DIFFERENTIAL-EFFECTS OF BQ-123 AGAINST ENDOTHELIN-1 AND ENDOTHELIN-3 ON THE RAT VAS-DEFERENS - EVIDENCE FOR AN ATYPICAL ENDOTHELIN RECEPTOR

被引：34
作者：
EGLEZOS, A
CUCCHI, P
PATACCHINI, R
QUARTARA, L
MAGGI, CA
MIZRAHI, J
机构：
[1] LAB GUIDOTTI SPA,DEPT PHARMACOL,I-5612 PISA,ITALY
[2] A MENARINI PHARMACEUT SRL,DEPT PHARMACOL,FLORENCE,ITALY
来源：
BRITISH JOURNAL OF PHARMACOLOGY | 1993年 / 109卷 / 03期
关键词：
ENDOTHELIN-1; ENDOTHELIN-3; RECEPTOR SUBTYPES; BQ-123; SARAFOTOXIN S6C; RAT VAS DEFERENS;
D O I：
10.1111/j.1476-5381.1993.tb13635.x
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
1 Endothelin-1 and endothelin-3 enhanced concentration-dependently the rat vas deferens twitch response to electrical stimulation, endothelin-1 being three times more potent. Sarafotoxin S6c was at least 200 times less active than endothelin-1. 2 The response to endothelin was antagonized in a competitive manner by the supposedly selective ET(A) receptor antagonist, BQ-123 (pA2:7.0 +/- 0.1). In contrast, the endothelin-1 concentration-response curve was only shifted two fold in the presence of 10 mum BQ-123, while no effect was observed at 1 muM. 3 This evidence suggests the rat vas deferens contains an endothelin receptor not conforming to the ET(A)/ET(B) receptor subtype classification so far proposed.
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收藏
页码：736 / 738
页数：3
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