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Issue 3, 2013
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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

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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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Publication details

The article was received on 18 Dec 2012, accepted on 21 Jan 2013 and first published on 22 Jan 2013


Article type: Concise Article
DOI: 10.1039/C3MD20374C
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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