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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Published in: | Molecular pharmacology 1997-09, Vol.52 (3), p.524-534 |
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Main Authors: | , , |
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 ( |
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ISSN: | 0026-895X |
DOI: | 10.1124/mol.52.3.524 |