[(3)H]哌唑嗪与大鼠肾膜中α(1A)-和α(1B)-肾上腺素能受体以及西咪替丁敏感的非α(1)结合位点的结合。

Binding of [(3)H]prazosin to alpha(1A)- and alpha(1B)-adrenoceptors, and to a cimetidine-sensitive non-alpha(1) binding site in rat kidney membranes.

作者信息

Mugisha Paul, Gründemann Dirk, Schömig Edgar, Uhlén Staffan

机构信息

Department of Physiology, Uppsala University, Box 572 BioMedical Centre, 751 23 Uppsala, Sweden.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 2002 May;365(5):335-40. doi: 10.1007/s00210-002-0536-z. Epub 2002 Apr 5.

DOI:10.1007/s00210-002-0536-z

PMID:12012018

Abstract

[(3)H]Prazosin bound to alpha(1A)- and alpha(1B)-adrenoceptors, as well as to a cimetidine-sensitive non-alpha(1)-adrenoceptor binding site in rat kidney membranes. An experimental design is presented where the alpha(1)-adrenoceptors are selectively exposed by blocking the non-alpha(1) binding site with 60 microM cimetidine. Conversely, the non-alpha(1) binding site can be selectively exposed by blocking the alpha(1)-adrenoceptors with 600 nM metitepine. The identity of the non-alpha(1) binding site for [(3)H]prazosin in the rat kidney, herein pharmacologically characterized by 33 competing substances, is still unknown.

摘要

[³H]哌唑嗪与大鼠肾膜中的α₁A-和α₁B-肾上腺素能受体以及西咪替丁敏感的非α₁-肾上腺素能受体结合位点结合。本文提出了一种实验设计，通过用60微摩尔西咪替丁阻断非α₁结合位点来选择性地暴露α₁-肾上腺素能受体。相反，用600纳摩尔美替平阻断α₁-肾上腺素能受体可以选择性地暴露非α₁结合位点。大鼠肾脏中[³H]哌唑嗪的非α₁结合位点的身份仍然未知，本文通过33种竞争物质对其进行了药理学表征。