Issue 3, 2013
From the journal:

MedChemComm

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

Guangrong Zheng,a   David B. Horton,b   Narsimha Reddy Penthala,a   Justin R. Nickell,b   John P. Culver,b   Agripina G. Deaciuc,b   Linda P. Dwoskinb  and  Peter A. Crooks*a  

* Corresponding authors

a Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA
E-mail: pacrooks@uams.edu
Fax: +1-501-686-6057
Tel: +1-501-686-6495

b Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA

Abstract

A series of N-substituted lobelane analogues was synthesized and evaluated for their [3H]dihydrotetrabenazine binding affinity at the vesicular monoamine transporter and for their inhibition of vesicular [3H]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.

Graphical abstract: 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

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Article information

DOI
https://doi.org/10.1039/C3MD20374C
Article type
Concise Article
Submitted
18 Dec 2012
Accepted
21 Jan 2013
First published
22 Jan 2013

Med. Chem. Commun., 2013,4, 564-568

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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

G. Zheng, D. B. Horton, N. R. Penthala, J. R. Nickell, J. P. Culver, A. G. Deaciuc, L. P. Dwoskin and P. A. Crooks, Med. Chem. Commun., 2013, 4, 564 DOI: 10.1039/C3MD20374C

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