Regulation of human alpha 4 beta 2 neuronal nicotinic acetylcholine receptors by cholinergic channel ligands and second messenger pathways

The alpha 4 beta 2 nicotinic acetylcholine receptors (nAChRs), a major subtype in the brain, have been shown to be modulated by chronic treatment with nicotine. In this study, the regulation of recombinant human alpha 4 beta 2 nAChR subtype by (-)-nicotine and other cholinergic channel modulators wa...

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Bibliographic Details
Published in:Molecular pharmacology 1997-09, Vol.52 (3), p.524-534
Main Authors: Gopalakrishnan, M, Molinari, E J, Sullivan, J P
Format: Article
Language:English
Online Access:Get full text
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Summary:The alpha 4 beta 2 nicotinic acetylcholine receptors (nAChRs), a major subtype in the brain, have been shown to be modulated by chronic treatment with nicotine. In this study, the regulation of recombinant human alpha 4 beta 2 nAChR subtype by (-)-nicotine and other cholinergic channel modulators was studied using human embryonic kidney 293 cells stably expressing this subunit combination. The treatment of transfected cells with (-)-nicotine and other activator ligands, including (-)-cytisine, 1,1-dimethyl-4-phenylpiperazinium, (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole, and ( plus or minus )-epibatidine, resulted in concentration-dependent increases in the levels of alpha 4 beta 2 nAChRs. The increase in [ super(3)H]cytisine binding sites was initiated by low concentrations of (-)-nicotine (
ISSN:0026-895X
DOI:10.1124/mol.52.3.524