N-（1-苄基吡咯烷-3-基）芳基苯甲酰胺作为强效和选择性的人多巴胺D4拮抗剂。

N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.

作者信息

Egle Ian, Barriault Nancy, Bordeleau Michel, Drage Jillian, Dube Laurence, Peragine Jack, Mazzocco Lucy, Arora Jalaj, Jarvie Keith, Tehim Ashok

机构信息

NPS Pharmaceuticals Inc., 6850 Goreway Dr., Mississauga, Ontario L4V 1V7, Canada.

出版信息

Bioorg Med Chem Lett. 2004 Oct 4;14(19):4847-50. doi: 10.1016/j.bmcl.2004.07.045.

DOI:10.1016/j.bmcl.2004.07.045

PMID:15341937

Abstract

A series of N-(1-benzylpyrrolidin-3-yl)arylbenzamides 8 has been prepared, and their structure-activity relationships studied. Potent ligands selective for human D(4) (hD(4)) over hD(2) and alpha(1) have been identified. One example was determined to be an antagonist in a cAMP assay, with an IC(50) of 1500 nM.

摘要

已经制备了一系列N-(1-苄基吡咯烷-3-基)芳基苯甲酰胺8，并研究了它们的构效关系。已鉴定出对人D(4)(hD(4))比对hD(2)和α(1)具有选择性的强效配体。其中一个例子在cAMP测定中被确定为拮抗剂，IC(50)为1500 nM。