Literature DB >> 15050621

Epibatidine structure-activity relationships.

F Ivy Carroll1.   

Abstract

Epibatidine is a potent but nonselective nAChR agonist. Its biological effects appear to be mediated largely by alpha4beta2 nAChRs. Surprisingly, only a limited number of epibatidine analogues have been synthesized and evaluated in in vitro assays. Even fewer analogues have received in vivo pharmacological evaluation. In this paper, SAR studies directed toward epibatidine analogues will be reviewed.

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Year:  2004        PMID： 15050621     DOI： 10.1016/j.bmcl.2004.02.007

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


  19 in total

1.  Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.

Authors:  Nurulain Zaveri; Faming Jiang; Cris Olsen; Willma Polgar; Lawrence Toll
Journal:  J Med Chem       Date:  2010-10-27       Impact factor: 7.446

2.  Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs.

Authors:  F Ivy Carroll; Yasuno Yokota; Wei Ma; Jeffrey R Lee; Lawrence E Brieaddy; Jason P Burgess; Hernán A Navarro; M I Damaj; Billy R Martin
Journal:  Bioorg Med Chem       Date:  2007-10-13       Impact factor: 3.641

3.  Investigating the hydrogen-bond acceptor site of the nicotinic pharmacophore model: a computational and experimental study using epibatidine-related molecular probes.

Authors:  Clelia Dallanoce; Giovanni Grazioso; Diego Yuri Pomè; Miriam Sciaccaluga; Carlo Matera; Cecilia Gotti; Sergio Fucile; Marco De Amici
Journal:  J Comput Aided Mol Des       Date:  2013-11-26       Impact factor: 3.686

4.  Synthesis and nicotinic acetylcholine receptor in vitro and in vivo pharmacological properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues of 2'-fluoro-3'-(4-nitrophenyl)deschloroepibatidine.

Authors:  Pauline Ondachi; Ana Castro; Charles W Luetje; M Imad Damaj; S Wayne Mascarella; Hernán A Navarro; F Ivy Carroll
Journal:  J Med Chem       Date:  2012-07-11       Impact factor: 7.446

5.  Design, synthesis, and biological activity of 5'-phenyl-1,2,5,6-tetrahydro-3,3'-bipyridine analogues as potential antagonists of nicotinic acetylcholine receptors.

Authors:  Yafei Jin; Xiaoqin Huang; Roger L Papke; Emily M Jutkiewicz; Hollis D Showalter; Chang-Guo Zhan
Journal:  Bioorg Med Chem Lett       Date:  2017-08-14       Impact factor: 2.823

6.  Differential regulation of alcohol taking and seeking by antagonism at α4β2 and α3β4 nAChRs.

Authors:  Andrea Cippitelli; Gloria Brunori; Jennifer Schoch; Christopher J Armishaw; Jinhua Wu; Nurulain T Zaveri; Marc A Giulianotti; Gregory S Welmaker; Lawrence Toll
Journal:  Psychopharmacology (Berl)       Date:  2018-03-23       Impact factor: 4.530

7.  Synthesis of phantasmidine.

Authors:  Quan Zhou; Barry B Snider
Journal:  Org Lett       Date:  2010-12-22       Impact factor: 6.005

8.  Effects of the specific α4β2 nAChR antagonist, 2-fluoro-3-(4-nitrophenyl) deschloroepibatidine, on nicotine reward-related behaviors in rats and mice.

Authors:  K M Tobey; D M Walentiny; J L Wiley; F I Carroll; M I Damaj; M R Azar; G F Koob; O George; L S Harris; R E Vann
Journal:  Psychopharmacology (Berl)       Date:  2012-04-22       Impact factor: 4.530

9.  Computational analysis of the binding ability of heterocyclic and conformationally constrained epibatidine analogs in the neuronal nicotinic acetylcholine receptor.

Authors:  Elena Soriano; José Marco-Contelles; Inés Colmena; Luis Gandía
Journal:  Mol Divers       Date:  2009-05-29       Impact factor: 2.943

10.  3'-Fluoro substitution in the pyridine ring of epibatidine improves selectivity and efficacy for alpha4beta2 versus alpha3beta4 nAChRs.

Authors:  Galya R Abdrakhmanova; F Ivy Carroll; M I Damaj; Billy R Martin
Journal:  Neuropharmacology       Date:  2008-08-15       Impact factor: 5.250
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