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Lobelane analogues as novel ligands for the vesicular monoamine transporter-2

G Zheng, LP Dwoskin, AG Deaciuc, J Zhu…

文献索引:Zheng, Guangrong; Dwoskin, Linda P.; Deaciuc, Agripina G.; Zhu, Jun; Jones, Marlon D.; Crooks, Peter A. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 12 p. 3899 - 3909

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被引用次数: 33

摘要

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 Ki values ranging from 430 to 580nM.