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Design, synthesis, and biological evaluation of structurally constrained hybrid analogues containing ropinirole moiety as a novel class of potent and selective dopamine D3 receptor ligands
Author(s) -
Zhou Benhua,
Hong Kwon Ho,
Ji Min,
Cai Jin
Publication year - 2018
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.13324
Subject(s) - dopamine receptor d3 , radioligand , moiety , chemistry , ropinirole , affinities , ligand (biochemistry) , radioligand assay , selectivity , dopamine , dopamine receptor d2 , stereochemistry , binding affinities , receptor , dopamine receptor , combinatorial chemistry , biochemistry , dopamine agonist , biology , agonist , neuroscience , catalysis
Two series of hybrid analogues were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine D3 receptor. Binding affinities of target compounds were determined (using the method of radioligand binding assay). Compared to comparator agent BP 897, compounds 2a and 2c were found to demonstrate a considerable binding affinity and selectivity for D3 receptor, and especially compound 2h was similarly potent and more selective D3R ligand than BP 897, a positive reference. Thus, they may provide valuable information for the discovery and development of highly potent dopamine D3 receptor ligands with outstanding selectivity.