Zheng Guangrong, Dwoskin Linda P, Deaciuc Agripina G, Zhu Jun, Jones Marlon D, Crooks Peter A
College of Pharmacy, University of Kentucky, Rose Street, Lexington, KY 40536-0082, USA.
Bioorg Med Chem. 2005 Jun 2;13(12):3899-909. doi: 10.1016/j.bmc.2005.04.013.
A series of lobelane analogues has been synthesized and their structure-activity relationships at the vesicular monoamine transporter-2 (VMAT2) have been evaluated. The most potent analogues in this series were the cis-2,6-piperidino analogues, 25b, 27b, 28b, and 30b, with K(i) values ranging from 430 to 580 nM.
已经合成了一系列洛贝林类似物,并评估了它们在囊泡单胺转运体2(VMAT2)上的构效关系。该系列中最有效的类似物是顺式-2,6-哌啶基类似物25b、27b、28b和30b,其抑制常数(K(i))值在430至580 nM之间。