Exploring the effect of N-substitution in nor-lobelane on the interaction with VMAT2: discovery of a potential clinical candidate for treatment of methamphetamine abuse

A series of N -substituted lobelane analogues was synthesized and evaluated for their [ 3 H]dihydrotetrabenazine binding affinity at the vesicular monoamine transporter and for their inhibition of vesicular [ 3 H]dopamine uptake. Compound 19a , which contains an N -1,2( R )-dihydroxypropyl group, ha...

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Published in:MedChemComm 2013-03, Vol.4 (3), p.564-568
Main Authors: Zheng, Guangrong, Horton, David B, Penthala, Narsimha Reddy, Nickell, Justin R, Culver, John P, Deaciuc, Agripina G, Dwoskin, Linda P, Crooks, Peter A
Format: Article
Language:English
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Summary:A series of N -substituted lobelane analogues was synthesized and evaluated for their [ 3 H]dihydrotetrabenazine binding affinity at the vesicular monoamine transporter and for their inhibition of vesicular [ 3 H]dopamine uptake. Compound 19a , which contains an N -1,2( R )-dihydroxypropyl group, had been identified as a potential clinical candidate for the treatment of methamphetamine abuse. N -1,2( R )-Dihydroxypropyl containing lobelane analogues as potential treatments for methamphetamine abuse.
ISSN:2040-2503
2040-2511
DOI:10.1039/c3md20374c