在小鼠离体输精管中，西格玛[校正后]配体利米卡唑拮抗（+）SKF 10,047，但不拮抗（+）3 - PPP。

The sigma [corrected] ligand rimcazole antagonises (+)SKF 10,047, but not (+)3-PPP, in the mouse isolated vas deferens.

作者信息

Kennedy C, Jarvis G E, Henderson G

机构信息

Department of Pharmacology, University of Cambridge, U.K.

出版信息

Eur J Pharmacol. 1990 Jun 8;181(3):315-8. doi: 10.1016/0014-2999(90)90097-p.

DOI:10.1016/0014-2999(90)90097-p

PMID:1974518

Abstract

We have characterized the actions of several sigma receptor ligands on the electrically evoked, neurogenic contractions of the mouse isolated vas deferens. (-)SKF 10,047 was significantly more potent than (+)SKF 10,047 in potentiating twitch contractions and was equipotent with (+)3-PPP. Rimcazole (1 and 3 microM) antagonised the potentiation induced by 100 microM (+)SKF 10,047 and, to a lesser extent, that induced by 30 microM (-)SKF 10,047 but increased that elicited by (+)3-PPP (30 microM). This apparent contradiction may arise from sigma agonists acting in this tissue at both sigma and non-sigma sites.

摘要

我们已对几种σ受体配体对小鼠离体输精管电诱发的神经源性收缩的作用进行了表征。（-）SKF 10,047在增强抽搐收缩方面比（+）SKF 10,047显著更有效，且与（+）3-PPP等效。利咪唑（1和3 microM）拮抗由100 microM（+）SKF 10,047诱导的增强作用，并在较小程度上拮抗由30 microM（-）SKF 10,047诱导的增强作用，但增加了由30 microM（+）3-PPP引起的增强作用。这种明显的矛盾可能源于σ激动剂在该组织中的σ和非σ位点均起作用。