ANTAGONISM OF LEUKOTRIENE RESPONSES IN HUMAN AIRWAYS BY BAY X7195

被引：7

作者：

GORENNE, I

ORTIZ, JL

LABAT, C

ABRAM, T

TUDHOP, S

CUTHBERT, N

NORMAN, P

GARDINER, P

MORCILLO, E

BRINK, C

机构：

[1] CTR CHIRURG MARIE LANNELONGUE,CNRS,URA 1159,F-92350 LE PLESSIS ROBINS,FRANCE

[2] BAYER PLC,RES DEPT,PHARMACEUT BUSINESS GRP,STOKE POGES SL2 4LY,BUCKS,ENGLAND

[3] UNIV VALENCIA,DEPT FARMACOL,E-46100 VALENCIA,SPAIN

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1995年 / 275卷 / 02期

关键词：

AIRWAY HUMAN; LEUKOTRIENE; ANTIIMMUNOGLOBULIN E; CONTRACTION; CYSTEINYL LEUKOTRIENE RECEPTOR ANTAGONIST;

D O I：

10.1016/0014-2999(94)00777-5

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Contractions induced by leukotriene and anti-IgE (sheep antiserum to human IgE) were antagonized by pretreatment of human airways with the cysteinyl leukotriene receptor antagonist BAY x7195 ((4S)-[4-carboxyphenylthio]-7-[4-(4-phenoxybutoxy)-phenyl]-hept-5-(z)-enoic acid). However, this receptor antagonist did not inhibit either leukotriene D-4- or leukotriene C-4-induced contractions in human pulmonary veins. The pA(2) value for BAY x7195 in human airways against leukotriene D-4 was 7.83 +/- 0.16 with a slope of 1.07 +/- 0.15 (means +/- S.E.M; n = 11). The IC50 value for BAY x7195 in human airways contracted with anti-IgE was 0.31 +/- 0.08 mu M (n = 11). These results were comparable to those obtained with ICI 204,219 (4-(5-cyclopentyl-oxycarbonylamino-1-methylindol-3-ylmethyl)-3-methoxy-N-otolyl-sulfonylbenzamide). These data demonstrate that BAY x7195 is a potent selective leukotriene receptor antagonist which may block allergic reactions in the lung.

引用

页码：207 / 212

页数：6

共 22 条

[1] THE EFFECT OF AN ORAL LEUKOTRIENE ANTAGONIST L-649,923 ON HISTAMINE AND LEUKOTRIENE-D4-INDUCED BRONCHOCONSTRICTION IN NORMAL MAN [J].