418-9 2001 In addition, the M-tropic ADA (CCR5-dependent)-pseudotyped HIV infection of MDM was markedly inhibited by CP-96,345, whereas murine leukemia virus-pseudotyped HIV was not affected, indicating that the major effect of CP-96,345 is regulated by Env-determined early events in HIV infection of MDM. CP96 106-111 C-C motif chemokine receptor 5 Homo sapiens 31-35 11274418-9 2001 In addition, the M-tropic ADA (CCR5-dependent)-pseudotyped HIV infection of MDM was markedly inhibited by CP-96,345, whereas murine leukemia virus-pseudotyped HIV was not affected, indicating that the major effect of CP-96,345 is regulated by Env-determined early events in HIV infection of MDM. CP96 217-222 C-C motif chemokine receptor 5 Homo sapiens 31-35 11005759-7 2000 The NK1-R antagonist CP-96,345 blocked SP-induced plasma extravasation. CP96 21-26 tachykinin receptor 1 Rattus norvegicus 4-9 12098517-3 2002 We recently demonstrated that SP modulates HIV replication and that a non-peptide SP antagonist CP-96,345 inhibits HIV replication in human monocyte-derived macrophages (MDM) by affecting the SP-NK-1R interaction. CP96 96-101 tachykinin precursor 1 Homo sapiens 82-84 12098517-3 2002 We recently demonstrated that SP modulates HIV replication and that a non-peptide SP antagonist CP-96,345 inhibits HIV replication in human monocyte-derived macrophages (MDM) by affecting the SP-NK-1R interaction. CP96 96-101 tachykinin receptor 1 Homo sapiens 195-200 12098517-8 2002 CP-96,345 inhibited HIV replication in MDM, associated with down-regulated SP mRNA expression in comparison to HIV infection controls. CP96 0-5 tachykinin precursor 1 Homo sapiens 75-77 11404389-7 2001 Two selective NK-1 antagonists, CP96,345 and L703,606, dose dependently inhibited SP priming effects. CP96 32-36 tachykinin receptor 1 Homo sapiens 14-18 11039544-8 2000 Prior treatment with CP-96,345 altered muscle responses to SP and EFS, suggesting that SP was released from depolarized myenteric neurons. CP96 21-26 tachykinin precursor 1 Equus caballus 59-61 11039544-8 2000 Prior treatment with CP-96,345 altered muscle responses to SP and EFS, suggesting that SP was released from depolarized myenteric neurons. CP96 21-26 tachykinin precursor 1 Equus caballus 87-89 10771345-6 2000 The substance P antagonists CP96,345 and CP99,994 blocked the nociceptin-induced hyperalgesia, but not the allodynia. CP96 28-32 tachykinin 1 Mus musculus 4-15 10710549-9 2000 These changes are partly mediated by the neurokinin-1 (NK1) receptor (NK1R), as 4 mg/kg of CP-96,345, a highly selective NK1 antagonist, increased fusion in inflamed bladders but had no effect on control bladders. CP96 91-96 substance-P receptor Cavia porcellus 41-68 10710549-9 2000 These changes are partly mediated by the neurokinin-1 (NK1) receptor (NK1R), as 4 mg/kg of CP-96,345, a highly selective NK1 antagonist, increased fusion in inflamed bladders but had no effect on control bladders. CP96 91-96 substance-P receptor Cavia porcellus 70-74 10696090-10 2000 Pretreatment with the NK(1) receptor antagonist, CP-96,994, abolished the ability of L-NAME to increase bronchoconstriction to aerosolized NKA. CP96 49-54 substance-P receptor Cavia porcellus 22-36 10030226-13 1999 The laryngeal adductor response to SP infusion was blocked when animals were pretreated with a systemic SP antagonist (Pfizer CP-96,345). CP96 126-131 tachykinin precursor 1 Homo sapiens 35-37 10455330-14 1999 The NK1 receptor antagonists, CP-96,345, CP-99,994 and sendide, inhibited nociceptin-induced behavioural response in a dose-dependent manner. CP96 30-35 tachykinin receptor 1 Mus musculus 4-16 10455330-14 1999 The NK1 receptor antagonists, CP-96,345, CP-99,994 and sendide, inhibited nociceptin-induced behavioural response in a dose-dependent manner. CP96 30-35 prepronociceptin Homo sapiens 74-84 10079105-9 1999 Our results show that neurotensin-induced mast cell degranulation in colonic explants is inhibited by the substance P (neurokinin-1) receptor antagonist CP-96,345, indicating that colonic mast activation in response to neurotensin involves release of substance P. We conclude that neurotensin plays a key role in the pathogenesis of C. difficile-induced colonic inflammation and mast cell activation. CP96 153-158 neurotensin Rattus norvegicus 22-33 10079105-9 1999 Our results show that neurotensin-induced mast cell degranulation in colonic explants is inhibited by the substance P (neurokinin-1) receptor antagonist CP-96,345, indicating that colonic mast activation in response to neurotensin involves release of substance P. We conclude that neurotensin plays a key role in the pathogenesis of C. difficile-induced colonic inflammation and mast cell activation. CP96 153-158 tachykinin receptor 1 Rattus norvegicus 119-141 10079105-9 1999 Our results show that neurotensin-induced mast cell degranulation in colonic explants is inhibited by the substance P (neurokinin-1) receptor antagonist CP-96,345, indicating that colonic mast activation in response to neurotensin involves release of substance P. We conclude that neurotensin plays a key role in the pathogenesis of C. difficile-induced colonic inflammation and mast cell activation. CP96 153-158 neurotensin Rattus norvegicus 219-230 10079105-9 1999 Our results show that neurotensin-induced mast cell degranulation in colonic explants is inhibited by the substance P (neurokinin-1) receptor antagonist CP-96,345, indicating that colonic mast activation in response to neurotensin involves release of substance P. We conclude that neurotensin plays a key role in the pathogenesis of C. difficile-induced colonic inflammation and mast cell activation. CP96 153-158 neurotensin Rattus norvegicus 219-230 10414986-3 1999 In electrophysiological experiments on single dorsal horn neurons in vivo, the excitatory responses to subcutaneous formalin injection (50 microliter, 2.5%) were attenuated by subsequent intravenously administration of the NK-1 receptor antagonist CP-96,345 (0.5 mg/kg; n = 8), given 35-40 min after formalin, but not by the inactive enantiomer CP-96,344 (0.5 mg/kg; n = 9). CP96 248-253 tachykinin receptor 1 Rattus norvegicus 223-236 10414986-3 1999 In electrophysiological experiments on single dorsal horn neurons in vivo, the excitatory responses to subcutaneous formalin injection (50 microliter, 2.5%) were attenuated by subsequent intravenously administration of the NK-1 receptor antagonist CP-96,345 (0.5 mg/kg; n = 8), given 35-40 min after formalin, but not by the inactive enantiomer CP-96,344 (0.5 mg/kg; n = 9). CP96 345-350 tachykinin receptor 1 Rattus norvegicus 223-236 10030226-13 1999 The laryngeal adductor response to SP infusion was blocked when animals were pretreated with a systemic SP antagonist (Pfizer CP-96,345). CP96 126-131 tachykinin precursor 1 Homo sapiens 104-106 9558284-7 1998 Administration of a specific substance P-receptor antagonist (CP-96,345) reduced toxin A-induced intestinal fluid secretion and inhibited neutrophil infiltration in normal, mast cell-deficient KitW/KitW-v, and mast cell-reconstituted KitW/KitW-v mice. CP96 62-67 tachykinin receptor 1 Mus musculus 29-49 10422886-6 1999 The GR73632-induced behavioral response was inhibited by IT co-administration of CP-96,345, a non-peptide NK1 receptor antagonist, but not its inactive enantiomer CP-96,344. CP96 81-86 tachykinin receptor 1 Mus musculus 106-118 10422886-7 1999 CP-96,345, co-injected IT with substance P, also inhibited the behavioral response to substance P. CP96 0-5 tachykinin 1 Mus musculus 31-42 10422886-7 1999 CP-96,345, co-injected IT with substance P, also inhibited the behavioral response to substance P. CP96 0-5 tachykinin 1 Mus musculus 86-97 9547942-4 1998 This current investigation employs site directed mutagenesis of the NK-1 receptor to compare the binding site of CP-96,345 with that of a related compound CP-99,994. CP96 113-118 tachykinin receptor 1 Homo sapiens 68-81 9114070-6 1997 Pretreatment of rats with the SP antagonist CP-96,345 inhibits toxin A-mediated TNFalpha release from isolated LPMs, whereas an inactive enantiomer (CP-96,344) of the SP antagonist has no effect. CP96 44-49 tumor necrosis factor Rattus norvegicus 80-88 9453348-6 1998 After nTS injection of the NK1-selective SP antagonist CP-96,345 (30 pmol in 60 nL), Ang II-induced hypotension was blocked in both groups, as was the pressor component in hypertensive rats. CP96 55-60 angiotensinogen Rattus norvegicus 85-91 9190858-0 1997 CP-96,345, which inhibits [3H] substance P binding, selectively inhibits the behavioral response to intrathecally administered N-methyl-D-aspartate, but not substance P, in the mouse. CP96 0-5 tachykinin 1 Mus musculus 31-42 9190858-1 1997 ((2S,3S)-[cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)-methyl]-1-az abicyclo[2.2.2]octan-3-amine]) (CP-96,345) noncompetitively inhibits substance P (SP) binding at the neurokinin-1 (NK-1) site and has been widely used to determine the extent of NK-1 activity in nociception. CP96 99-104 tachykinin 1 Mus musculus 136-147 9190858-1 1997 ((2S,3S)-[cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)-methyl]-1-az abicyclo[2.2.2]octan-3-amine]) (CP-96,345) noncompetitively inhibits substance P (SP) binding at the neurokinin-1 (NK-1) site and has been widely used to determine the extent of NK-1 activity in nociception. CP96 99-104 tachykinin 1 Mus musculus 149-151 9190858-1 1997 ((2S,3S)-[cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)-methyl]-1-az abicyclo[2.2.2]octan-3-amine]) (CP-96,345) noncompetitively inhibits substance P (SP) binding at the neurokinin-1 (NK-1) site and has been widely used to determine the extent of NK-1 activity in nociception. CP96 99-104 tachykinin 1 Mus musculus 168-180 9190858-1 1997 ((2S,3S)-[cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)-methyl]-1-az abicyclo[2.2.2]octan-3-amine]) (CP-96,345) noncompetitively inhibits substance P (SP) binding at the neurokinin-1 (NK-1) site and has been widely used to determine the extent of NK-1 activity in nociception. CP96 99-104 tachykinin 1 Mus musculus 182-186 9190858-1 1997 ((2S,3S)-[cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)-methyl]-1-az abicyclo[2.2.2]octan-3-amine]) (CP-96,345) noncompetitively inhibits substance P (SP) binding at the neurokinin-1 (NK-1) site and has been widely used to determine the extent of NK-1 activity in nociception. CP96 99-104 tachykinin 1 Mus musculus 245-249 9190858-7 1997 The more potent inhibitor of [3H] SP binding, (+)-(2S,3S)-3-(2-methoxybenzylamino)-2-phenylpiperidine (CP-99,994), was approximately 10 times more potent in inhibiting NMDA-induced activity than CP-96,345. CP96 195-200 tachykinin 1 Mus musculus 34-36 9190858-9 1997 Also attenuated by CP-96,345 was the development of sensitization to the behavioral effects produced by repeated injections of KA and desensitization to repeated injections of SP, phenomena linked to an action of the N-terminus of SP. CP96 19-24 tachykinin 1 Mus musculus 176-178 9190858-9 1997 Also attenuated by CP-96,345 was the development of sensitization to the behavioral effects produced by repeated injections of KA and desensitization to repeated injections of SP, phenomena linked to an action of the N-terminus of SP. CP96 19-24 tachykinin 1 Mus musculus 231-233 9190858-12 1997 Whether CP-96,345 acts by a mechanism that involves inhibition of calcium channels and/or SP N-terminal activity requires further testing. CP96 8-13 tachykinin 1 Mus musculus 90-92 9808062-4 1998 Pretreatment with CP-96,345 and SR-48,968 (neurokinin-1 and -2 receptor antagonists; each 1 mg/kg) in combination totally prevented this SIAHR, while pretreatment with CP-96,344 and SR48,965 (inactive enantiomers of CP-96,345 and SR-48,968, each 1 mg/kg) in combination failed to do so. CP96 18-23 substance-P receptor Cavia porcellus 43-71 9114070-8 1997 In addition, LPMs obtained from toxin A-injected ileal loops incubated in vitro with CP-96,345 showed a diminished TNFalpha release. CP96 85-90 tumor necrosis factor Rattus norvegicus 115-123 8672532-9 1996 The NK1 receptor antagonist, CP96,345 specifically inhibited the SP-stimulated changes in [Ca2+]i and pepsinogen secretion. CP96 29-33 tachykinin receptor 1 Homo sapiens 4-16 8944719-3 1996 The SP (10(-8) M)-induced contraction was inhibited by tachykinin NK1 receptor antagonists (rank order of potency: SR-140333 > CP-96,345 > RP-67580) but not by the tachykinin NK2 receptor antagonist SR-48968. CP96 130-135 tachykinin precursor 1 Homo sapiens 4-6 8944719-3 1996 The SP (10(-8) M)-induced contraction was inhibited by tachykinin NK1 receptor antagonists (rank order of potency: SR-140333 > CP-96,345 > RP-67580) but not by the tachykinin NK2 receptor antagonist SR-48968. CP96 130-135 tachykinin receptor 1 Homo sapiens 66-69 8895243-4 1996 Intrathecal pretreatment with the NK-1 receptor antagonist CP-96,345 (100, 50, 25 nmol) dose-dependently attenuated the thermal (46%, 27% and 16%, respectively) and mechanical (66%, 37% and 3%, respectively) hyperalgesia produced by 2 mg carrageenan, but not 6 mg carrageenan, 3 h after the induction of inflammation. CP96 59-64 tachykinin receptor 1 Rattus norvegicus 34-47 9113332-5 1997 Also, a superposition based on pharmacophoric elements in the crystal structure conformations of two prototypic NK1 antagonists, CP-96,345 (1) and CP-99,994 (4), suggests how both compounds might interact with the human NK1 receptor in a similar manner. CP96 129-134 tachykinin receptor 1 Homo sapiens 112-115 9113332-5 1997 Also, a superposition based on pharmacophoric elements in the crystal structure conformations of two prototypic NK1 antagonists, CP-96,345 (1) and CP-99,994 (4), suggests how both compounds might interact with the human NK1 receptor in a similar manner. CP96 129-134 tachykinin receptor 1 Homo sapiens 220-232 8997258-5 1996 SP-afforded protection was reduced by the neurokinin (NK)-1 receptor antagonist CP-96,345.NK1 and NK3 receptor agonists also inhibited ozone-induced permeability, whereas an NK2 receptor agonist was without significant effect. CP96 80-85 tachykinin precursor 1 Homo sapiens 0-2 8997258-5 1996 SP-afforded protection was reduced by the neurokinin (NK)-1 receptor antagonist CP-96,345.NK1 and NK3 receptor agonists also inhibited ozone-induced permeability, whereas an NK2 receptor agonist was without significant effect. CP96 80-85 tachykinin receptor 1 Homo sapiens 42-68 8997258-5 1996 SP-afforded protection was reduced by the neurokinin (NK)-1 receptor antagonist CP-96,345.NK1 and NK3 receptor agonists also inhibited ozone-induced permeability, whereas an NK2 receptor agonist was without significant effect. CP96 80-85 tachykinin receptor 1 Homo sapiens 90-93 8997258-5 1996 SP-afforded protection was reduced by the neurokinin (NK)-1 receptor antagonist CP-96,345.NK1 and NK3 receptor agonists also inhibited ozone-induced permeability, whereas an NK2 receptor agonist was without significant effect. CP96 80-85 tachykinin receptor 2 Homo sapiens 174-186 8982105-4 1996 The stimulatory effects of SP on TNF-alpha secretion are inhibited by a anti-SP polyclonal antibody and SP antagonists, spantide ([D-Arg-1-D-Trp-7-D-Trp-9-Leu-11]-SP) and CP-96,345 (a nonpeptide antagonist of the SP receptor). CP96 171-176 tumor necrosis factor Homo sapiens 33-42 8672532-9 1996 The NK1 receptor antagonist, CP96,345 specifically inhibited the SP-stimulated changes in [Ca2+]i and pepsinogen secretion. CP96 29-33 tachykinin precursor 1 Homo sapiens 65-67 8622630-4 1996 SP prevented photolabeling only at concentrations higher than expected from its binding affinity but similar to those shown in a competition binding assay to displace radioiodinated analogue of CP-96,345. CP96 194-199 tachykinin precursor 1 Homo sapiens 0-2 8738221-10 1996 In addition, pretreatment with CP96,345 into the medial hypothalamus blocked the suppressive effects of subsequent delivery of [Sar9,Met(O2)11]-substance P into the same medial hypothalamic site. CP96 31-35 tachykinin precursor 1 Homo sapiens 144-155 8925284-4 1995 The release was also blocked by intrathecal pretreatment with the NMDA antagonist MK-801 (3 micrograms) and the NK-1 receptor antagonist CP96,345 (200 micrograms), whereas the AMPA receptor antagonist NBQX (6 micrograms) yielded no significant inhibition. CP96 137-141 tachykinin receptor 1 Rattus norvegicus 112-125 8738221-7 1996 In the second phase of the study, dose and time dependent decreases in response suppression were noted following the infusion of the substance P (NK1) receptor antagonist, CP96.345 (in doses of 0.05, 0.5 and 2.5 nmol) into the medial hypothalamus. CP96 172-176 tachykinin precursor 1 Homo sapiens 133-144 8738221-7 1996 In the second phase of the study, dose and time dependent decreases in response suppression were noted following the infusion of the substance P (NK1) receptor antagonist, CP96.345 (in doses of 0.05, 0.5 and 2.5 nmol) into the medial hypothalamus. CP96 172-176 tachykinin receptor 1 Homo sapiens 146-159 9123986-6 1996 The NK1 receptor antagonist CP-96,345 similarly inhibited responses to these agonists, although with higher IC50 estimates of 0.84 microM (0.51-1.40 microM) against SPOMe, 0.79 microM (0.50-1.17 microM) against/Sar9/-SP-sulphone and 0.37 microM (0.27-0.51 microM) against septide. CP96 28-33 tachykinin receptor 1 Rattus norvegicus 4-16 8731437-4 1996 The plateau contraction induced by SP (60 nM) was significantly reduced by the NK1 receptor antagonist CP-96,345 (200 nM) added 5 min after SP, but was not affected by its inactive enantiomer CP-96,344 (200 nM). CP96 103-108 substance-P receptor Cavia porcellus 79-91 8577379-5 1995 CP-96,345 and WIN 51,708, neurokinin1 receptor antagonists, attenuated the response to substance P, neurokinin A and neurokinin B. CP96 0-5 tachykinin receptor 1 Rattus norvegicus 26-46 7472514-6 1995 Multiple injections of the NK-1 receptor antagonist, CP-96,345, suppressed stimulus-induced Fos expression in gracile nucleus neurons including thalamic relay neurons. CP96 53-58 tachykinin receptor 1 Rattus norvegicus 27-40 7472514-6 1995 Multiple injections of the NK-1 receptor antagonist, CP-96,345, suppressed stimulus-induced Fos expression in gracile nucleus neurons including thalamic relay neurons. CP96 53-58 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 92-95 8545836-7 1995 In mice exposed to acute or multiple injections of the SP antagonist CP-96,345 before DNFB application, ear swelling was depressed (relative to DNFB-treated animals) by 64 and 36% (acute, sc, 10 mg/kg) and 91 and 88% (multiple, ip, cumulative 35 mg/kg) at 0.5 and 1 hr postexposure, respectively. CP96 69-74 tachykinin 1 Mus musculus 55-57 8577379-5 1995 CP-96,345 and WIN 51,708, neurokinin1 receptor antagonists, attenuated the response to substance P, neurokinin A and neurokinin B. CP96 0-5 tachykinin precursor 3 Rattus norvegicus 117-129 7537470-4 1995 The effect of increased microvessel permeability induced by substance P (10(-11) M) was blocked with the nonpeptide substance P receptor antagonist CP-96,345 and NG-nitro-L-arginine methyl ester (L-NAME), an inhibitor of nitric oxide synthase. CP96 148-153 tachykinin precursor 1 Homo sapiens 60-71 7553724-12 1995 The beneficial effects of SP were abolished by an NK-1 receptor antagonist, CP-96,345 (10(-6) M). CP96 76-81 tachykinin receptor 1 Rattus norvegicus 50-63 7537470-4 1995 The effect of increased microvessel permeability induced by substance P (10(-11) M) was blocked with the nonpeptide substance P receptor antagonist CP-96,345 and NG-nitro-L-arginine methyl ester (L-NAME), an inhibitor of nitric oxide synthase. CP96 148-153 tachykinin precursor 1 Homo sapiens 116-127 7532789-3 1995 The presumed contact points for the prototype NK-1 antagonist CP96,345 cluster on opposing faces of the outer portions of transmembrane helices V and VI (refs 1-5). CP96 62-66 tachykinin receptor 1 Homo sapiens 46-50 7539706-9 1995 The increase in reaction time in response to immersion at 55 degrees C was attenuated or blocked by the novel, nonpeptide substance P (NK-1) receptor antagonist, CP-96,345, administered s.c. 30 or 60 min, respectively, prior to paw immersion. CP96 162-167 tachykinin receptor 1 Rattus norvegicus 135-149 7528145-7 1994 These results indicate that sendide and CP-96,345 are selective antagonists of tachykinin NK1 receptors with a long duration of action. CP96 40-45 tachykinin 1 Mus musculus 90-93 7810651-3 1994 The CGRP antagonist, human CGRP-(8-37) [hCGRP-(8-37)], injected intravenously (15 micrograms/kg bolus and 3 micrograms.kg-1.h-1) inhibited by 100, 97, and 73% the gastric hyperemic response to alpha-CGRP, TRH analogue, and bethanechol, respectively, whereas the substance P antagonist CP-96,345 (3 mg/kg iv) had no effect. CP96 285-290 calcitonin related polypeptide alpha Homo sapiens 40-45 7880176-0 1994 [Preparation and characteristics of a tritiated derivative of CP-96,345--a nonpeptide antagonist of the substance P receptor with a high specific radioactivity]. CP96 62-67 substance-P receptor Cavia porcellus 104-124 7530891-10 1994 Furthermore, CP-96,345 is a useful tool in the evaluation of NK1 receptor-mediated responses. CP96 13-18 tachykinin receptor 1 Rattus norvegicus 61-73 7864147-6 1995 Pretreatment with the NK1 receptor antagonist CP-96,345 (4 mg/kg iv), before challenge with substance P, capsaicin, or aerosol hypertonic saline, reduced the amount of neutrophil adhesion by 56%, 93%, and 57% and reduced the amount of eosinophil adhesion by 70%, 83%, and 65%, respectively. CP96 46-51 tachykinin receptor 1 Rattus norvegicus 22-34 7533634-4 1994 These effects were reduced by ionophoretic application of the specific neurokinin-1 receptor antagonist CP96,345 (ejected at 25-80 nA) but not by CP96,344, its inactive enantiomer. CP96 104-108 tachykinin receptor 1 Rattus norvegicus 71-92 7525925-4 1994 The selective NK1 antagonist CP-96,345 (10(-7) M), blocked 6-keto-PGF1 alpha release from substance P (10(-7) M), [Sar9,Met(O2)11]substance P (10(-7) M) and neurokinin A (10(-7) M). CP96 29-34 tachykinin precursor 1 Homo sapiens 157-169 7529387-4 1994 Binding of [3H]SP to mouse spinal cord membranes was inhibited by SP, CP-96,345, and to a lesser extent by SP(5-11), but not SP(1-7), consistent with these binding sites being NK-1 receptors. CP96 70-75 tachykinin 1 Mus musculus 15-17 8556479-7 1994 The stimulatory effect of SP was inhibited by two SP antagonists, spantide ([D-Arg-1-D-Trp-7-D-Trp-7-D-Trp-9-leu-11]-SP) and CP-96,345 (a nonpeptide antagonist of the SP receptor). CP96 125-130 tachykinin precursor 1 Homo sapiens 26-28 8039546-6 1994 Combined pretreatment with the NK1 and NK2 receptor antagonists, CP-96,345 and SR-48968, attenuated the effect of diamide. CP96 65-70 substance-K receptor Cavia porcellus 39-51 7512452-3 1994 The present study was designed to assess the effects of SP receptor blockade by CP-96,945 and its inactive enantiomer CP-96,344 on tissue cytokine levels and in vivo oxidative indexes. CP96 80-85 tachykinin precursor 1 Homo sapiens 56-58 7512452-5 1994 In addition, CP-96,345 significantly reduced (by 53%) the accumulation of tumor necrosis factor-alpha (TNF-alpha) (but not interleukin-1 and interleukin-6) within the lesions; the effect of the enantiomer was insignificant. CP96 13-18 tumor necrosis factor Homo sapiens 74-101 7512452-5 1994 In addition, CP-96,345 significantly reduced (by 53%) the accumulation of tumor necrosis factor-alpha (TNF-alpha) (but not interleukin-1 and interleukin-6) within the lesions; the effect of the enantiomer was insignificant. CP96 13-18 tumor necrosis factor Homo sapiens 103-112 7512452-6 1994 We conclude that treatment with CP-96,345 inhibits SP and TNF-alpha tissue levels in cardiac lesions, indicating a linkage between this neuropeptide and TNF-alpha. CP96 32-37 tumor necrosis factor Homo sapiens 58-67 7512452-6 1994 We conclude that treatment with CP-96,345 inhibits SP and TNF-alpha tissue levels in cardiac lesions, indicating a linkage between this neuropeptide and TNF-alpha. CP96 32-37 tumor necrosis factor Homo sapiens 153-162 7511664-8 1994 This production requires de novo synthesis and is blocked by two different SP-R antagonists, spantide and CP-96,345-1. CP96 106-111 tachykinin precursor 1 Homo sapiens 75-77 7513838-2 1994 Both effects were dose dependent, and completely blocked by CP-96,345 suggesting the involvement of an NK1 receptor. CP96 60-65 tachykinin receptor 1 Homo sapiens 103-115 7512575-8 1994 In addition, the non-peptide NK-1 receptor antagonist, (+/-)CP-96,345, inhibited SP (Ki = 4 nM), but not IL-1-induced IL-6 release. CP96 60-65 tachykinin receptor 1 Homo sapiens 29-42 7512575-8 1994 In addition, the non-peptide NK-1 receptor antagonist, (+/-)CP-96,345, inhibited SP (Ki = 4 nM), but not IL-1-induced IL-6 release. CP96 60-65 tachykinin precursor 1 Homo sapiens 81-83 7518061-6 1994 The selective NK1 receptor antagonist (+/-) CP96 345 (100 nM) reversibly blocked the enhancement of NMDA-evoked depolarization by SPOMe. CP96 44-48 tachykinin receptor 1 Rattus norvegicus 14-26 7519186-0 1994 Ventilatory responses to hypoxia in rats pretreated with nonpeptide NK1 receptor antagonist CP-96,345. CP96 92-97 tachykinin receptor 1 Rattus norvegicus 68-80 7507964-6 1994 Importantly, pretreatment of the BBECs with the tachykinin SP receptor (NK1) antagonist, CP-96,345, significantly reduced the increase in adhesion induced by SP (p < 0.01). CP96 89-94 Antimicrobial peptide NK-lysin-like Bos taurus 72-75 7507964-6 1994 Importantly, pretreatment of the BBECs with the tachykinin SP receptor (NK1) antagonist, CP-96,345, significantly reduced the increase in adhesion induced by SP (p < 0.01). CP96 89-94 tachykinin precursor 1 Bos taurus 59-61 7507964-9 1994 This effect was also mediated by the carboxy end of the molecule and was decreased by CP-96,345, again suggesting that this effect was NK1 mediated. CP96 86-91 Antimicrobial peptide NK-lysin-like Bos taurus 135-138 7505019-17 1993 However, mice treated with CP-96,345 or octreotide (SOM agonist) in vivo produced granulomas that made little or no IgG2a. CP96 27-32 somatostatin Mus musculus 52-55 8170503-6 1994 The NK-1 selective antagonist CP-96,345 (0.3 microM) had a slight stimulant influence on peristalsis, whereas the NK-2 selective antagonists MEN-10,376 (10 microM), GR-94,800 (0.3 microM) and SR-48,968 (0.1 microM) led to a small inhibition of motor activity. CP96 30-35 tachykinin receptor 1 Homo sapiens 4-8 7511108-3 1994 The non-peptide selective NK1 receptor antagonists, RP 67580 and CP-96,345, both inhibited substance P-induced contraction (pKB values 6.7 and 5.7; ED50 = 1.4 and 5.0 mg/kg i.v., respectively) and septide-induced contraction (pKB values 7.5 and 6.5; ED50 = 0.076 and 0.250 mg/kg i.v., respectively). CP96 65-70 tachykinin receptor 1 Rattus norvegicus 26-38 8287060-2 1994 L-703,606 is an iodinated analog of the NK1 antagonist CP-96,345 in which the methoxy group has been replaced by an iodine substituent. CP96 55-60 tachykinin receptor 1 Homo sapiens 40-43 7505019-17 1993 However, mice treated with CP-96,345 or octreotide (SOM agonist) in vivo produced granulomas that made little or no IgG2a. CP96 27-32 immunoglobulin heavy variable V1-9 Mus musculus 116-121 7902193-9 1993 The simultaneous application of D-AP5 (20 microM) with either MEN,10376 (100 nM) or CP-96,345 (500 nM) together produced a reduction in the area of the evoked VRP which was comparable to the value obtained by addition of their individual effects. CP96 84-89 eukaryotic translation initiation factor 4 gamma 2 Homo sapiens 32-37 7692775-2 1993 SR 48968 (0.3 mumol/kg) and CP-96,345 (2 mumol/kg) given intravenously completely blocked the response to the selective NK2 receptor agonist [beta Ala8]neurokinin A(4-10) and NK1 receptor agonist [Sar9,Met(O2)11]substance P, respectively. CP96 28-33 substance-K receptor Cavia porcellus 120-132 7507164-5 1993 The results indicate that in guinea-pig isolated airway smooth muscle CP-96,345 can non-selectively inhibit neurogenic responses probably via neurokinin-1 receptor-dependent and independent mechanisms. CP96 70-75 substance-P receptor Cavia porcellus 142-163 7692775-2 1993 SR 48968 (0.3 mumol/kg) and CP-96,345 (2 mumol/kg) given intravenously completely blocked the response to the selective NK2 receptor agonist [beta Ala8]neurokinin A(4-10) and NK1 receptor agonist [Sar9,Met(O2)11]substance P, respectively. CP96 28-33 substance-P receptor Cavia porcellus 175-187 8117379-1 1993 Molecular modeling studies based on the potent NK-1 antagonist CP-96,345 led us to the identification of some 2-benzylidene- and 2-benzyl-3-benzylaminoquinuclidine derivatives as potential antagonists at the NK receptor subtypes. CP96 63-68 tachykinin receptor 1 Homo sapiens 47-51 8117379-1 1993 Molecular modeling studies based on the potent NK-1 antagonist CP-96,345 led us to the identification of some 2-benzylidene- and 2-benzyl-3-benzylaminoquinuclidine derivatives as potential antagonists at the NK receptor subtypes. CP96 63-68 killer cell immunoglobulin like receptor, three Ig domains and long cytoplasmic tail 1 Homo sapiens 208-219 7694765-8 1993 The effect of SP on ACh release is probably mediated via NK-1 receptors since ACh release in response to SP was reduced in a dose dependent manner by the NK-1 receptor antagonists CP-96,345 and RP-67580. CP96 180-185 tachykinin receptor 1 Rattus norvegicus 57-70 7692490-0 1993 Discovery of CP-96,345 and its characterization in disease models involving substance P. CP96 13-18 tachykinin precursor 1 Homo sapiens 76-87 7693493-3 1993 Substance P-mediated dyspnea and significant respiratory events were inhibited by the NK1 receptor antagonist, CP-96,345. CP96 111-116 substance-P receptor Cavia porcellus 86-98 7693284-0 1993 The interaction of the NK1 receptor antagonist CP-96,345 with L-type calcium channels and its functional consequences. CP96 47-52 tachykinin receptor 1 Rattus norvegicus 23-35 7693284-17 1993 The results indicate that in addition to possessing affinity for the NK1 receptor, the non-peptide antagonist, CP-96,345, displays high affinity for [3H]-diltiazem binding sites on L-type calcium channels.The functional effect that may be observed in integrated models will be a consequence of either property, or be a composite effect of NK1 receptor antagonism and L-channel blockade. CP96 111-116 tachykinin receptor 1 Rattus norvegicus 69-81 7693284-17 1993 The results indicate that in addition to possessing affinity for the NK1 receptor, the non-peptide antagonist, CP-96,345, displays high affinity for [3H]-diltiazem binding sites on L-type calcium channels.The functional effect that may be observed in integrated models will be a consequence of either property, or be a composite effect of NK1 receptor antagonism and L-channel blockade. CP96 111-116 tachykinin receptor 1 Rattus norvegicus 339-351 8394992-10 1993 Competition experiments with agonists also demonstrated binding to high and low affinity states, with the following order of potency: NKA > [Nle10]NKA(4-10) > [beta-Ala8]NKA(4-10) >> substance P; Senktide and the NK-1 antagonist CP96,345 (10 microM) did not inhibit binding. CP96 241-245 tachykinin precursor 1 Homo sapiens 134-137 8394992-10 1993 Competition experiments with agonists also demonstrated binding to high and low affinity states, with the following order of potency: NKA > [Nle10]NKA(4-10) > [beta-Ala8]NKA(4-10) >> substance P; Senktide and the NK-1 antagonist CP96,345 (10 microM) did not inhibit binding. CP96 241-245 tachykinin precursor 1 Homo sapiens 150-153 8394992-10 1993 Competition experiments with agonists also demonstrated binding to high and low affinity states, with the following order of potency: NKA > [Nle10]NKA(4-10) > [beta-Ala8]NKA(4-10) >> substance P; Senktide and the NK-1 antagonist CP96,345 (10 microM) did not inhibit binding. CP96 241-245 tachykinin precursor 1 Homo sapiens 150-153 7692520-0 1993 Role of NK-1 receptor in central cardiovascular regulation in rats: studies on a novel non-peptide antagonist, CP-96,345, of substance P NK-1 receptor. CP96 111-116 tachykinin receptor 1 Rattus norvegicus 137-150 7692533-0 1993 Different behavioral profiles of the non-peptide substance P (NK-1) antagonists CP-96,345 and RP 67580. CP96 80-85 tachykinin precursor 1 Homo sapiens 49-60 7692490-1 1993 Studies with CP-96,345, a potent, selective, orally active, nonpeptide NK1 receptor antagonist, have provided considerable insight into SP pharmacology. CP96 13-18 tachykinin receptor 1 Homo sapiens 71-83 7692533-0 1993 Different behavioral profiles of the non-peptide substance P (NK-1) antagonists CP-96,345 and RP 67580. CP96 80-85 tachykinin receptor 1 Homo sapiens 62-66 7692512-0 1993 Selective blockade of sensory response of the carotid body to hypoxia by NK-1 receptor antagonist CP-96,345. CP96 98-103 tachykinin receptor 1 Homo sapiens 73-86 7692558-0 1993 Is the selective non-peptide NK-1 receptor antagonist CP96,345 a peripherally acting analgesic? CP96 54-58 tachykinin receptor 1 Homo sapiens 29-42 7686934-13 1993 Moreover, animals treated in vivo with the NK-1 receptor antagonist CP-96,345 produced smaller granulomas. CP96 68-73 tachykinin receptor 1 Mus musculus 43-56 7687062-5 1993 At the same time the affinity for the NK1-selective compound CP-96,345 decreased > 30-fold. CP96 61-66 tachykinin receptor 1 Homo sapiens 38-41 7683033-4 1993 Autoradiographic ligand binding to human umbilical cord sections demonstrates the presence of SP binding sites with characteristics of the neurokinin 1 (NK-1) receptor (displacement by GTP analogues and the NK-1 specific antagonist CP-96,345) on human umbilical arterial, but not venous, endothelium. CP96 232-237 tachykinin receptor 1 Homo sapiens 153-167 8393002-6 1993 The mechanism of extravasation also varied with the mode of bradykinin delivery: when bradykinin was instilled locally in the nose, the selective neurokinin 1 (NK1) receptor antagonist CP-96,345 markedly inhibited the response, whereas it had no effect on Evans blue extravasation when bradykinin was injected intravenously. CP96 185-190 tachykinin receptor 1 Rattus norvegicus 146-173 7683033-4 1993 Autoradiographic ligand binding to human umbilical cord sections demonstrates the presence of SP binding sites with characteristics of the neurokinin 1 (NK-1) receptor (displacement by GTP analogues and the NK-1 specific antagonist CP-96,345) on human umbilical arterial, but not venous, endothelium. CP96 232-237 tachykinin precursor 1 Homo sapiens 153-157 7682312-0 1993 Different behavioral profiles of the non-peptide substance P (NK1) antagonists CP-96,345 and RP 67580 in Swiss albino mice in the black-and-white box. CP96 79-84 tachykinin 1 Mus musculus 62-65 7683436-8 1993 Also the contraction caused by the NK2 receptor agonist was inhibited competitively by (+/-) CP-96,345 with a pA2 value of 5.7, supporting the view that the two agonists (Sar9,Met(O2)11)SP and (Nle10)NKA(4-10) interact with the same receptor. CP96 93-98 substance-K receptor Oryctolagus cuniculus 35-47 7686104-2 1993 This effect was blocked by the specific tachykinin antagonists CP-96,345, which acts at the NK1 receptor, and Men 10207, which acts at the NK2 receptor. CP96 63-68 tachykinin receptor 1 Homo sapiens 92-104 1383834-4 1992 The inhibition by (+/-)CP-96,345 of contractions evoked by neurokinin B and by bradykinin (pIC50 6.1 and 4.9, respectively) was attributed to unspecific effects of the antagonist. CP96 23-28 tachykinin-3 Cavia porcellus 59-71 7679096-0 1993 Molecular basis for the species selectivity of the substance P antagonist CP-96,345. CP96 74-79 tachykinin precursor 1 Homo sapiens 51-62 7679096-1 1993 The non-peptide substance P (SP) antagonist CP-96,345 has a 90-fold selectivity for the human neurokinin-1 (NK-1) or SP receptor over the rat NK-1 receptor, while the agonist SP shows no such selectivity. CP96 44-49 tachykinin precursor 1 Homo sapiens 16-27 7679096-1 1993 The non-peptide substance P (SP) antagonist CP-96,345 has a 90-fold selectivity for the human neurokinin-1 (NK-1) or SP receptor over the rat NK-1 receptor, while the agonist SP shows no such selectivity. CP96 44-49 tachykinin precursor 1 Homo sapiens 29-31 7679096-1 1993 The non-peptide substance P (SP) antagonist CP-96,345 has a 90-fold selectivity for the human neurokinin-1 (NK-1) or SP receptor over the rat NK-1 receptor, while the agonist SP shows no such selectivity. CP96 44-49 tachykinin precursor 1 Homo sapiens 94-106 7679096-1 1993 The non-peptide substance P (SP) antagonist CP-96,345 has a 90-fold selectivity for the human neurokinin-1 (NK-1) or SP receptor over the rat NK-1 receptor, while the agonist SP shows no such selectivity. CP96 44-49 tachykinin precursor 1 Homo sapiens 108-112 7679096-1 1993 The non-peptide substance P (SP) antagonist CP-96,345 has a 90-fold selectivity for the human neurokinin-1 (NK-1) or SP receptor over the rat NK-1 receptor, while the agonist SP shows no such selectivity. CP96 44-49 tachykinin receptor 1 Rattus norvegicus 142-155 7680798-6 1993 Responses to substance P methyl ester and GR73 632 were selectively reduced by the neurokinin-1 receptor antagonist CP96,345, and responses to neurokinin-A were completely blocked by the neurokinin-2 receptor antagonist MEN10 376. CP96 116-120 tachykinin receptor 1 Rattus norvegicus 83-104 7679031-0 1993 Non-peptide antagonists, CP-96,345 and RP 67580, distinguish species variants in tachykinin NK1 receptors. CP96 25-30 tachykinin receptor 1 Homo sapiens 92-95 7679031-2 1993 The potency of the non-peptide antagonists CP-96,345 and RP 67580 on NK1 receptor-stimulated [3H]-inositol phosphate accumulation in cell lines or tissue from three different species has been examined. CP96 43-48 tachykinin receptor 1 Homo sapiens 69-81 7679031-9 1993 In conclusion, we have demonstrated that previously reported species differences in binding affinities for the non-peptide NK1 antagonists, CP-96,345 and RP 67580, are also observed in inhibition of NK1 receptor stimulated hydrolysis of inositol phospholipids. CP96 140-145 tachykinin receptor 1 Homo sapiens 123-126 7679031-9 1993 In conclusion, we have demonstrated that previously reported species differences in binding affinities for the non-peptide NK1 antagonists, CP-96,345 and RP 67580, are also observed in inhibition of NK1 receptor stimulated hydrolysis of inositol phospholipids. CP96 140-145 tachykinin receptor 1 Homo sapiens 199-211 7680128-6 1993 Remarkably the nonpeptide substance P antagonists R 30732 (10 microM), R 32602 (10 microM), and CP-96,345 (10 microM) showed a similar inhibition of PRL release and a stimulation of GH release. CP96 96-101 prolactin Rattus norvegicus 149-152 1280591-1 1992 The effects of the non-peptide NK1 receptor antagonist, CP-96,345, on cardiovascular homeostasis were investigated in conscious and anaesthetized rats in vivo and on heart function and muscle tonicity of vessels in vitro. CP96 56-61 tachykinin receptor 1 Rattus norvegicus 31-43 1280591-8 1992 As only the enantiomer with NK1 antagonistic activity inhibited cigarette smoke-induced plasma protein extravasation in rat trachea, CP-96,345 remains a useful tool for elucidating NK1 receptor-mediated responses, provided CP-96,344 is included as control. CP96 133-138 tachykinin receptor 1 Rattus norvegicus 181-193 1385177-0 1992 The substance P receptor antagonist CP-96,345 interacts with Ca2+ channels. CP96 36-41 tachykinin receptor 1 Homo sapiens 4-24 1385177-1 1992 The nonpeptide substance P receptor antagonist CP-96,345 was found to displace binding to Ca2+ channel binding sites labelled with either [3H]desmethoxyverapamil or [3H]diltiazem and to enhance [3H]nitrendipine binding. CP96 47-52 tachykinin receptor 1 Homo sapiens 15-35 1385177-3 1992 It is concluded that CP-96,345 may act as an antagonist of L-type Ca2+ channels in addition to being a potent NK1 receptor (substance P) antagonist. CP96 21-26 tachykinin receptor 1 Homo sapiens 110-122 1385177-3 1992 It is concluded that CP-96,345 may act as an antagonist of L-type Ca2+ channels in addition to being a potent NK1 receptor (substance P) antagonist. CP96 21-26 tachykinin precursor 1 Homo sapiens 124-135 8384427-0 1993 Effects of the substance P receptor antagonist CP-96,345 on renal sensory receptor activation. CP96 47-52 tachykinin receptor 1 Rattus norvegicus 15-35 7680318-1 1993 We have investigated the effect of a new non-peptide NK1 receptor antagonist, CP-96,345, against substance P (SP)-, bradykinin (BK)- and allergen-induced airway microvascular leakage, bronchoconstriction and hypotension in anesthetized guinea pigs. CP96 78-83 substance-P receptor Cavia porcellus 53-65 7678436-3 1993 However, a recently developed non-peptide SP antagonist, CP-96,345, is specific for the NK-1 receptor. CP96 57-62 tachykinin receptor 1 Rattus norvegicus 88-101 1385160-2 1992 administered CP-96,345, a non-peptide NK1 receptor ligand, on the spinal nociceptive flexor reflex and on the facilitation of this reflex evoked by i.t. CP96 13-18 tachykinin receptor 1 Rattus norvegicus 38-50 1330589-1 1992 CP-96,345, a potent non-peptide antagonist of the substance P (SP) receptor, inhibited SP-, neurokinin A (NKA)- and neurokinin B-induced plasma extravasation in guinea pig dorsal skin. CP96 0-5 substance-P receptor Cavia porcellus 50-75 1330589-1 1992 CP-96,345, a potent non-peptide antagonist of the substance P (SP) receptor, inhibited SP-, neurokinin A (NKA)- and neurokinin B-induced plasma extravasation in guinea pig dorsal skin. CP96 0-5 tachykinin-3 Cavia porcellus 116-128 1378901-1 1992 We describe the structure-activity relationship development of a series of quinuclidines which culminated in the first potent, selective, nonpeptide substance P (SP) antagonist, (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxy-phenyl)methyl]-1- azabicyclo[2.2.2]octan-3-amine, 3 (CP-96,345). CP96 276-281 tachykinin precursor 1 Homo sapiens 149-160 1378901-1 1992 We describe the structure-activity relationship development of a series of quinuclidines which culminated in the first potent, selective, nonpeptide substance P (SP) antagonist, (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxy-phenyl)methyl]-1- azabicyclo[2.2.2]octan-3-amine, 3 (CP-96,345). CP96 276-281 tachykinin precursor 1 Homo sapiens 162-164 1328962-0 1992 Role of NK-1 receptor in central cardiovascular regulation in rats: studies on a novel non-peptide antagonist, CP-96,345, of substance P NK-1 receptor. CP96 111-116 tachykinin receptor 1 Rattus norvegicus 137-150 1279753-7 1992 CP-96,345 (5 microM), a nonpeptide NK-1 antagonist, and the peptide NK-1 antagonist, GR82334 (1 microM), reduced the secretory response to substance P (50 nM) in the presence and absence of tetrodotoxin (0.2 microM). CP96 0-5 tachykinin precursor 1 Homo sapiens 139-150 1378274-1 1992 CP-96,345 [(2S, 3S) cis-2-(diphenylmethyl)-N-((2-methoxyphenyl)-methyl)-1- azabicyclo[2.2.2]octan-3-amine] belongs to a new class of nonpeptide antagonists of the substance P (SP) receptor. CP96 0-5 tachykinin receptor 1 Homo sapiens 163-188 1378274-4 1992 The CP-96,345-induced inhibition of [Ca2+]i responses to SP appeared reversible after withdrawal of the antagonist and was overcome by increasing the concentration of the agonist. CP96 4-9 tachykinin precursor 1 Homo sapiens 57-59 1378274-5 1992 CP-96,345 was consequently a specific and potent competitive antagonist for SP receptors on pancreatic acinar cells. CP96 0-5 tachykinin precursor 1 Homo sapiens 76-78 1319017-0 1992 NK-1, but not NK-2, tachykinin receptors mediate plasma extravasation induced by antidromic C-fiber stimulation in rat hindpaw: demonstrated with the NK-1 antagonist CP-96,345 and the NK-2 antagonist Men 10207. CP96 166-171 tachykinin receptor 1 Homo sapiens 0-4 1319017-4 1992 Plasma extravasation induced by intravenously injected substance P was also inhibited by CP-96,345. CP96 89-94 tachykinin precursor 1 Homo sapiens 55-66 1319017-5 1992 Since CP-96,345 is a highly selective antagonist for NK-1 tachykinin receptors, it is suggested that the plasma extravasation induced by antidromic C-fiber stimulation and by systemically applied tachykinins is mediated by NK-1 tachykinin receptors. CP96 6-11 tachykinin receptor 1 Homo sapiens 53-57 1319017-5 1992 Since CP-96,345 is a highly selective antagonist for NK-1 tachykinin receptors, it is suggested that the plasma extravasation induced by antidromic C-fiber stimulation and by systemically applied tachykinins is mediated by NK-1 tachykinin receptors. CP96 6-11 tachykinin receptor 1 Homo sapiens 223-227 1548463-9 1992 The results of this study suggest that [3H]CP-96,501 is a useful agonist radioligand for the 5-HT1B receptor. CP96 43-48 5-hydroxytryptamine receptor 1B Rattus norvegicus 93-99 1548463-1 1992 3-(1,2,5,6-Tetrahydro-4-pyridyl)-5-n-propoxyindole (CP-96,501) was found to be more selective ligand at the serotonin 5-HT1B receptor than the commonly used 5-HT1B agonist, 3-(1,2,5,6-tetrahydro-4-pyridyl)-5-methoxyindole (RU 24969). CP96 52-57 5-hydroxytryptamine receptor 1B Rattus norvegicus 118-124 1373095-0 1992 Inhibition of neurogenic plasma exudation in guinea-pig airways by CP-96,345, a new non-peptide NK1 receptor antagonist. CP96 67-72 substance-P receptor Cavia porcellus 96-108 1548463-1 1992 3-(1,2,5,6-Tetrahydro-4-pyridyl)-5-n-propoxyindole (CP-96,501) was found to be more selective ligand at the serotonin 5-HT1B receptor than the commonly used 5-HT1B agonist, 3-(1,2,5,6-tetrahydro-4-pyridyl)-5-methoxyindole (RU 24969). CP96 52-57 5-hydroxytryptamine receptor 1B Rattus norvegicus 157-163 1328736-1 1992 CP-96,345, a novel non-peptide antagonist of the NK1 receptor, at 10(-8)-10(-6) M decreased the frequency of peristalsis and reduced peristalsis-associated longitudinal muscle contractions in isolated guinea pig ileum. CP96 0-5 substance-P receptor Cavia porcellus 49-61 1665790-0 1991 Cigarette smoke-induced airway oedema is blocked by the NK1 antagonist, CP-96,345. CP96 72-77 tachykinin receptor 1 Homo sapiens 56-59 1665729-0 1991 Investigation into species variants in tachykinin NK1 receptors by use of the non-peptide antagonist, CP-96,345. CP96 102-107 tachykinin receptor 1 Homo sapiens 50-53 1665729-1 1991 The affinity of the non-peptide antagonist CP-96,345 for tachykinin NK1 receptors has been estimated in a range of species by use of both radioligand binding and functional assays. CP96 43-48 tachykinin receptor 1 Homo sapiens 68-71 1665729-2 1991 CP-96,345 was 30-120 fold less active at NK1 receptors in rat and mouse than in the other species examined, including man. CP96 0-5 tachykinin receptor 1 Homo sapiens 41-44 1712587-1 1991 CP-96,345, a quinuclidine, is a potent inhibitor of substance P for the NK1 receptor of bovine brain, but has reduced potency for the corresponding receptor of the rat and mouse, and none for NK2 or NK3 receptors. CP96 0-5 tachykinin precursor 1 Bos taurus 52-63 1722327-2 1991 Here, we present evidence that CP-96,345, a specific substance P (NK-1) receptor antagonist, selectively blocks a slow, prolonged excitatory postsynaptic potential following noxious cutaneous stimulation or a train of intense electrical stimuli to sensory nerves but does not affect the response to innocuous input or the brief response to single electrical stimuli to C fibers. CP96 31-36 tachykinin precursor 1 Homo sapiens 53-64 1722327-2 1991 Here, we present evidence that CP-96,345, a specific substance P (NK-1) receptor antagonist, selectively blocks a slow, prolonged excitatory postsynaptic potential following noxious cutaneous stimulation or a train of intense electrical stimuli to sensory nerves but does not affect the response to innocuous input or the brief response to single electrical stimuli to C fibers. CP96 31-36 tachykinin receptor 1 Homo sapiens 66-80 1703323-1 1991 CP-96,345 [(2S, 3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)- methyl]-1-azabicyclo[2.2.2]octan-3-amine] is a potent nonpeptide antagonist of the substance P (NK1) receptor. CP96 0-5 tachykinin receptor 1 Rattus norvegicus 161-174 1721102-1 1991 CP-96,345 has been identified as being a highly selective, nonpeptidic agent with subnanomolar affinity for the NK1 receptor. CP96 0-5 tachykinin receptor 1 Rattus norvegicus 112-124