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; David B. Horton; Narsimha Reddy Penthala; Justin R. Nickell; John P. Culver; Agripina G. Deaciuc; Linda P. Dwoskin; Peter A. Crooks

doi:10.1039/c3md20374c

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, David B. Horton, Narsimha Reddy Penthala, Justin R. Nickell, John P. Culver, Agripina G. Deaciuc, Linda P. Dwoskin, Peter A. Crooks

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6 Scopus citations

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.

Original language	English
Pages (from-to)	564-568
Number of pages	5
Journal	MedChemComm
Volume	4
Issue number	3
DOIs	https://doi.org/10.1039/c3md20374c
State	Published - Mar 2013

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Organic Chemistry

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title = "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",

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.",

author = "Guangrong Zheng and Horton, \{David B.\} and Penthala, \{Narsimha Reddy\} and Nickell, \{Justin R.\} and Culver, \{John P.\} and Deaciuc, \{Agripina G.\} and Dwoskin, \{Linda P.\} and Crooks, \{Peter A.\}",

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T2 - Discovery of a potential clinical candidate for treatment of methamphetamine abuse

AU - Zheng, Guangrong

AU - Horton, David B.

AU - Penthala, Narsimha Reddy

AU - Nickell, Justin R.

AU - Culver, John P.

AU - Deaciuc, Agripina G.

AU - Dwoskin, Linda P.

AU - Crooks, Peter A.

PY - 2013/3

Y1 - 2013/3

N2 - 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.

AB - 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.

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UR - https://www.scopus.com/inward/citedby.url?scp=84874471208&partnerID=8YFLogxK

U2 - 10.1039/c3md20374c

DO - 10.1039/c3md20374c

M3 - Article

AN - SCOPUS:84874471208

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VL - 4

SP - 564

EP - 568

JO - MedChemComm

JF - MedChemComm

IS - 3

ER -

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

Abstract

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