代谢型P2Y1受体抑制大鼠背根神经节神经元中的P2X3受体通道。

Metabotropic P2Y1 receptors inhibit P2X3 receptor-channels in rat dorsal root ganglion neurons.

作者信息

Gerevich Zoltan, Müller Christoph, Illes Peter

机构信息

Rudolf-Boehm-Institute of Pharmacology and Toxicology, University of Leipzig, Haertelstrasse 16-18, D-04107 Leipzig, Germany.

出版信息

Eur J Pharmacol. 2005 Oct 3;521(1-3):34-8. doi: 10.1016/j.ejphar.2005.08.001. Epub 2005 Sep 19.

DOI:10.1016/j.ejphar.2005.08.001

PMID:16181623

Abstract

Whole-cell patch-clamp recordings from cultured rat dorsal root ganglion neurons demonstrated that the P2Y1 receptor agonists adenosine 5'-O-2-thiodiphosphate (ADP-beta-S) and 2-methylthio adenosine 5'-diphosphate (2-MeSADP) inhibit the alpha,beta-methylene adenosine 5'-triphosphate (alpha,beta-meATP)-induced P2X3 receptor-currents. This effect could be antagonized by the wide-spectrum G protein blocker GDP-beta-S and the P2Y(1) receptor antagonist MRS 2179. The P2Y12,13 receptor antagonist AR-C6993MX and pertussis toxin, a blocker of Galphai/o, did not interact with the effect of ADP-beta-S. Hence, the results indicate that ADP-sensitive P2Y1 receptors of rat dorsal root ganglion neurons inhibit ionotropic P2X3 receptors via G protein-activation.

摘要

来自培养的大鼠背根神经节神经元的全细胞膜片钳记录表明，P2Y1受体激动剂5'-O-2-硫代二磷酸腺苷（ADP-β-S）和2-甲硫基腺苷5'-二磷酸（2-MeSADP）抑制α,β-亚甲基腺苷5'-三磷酸（α,β-meATP）诱导的P2X3受体电流。这种效应可被广谱G蛋白阻滞剂GDP-β-S和P2Y(1)受体拮抗剂MRS 2179拮抗。P2Y12,13受体拮抗剂AR-C6993MX和百日咳毒素（一种Gαi/o阻滞剂）与ADP-β-S的效应无相互作用。因此，结果表明大鼠背根神经节神经元的ADP敏感型P2Y1受体通过G蛋白激活抑制离子型P2X3受体。