Document Report Card

ID: ALA1123334

Journal: J Med Chem

Title: 4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.

Authors: Guérémy C, Audiau F, Renault C, Benavides J, Uzan A, Le Fur G.

Abstract: A series of 4-amino-6-chloro-2-piperazinopyrimidines were synthesized and evaluated for their ability to interact with alpha 1- and alpha 2-adrenoceptors in vitro in binding assays using [3H]WB-4101, [3H]clonidine, and [3H]idazoxan as radioligands. Some compounds were also tested as inhibitors of [3H]spiroperidol binding. Several members of this series showed high and selective affinity for alpha 2-adrenoceptors. The nature of the 4-amino substituent seems to be the most critical factor in determining the potency at these receptors.

CiteXplore: 3016265

DOI: 10.1021/jm00158a013