Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 박혜영 | * |
dc.contributor.author | 김화정 | * |
dc.date.accessioned | 2018-05-30T08:14:23Z | - |
dc.date.available | 2018-05-30T08:14:23Z | - |
dc.date.issued | 2005 | * |
dc.identifier.issn | 0014-2999 | * |
dc.identifier.other | OAK-3008 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/243626 | - |
dc.description.abstract | Two novel compounds, N-phenylacetyl-N′-(4-methoxybenzyl)-N″-1- (4-chlorobenzhydryl)piperazine iminodiacetic acid triamide (compound I) and N-phenylacetyl-N′-(4-methylbenzyl)-N″-1-(4-chlorobenzhydryl) piperazine iminodiacetic acid triamide (compound II), designed and synthesized as novel non-peptide bradykinin B2 receptor antagonists, were studied for their functional activities in isolated guinea-pig ileum smooth muscle. These compounds were compared with the conventional peptide bradykinin B 2 receptor antagonist, icatibant (H-dArg-Arg-Pro-Hyp-Gly-Thi-Ser- dTic-Oic-Arg-OH) for their in vitro functional activities. Compounds I and II showed highly potent, time-dependent insurmountable antagonism against contractile responses to bradykinin (pKB 8.80 and 8.57, respectively) with progressive reduction of maximum effect maintaining the concentration producing half maximal-response unchanged. Otherwise, icatibant, known as a non-competitive antagonist, showed a rightward displacement of cumulative concentration-response curves to bradykinin with decrease of its maximum effect (pKB 8.73). The IC50 values of compounds I and II were 3.56 × 10- 8 and 6.30 × 10- 8 M, respectively, while that of icatibant was 5.02 × 10- 8 M. The profile of action of compounds I and II varied when contact time was prolonged from 5 to 60 min, whereas that of icatibant did not. The inhibitory effects of the newly synthesized compounds and icatibant on the contractile response to bradykinin were differently reverted by washout (icatibant < 100 min, compounds I and II > 100 min). This class of compounds containing the chlorobenzhydryl piperazine moiety is expected to be a novel non-peptide bradykinin B2 receptor antagonists. © 2005 Elsevier B.V. All rights reserved. | * |
dc.language | English | * |
dc.title | Antagonistic effects of novel non-peptide chlorobenzhydryl piperazine compounds on contractile response to bradykinin in the guinea-pig ileum | * |
dc.type | Article | * |
dc.relation.issue | 41277 | * |
dc.relation.volume | 523 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 143 | * |
dc.relation.lastpage | 150 | * |
dc.relation.journaltitle | European Journal of Pharmacology | * |
dc.identifier.doi | 10.1016/j.ejphar.2005.09.010 | * |
dc.identifier.wosid | WOS:000233298300019 | * |
dc.identifier.scopusid | 2-s2.0-27644488282 | * |
dc.author.google | Yoo L.K. | * |
dc.author.google | Jai Y.R. | * |
dc.author.google | Kim H.-J. | * |
dc.author.google | Hea-Young P.C. | * |
dc.contributor.scopusid | 박혜영(34972649500;57200273796) | * |
dc.contributor.scopusid | 김화정(56670336100) | * |
dc.date.modifydate | 20240118124308 | * |