Exploring the Effect of -substitution in -lobelane on the Interaction with VMAT2: Discovery of a Potential Clinical Candidate for Treatment of Methamphetamine Abuse

Overview

Journal Medchemcomm

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2013 Mar 26

PMID 23527317

Citations 4

Authors

Guangrong Zheng

David B Horton

Narsimha Reddy Penthala

Justin R Nickell

John P Culver

Agripina G Deaciuc

Linda P Dwoskin

Peter A Crooks

Affiliations

Soon will be listed here.

Abstract

A series of -substituted lobelane analogues was synthesized and evaluated for their [H]dihydrotetrabenazine binding affinity at the vesicular monoamine transporter and for their inhibition of vesicular [H]dopamine uptake. Compound 19a, which contains an -1,2()-dihydroxypropyl group, had been identified as a potential clinical candidate for the treatment of methamphetamine abuse.

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Synthesis of Lobeline, Lobelane and their Analogues. A Review.

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