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Involvement of sigma-receptors in the increase in contraction of mouse vas deferens induced by exogenous ATP.

作者信息

Matsuno K, Kobayashi T, Mita S

机构信息

Central Research Laboratories, Santen Pharmaceutical Co., Ltd., Osaka, Japan.

出版信息

J Pharm Pharmacol. 1996 Jan;48(1):96-9. doi: 10.1111/j.2042-7158.1996.tb05885.x.

Abstract

The effects of sigma-receptor ligands on the twitch contraction elicited by the exogenous application of adenosine 5'-triphosphate (ATP) in the unstimulated mouse vas deferens were studied. (-)-Pentazocine, 1,3-di(2-tolyl)guanidine(DTG) and two pairs of optical isomers of 3-(3-hydroxyphenyl)-N-(1-propyl)piperidine(3-PPP) and N-allylnormetazocine (SKF-10,047) potentiated the exogenous application of ATP-induced twitch-type contraction in a concentration-dependent manner, while (+)-pentazocine did not affect it. The order of potentiating ability was: (+)-3-PPP > (-)pentazocine > (-)-SKF-10,047> DTG > (-)-3-PPP > (+)-SKF-10,047. On the other hand, haloperidol and rimcazole, putataive sigma-receptor antagonists, suppressed this twitch contraction. In addition, these antagonists significantly blocked the (+)-3-PPP- and (-)-pentazocine-induced potentiation at concentrations which did not affect contractions per se. These findings indicate that the exogenous application of ATP-induced twitch contraction in the mouse vas deferens is regulated by sigma-receptors. In addition, the present ranking order suggests that the sigma-receptor potentiating the ATP-induced twitch contraction at post-junctional sites may differ from the sigma 1- and/or sigma 2-receptor subtypes.

摘要

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