Literature DB >> 15908213

In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.

Jotham W Coe1, Michael G Vetelino, Crystal G Bashore, Michael C Wirtz, Paige R Brooks, Eric P Arnold, Lorraine A Lebel, Carol B Fox, Steven B Sands, Thomas I Davis, David W Schulz, Hans Rollema, F David Tingley, Brian T O'Neill.   

Abstract

The preparation and biological activity of analogs of (-)-cytisine, an alpha4beta2 nicotinic receptor partial agonist, are discussed. All-carbon-containing phenyl ring replacements of the pyridone ring system, generated via Heck cyclization protocols, exhibited weaker affinity and lower efficacy partial agonist profiles relative to (-)-cytisine. In vivo, selected compounds exhibit lower efficacy partial agonist profiles than that of (-)-cytisine.

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Year:  2005        PMID： 15908213     DOI： 10.1016/j.bmcl.2005.04.036

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


  11 in total

1.  Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.

Authors:  Sheela K Chellappan; Yingxian Xiao; Werner Tueckmantel; Kenneth J Kellar; Alan P Kozikowski
Journal:  J Med Chem       Date:  2006-05-04       Impact factor: 7.446

Review 2.  Neuronal nicotinic acetylcholine receptors as pharmacotherapeutic targets for the treatment of alcohol use disorders.

Authors:  S Chatterjee; S E Bartlett
Journal:  CNS Neurol Disord Drug Targets       Date:  2010-03       Impact factor: 4.388

3.  α4β2 nicotinic acetylcholine receptor partial agonists with low intrinsic efficacy have antidepressant-like properties.

Authors:  Yann S Mineur; Emily B Einstein; Patricia A Seymour; Jotham W Coe; Brian T O'neill; Hans Rollema; Marina R Picciotto
Journal:  Behav Pharmacol       Date:  2011-08       Impact factor: 2.293

Review 4.  Varenicline: a review of its use as an aid to smoking cessation therapy.

Authors:  Gillian M Keating; M Asif A Siddiqui
Journal:  CNS Drugs       Date:  2006       Impact factor: 5.749

5.  Effects of the nicotinic receptor partial agonists varenicline and cytisine on the discriminative stimulus effects of nicotine in rats.

Authors:  Mark G LeSage; David Shelley; Jason T Ross; F Ivy Carroll; William A Corrigall
Journal:  Pharmacol Biochem Behav       Date:  2008-09-09       Impact factor: 3.533

6.  Cytisine-based nicotinic partial agonists as novel antidepressant compounds.

Authors:  Yann S Mineur; Christoph Eibl; Grace Young; Christopher Kochevar; Roger L Papke; Daniela Gündisch; Marina R Picciotto
Journal:  J Pharmacol Exp Ther       Date:  2009-01-22       Impact factor: 4.030

Review 7.  Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.

Authors:  Li-Fang Yu; Han-Kun Zhang; Barbara J Caldarone; J Brek Eaton; Ronald J Lukas; Alan P Kozikowski
Journal:  J Med Chem       Date:  2014-07-02       Impact factor: 7.446

8.  Partial nicotinic acetylcholine (alpha4beta2) agonists as promising new medications for smoking cessation.

Authors:  J Singh; Salil Budhiraja
Journal:  Indian J Pharmacol       Date:  2008-10       Impact factor: 1.200

Review 9.  Cognitive deficits in schizophrenia: focus on neuronal nicotinic acetylcholine receptors and smoking.

Authors:  Enrique L M Ochoa; Jose Lasalde-Dominicci
Journal:  Cell Mol Neurobiol       Date:  2007-08       Impact factor: 5.046

Review 10.  Orthosteric and Allosteric Ligands of Nicotinic Acetylcholine Receptors for Smoking Cessation.

Authors:  Tasnim S Mohamed; Selwyn S Jayakar; Ayman K Hamouda
Journal:  Front Mol Neurosci       Date:  2015-11-25       Impact factor: 5.639
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