Evaluation of N-phenyl homopiperazine analogs as potential dopamine D 3 receptor selective ligands

A Li, Y Mishra, M Malik, Q Wang, S Li, M Taylor…

Index: Li, Aixiao; Mishra, Yogesh; Malik, Maninder; Wang, Qi; Li, Shihong; Taylor, Michelle; Reichert, David E.; Luedtke, Robert R.; MacH, Robert H. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 11 p. 2988 - 2998

Full Text: HTML

Citation Number: 4

Abstract

A series of N-(2-methoxyphenyl) homopiperazine analogs was prepared and their affinities for dopamine D2, D3, and D4 receptors were measured using competitive radioligand binding assays. Several ligands exhibited high binding affinity and selectivity for the D3 dopamine receptor compared to the D2 receptor subtype. Compounds 11a, 11b, 11c, 11f, 11j and 11k had Ki values ranging from 0.7 to 3.9 nM for the D3 receptor with 30-to 170- ...