Design, synthesis, and evaluation of indolebutylamines as a novel class of selective dopamine D3 receptor ligands

…, J Huang, K Yu, R Zhao, B Gao, H Jiang…

Index: Du, Peng; Xu, Lili; Huang, Jiye; Yu, Kunqian; Zhao, Rui; Gao, Bo; Jiang, Hualiang; Zhao, Weili; Zhen, Xuechu; Fu, Wei Chemical Biology and Drug Design, 2013 , vol. 82, # 3 p. 326 - 335

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Citation Number: 4

Abstract

A series of indolebutylamine derivatives were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine 3 receptor. The most potent compound 11q binds to dopamine 3 receptor with a K i value of 124 nm and displays excellent selectivity over the dopamine 1 receptor and dopamine 2 receptor. Investigation based on structural information indicates that site S182 located in extracellular loop 2 may account for high selectivity of ...