title: Exploring the effect ofN-substitution innor-lobelane on the interaction with VMAT2: discovery of a potential clinical candidate for treatment of methamphetamine abuse.
abstract: A series ofN-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 anN-1,2(R)-dihydroxypropyl group, had been identified as a potential clinical candidate for the treatment of methamphetamine abuse.
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA.
authors.forename: Guangrong
authors.initials: G
authors.lastname: Zheng
authors.forename: David B
authors.initials: DB
authors.lastname: Horton
authors.forename: Narsimha Reddy
authors.initials: NR
authors.lastname: Penthala
authors.forename: Justin R
authors.initials: JR
authors.lastname: Nickell
authors.forename: John P
authors.initials: JP
authors.lastname: Culver
authors.forename: Agripina G
authors.initials: AG
authors.lastname: Deaciuc
authors.forename: Linda P
authors.initials: LP
authors.lastname: Dwoskin
authors.forename: Peter A
authors.initials: PA
authors.lastname: Crooks