TY - JOUR
T1 - Exploring the effect of N-substitution in nor-lobelane on the interaction with VMAT2
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.
N1 - Copyright:
Copyright 2013 Elsevier B.V., All rights reserved.
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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U2 - 10.1039/c3md20374c
DO - 10.1039/c3md20374c
M3 - Article
AN - SCOPUS:84874471208
SN - 2040-2503
VL - 4
SP - 564
EP - 568
JO - MedChemComm
JF - MedChemComm
IS - 3
ER -