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Design, Synthesis, and Evaluation of Indolebutylamines as a Novel Class of Selective Dopamine D 3 Receptor Ligands
Author(s) -
Du Peng,
Xu Lili,
Huang Jiye,
Yu Kunqian,
Zhao Rui,
Gao Bo,
Jiang Hualiang,
Zhao Weili,
Zhen Xuechu,
Fu Wei
Publication year - 2013
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12158
Subject(s) - dopamine , dopamine receptor , receptor , chemistry , selectivity , dopamine receptor d2 , dopamine receptor d3 , combinatorial chemistry , biochemistry , biology , neuroscience , catalysis
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 n m and displays excellent selectivity over the dopamine 1 receptor and dopamine 2 receptor. Investigation based on structural information indicates that site S 182 located in extracellular loop 2 may account for high selectivity of compounds. Interaction models of the dopamine 3 receptor‐ 11q complex and structure‐activity relationships were discussed by integrating all available experimental and computational data with the eventual aim to discover potent and selective ligands to dopamine 3 receptor.
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