Lobelane analogues as novel ligands for the vesicular monoamine transporter-2
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 K-i ranging from 430 to 580 nM.. (c) 2005 Elsevier Ltd. All rights reserved.
Lobelane analogues as novel ligands for the vesicular monoamine transporter-2
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 K-i ranging from 430 to 580 nM.. (c) 2005 Elsevier Ltd. All rights reserved.
2,6-disubstituted piperidines and piperazine compounds
申请人:——
公开号:US20040266824A1
公开(公告)日:2004-12-30
The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula:
1
which are used to treat diseases of the central nervous system, drug abuse, and withdrawal therefrom as well as treating eating disorders.
Lobelane analogues as novel ligands for the vesicular monoamine transporter-2
作者:Guangrong Zheng、Linda P. Dwoskin、Agripina G. Deaciuc、Jun Zhu、Marlon D. Jones、Peter A. Crooks
DOI:10.1016/j.bmc.2005.04.013
日期:2005.6
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 ranging from 430 to 580 nM.. (c) 2005 Elsevier Ltd. All rights reserved.