A STUDY OF PROSTACYCLIN MIMETICS DISTINGUISHES NEURONAL FROM NEUTROPHIL IP RECEPTORS

被引：21

作者：

WISE, H

QIAN, YM

JONES, RL

机构：

[1] Department of Pharmacology, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, N.T.

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1995年 / 278卷 / 03期

关键词：

PROSTACYCLIN RECEPTOR; CICAPROST; NONPROSTANOID PROSTACYCLIN MIMETIC; NEUTROPHIL; RAT; COLON;

D O I：

10.1016/0014-2999(95)00173-I

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The prostacyclin mimetics BMY 45778 (3-[4-(4,5-diphenyl-2-oxazolyl)-5-oxazolyl]phenoxy]acetic acid), BMY 42393 (2-[3-[2-(4,5-diphenyl-2-oxazolyl)ethyl]phenoxy]acetic acid) and EP 185 (rac 5-endo-(6'-carboxyhex-2'Z-enyl)-6-exo-(p-methoxyphenyl-methylazino)-bicyclo[2.2.2]oct-2-ene) inhibited rat neutrophil aggregation stimulated by N-formyl-methionyl-leucyl phenylalanine (IC50=20, 462, and 1195 nM respectively). In contrast only BMY 45778 (1-10 mu M) produced any significant inhibition (10-20%) of the spontaneous activity of rat colon. BMY 45778 (10 mu M) also attenuated the inhibitory effect of the prostacyclin analogue cicaprost on rat colon, whereas BMY 42393 and EP 185 did not. BMY 45778 appears to be a low affinity partial agonist at prostacyclin receptors on rat colon and its low potency in rat colon compared with rat neutrophils suggests the presence of a different prostacyclin receptor located on enteric neurones.

引用

页码：265 / 269

页数：5

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