Literature DB >> 15911306

Lobelane analogues as novel ligands for the vesicular monoamine transporter-2.

Guangrong Zheng1, Linda P Dwoskin, Agripina G Deaciuc, Jun Zhu, Marlon D Jones, Peter A Crooks.   

Abstract

A series of lobelane analogues has been synthesized and their structure-activity relationships at the vesicular monoamine transporter-2 (VMAT2) have been evaluated. The most potent analogues in this series were the cis-2,6-piperidino analogues, 25b, 27b, 28b, and 30b, with K(i) values ranging from 430 to 580 nM.

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Year:  2005        PMID： 15911306      PMCID： PMC3593046          DOI： 10.1016/j.bmc.2005.04.013

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  22 in total

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7.  Rhodium-catalyzed addition of arylboronic acids to alkynyl aza-heteroaromatic compounds in water.

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8.  Lobeline analogs with enhanced affinity and selectivity for plasmalemma and vesicular monoamine transporters.

Authors:  Dennis K Miller; Peter A Crooks; Guangrong Zheng; Vladimir P Grinevich; Seth D Norrholm; Linda P Dwoskin
Journal:  J Pharmacol Exp Ther       Date:  2004-04-30       Impact factor: 4.030

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10.  Indirect trapping of the retroconjugate addition reaction intermediate involved in the epimerization of lobeline: application to the synthesis of (-)-sedamine.

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  18 in total

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2.  Computational neural network analysis of the affinity of lobeline and tetrabenazine analogs for the vesicular monoamine transporter-2.

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3.  Phenyl ring-substituted lobelane analogs: inhibition of [³H]dopamine uptake at the vesicular monoamine transporter-2.

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Review 4.  Design, synthesis and interaction at the vesicular monoamine transporter-2 of lobeline analogs: potential pharmacotherapies for the treatment of psychostimulant abuse.

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6.  Lobelane analogues containing 4-hydroxy and 4-(2-fluoroethoxy) aromatic substituents: Potent and selective inhibitors of [(3)H]dopamine uptake at the vesicular monoamine transporter-2.

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Review 7.  The vesicular monoamine transporter-2: an important pharmacological target for the discovery of novel therapeutics to treat methamphetamine abuse.

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8.  Stereoselective Synthesis of Saturated Heterocycles via Pd-Catalyzed Alkene Carboetherification and Carboamination Reactions.

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9.  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.

Authors:  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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