Literature DB >> 16905316

Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.

Guangrong Zheng1, David B Horton, Agripina G Deaciuc, Linda P Dwoskin, Peter A Crooks.   

Abstract

A series of des-keto lobeline analogs has been synthesized and evaluated for their ability to inhibit the dopamine transporter (DAT) and serotonin transporter (SERT) function and for their affinity for the synaptic vesicle monoamine transporter (VMAT2), as well as for alpha4beta2( *) and alpha7( *) neuronal nicotinic acetylcholine receptors (nAChRs). The enantiomers 8R-hydroxylobel-9-ene (3a) and 10S-hydroxylobel-7-ene (3c) exhibited high potency and selectivity at SERT and DAT, respectively.

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Year:  2006        PMID： 16905316      PMCID： PMC3934794          DOI： 10.1016/j.bmcl.2006.07.070

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  18 in total

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Authors:  Linda P Dwoskin; Peter A Crooks
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5.  Lobeline inhibits nicotine-evoked [(3)H]dopamine overflow from rat striatal slices and nicotine-evoked (86)Rb(+) efflux from thalamic synaptosomes.

Authors:  D K Miller; P A Crooks; L P Dwoskin
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7.  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

8.  In vitro and in vivo studies of benzisoquinoline ligands for the brain synaptic vesicle monoamine transporter.

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  3 in total

Review 1.  Design, synthesis and interaction at the vesicular monoamine transporter-2 of lobeline analogs: potential pharmacotherapies for the treatment of psychostimulant abuse.

Authors:  Peter A Crooks; Guangrong Zheng; Ashish P Vartak; John P Culver; Fang Zheng; David B Horton; Linda P Dwoskin
Journal:  Curr Top Med Chem       Date:  2011       Impact factor: 3.295

2.  Synthesis of Lobeline, Lobelane and their Analogues. A Review.

Authors:  Guangrong Zheng; Peter A Crooks
Journal:  Org Prep Proced Int       Date:  2015-08-17       Impact factor: 1.628

3.  Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.

Authors:  Marhaba Hojahmat; David B Horton; Seth D Norrholm; Dennis K Miller; Vladimir P Grinevich; Agripina Gabriela Deaciuc; Linda P Dwoskin; Peter A Crooks
Journal:  Bioorg Med Chem       Date:  2009-12-06       Impact factor: 3.641
  3 in total

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