Improving selectivity of dopamine D3 receptor ligands.
作者： Marc Capet , Thierry Calmels , Nicolas Levoin , Denis Danvy , Isabelle Berrebi-Bertrand
DOI: 10.1016/J.BMCL.2015.12.068
关键词:
摘要: The seminal human dopamine D3 receptor (hD3R) ligand BP 897 has shown interesting properties during clinical trials. However, its lack of selectivity towards adrenergic impedes further development. Two approaches were followed to increase hD3R selectivity. lead optimisation succeeded, we disclose here ligands with subnanomolar potency for D3R, combined a good the closely related D2 and alpha-1 receptors.
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