Regulation of α4β2 nicotinic acetylcholine receptors in M10 cells following treatment with nicotinic agents
Abstract
The effects of chronic treatment (3 days) with the nicotinic agonists, nicotine and cytisine as well as the antagonists, d-tubocurarine, hexamethonium and dihydro-beta-erythroidine (DH beta E) on alpha 4 beta 2 nicotinic acetylcholine receptors (nAChRs) were investigated in a permanently transfected cell line, M10. The number of alpha 4 beta 2 nAChRs expressed in the cell line was assayed by (-)-[3H]nicotine binding. The two enantiomers of nicotine both significantly increased the number of nAChRs in a concentration dependent manner. No changes in the levels of mRNA for either alpha 4 or beta 2 subunits were found following chronic (-)-nicotine treatment. The effect of (-)-nicotine treatment on the number of nAChRs was partially blocked by the antagonists d-tubocurarine and hexamethonium, but not by dihydro-beta-erythroidine (DH beta E). Chronic exposure of the cells to each of the antagonists did not influence the number of nAChRs. Treatment with the agonist cytisine resulted in a bell-shaped dose-dependent effect on the number of alpha 4 beta 2 nAChRs. In the presence of cytisine (microM) the effect induced by chronic(-)-nicotine treatment on the number of the nAChRs was attenuated. These results indicate that nicotinic agents can induce different regulatory effects in M10 cells due to their individual pharmacological properties as agonist and/or antagonist.
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Greater β2*-nAChR availability is not associated with changes in β2*-nAChR mRNA, protein synthesis, rate of receptor internalization, postendocytic trafficking, or lysosomal degradation.
“Greater  2 *- nAChR availability is not associated with changes in  2 *-nAChR mRNA (Marks et al., 1992;Peng et al., 1994;Zhang et al., 1994) protein synthesis (Buisson and Bertrand, 2001), rate of receptor internalization, postendocytic trafficking, or lysosomal degradation (Darsow et al., 2005)”
From Human Tobacco Smokers in Early Abstinence Have Higher Levels of β<sub>2</sub>* Nicotinic Acetylcholine Receptors than Nonsmokers (2006) · cites this paper as Zhang et al., 1994
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Staley, J. K., Krishnan-Sarin, S., Cosgrove, K. P., Krantzler, E., Frohlich, E., Perry, E., Dubin, J. A., Estok, K., Brenner, E., Baldwin, R. M., et al. (2006) · The Journal of Neuroscience · doi:10.1523/jneurosci.0546-06.2006 · Cited by 223 · see citing works
“Greater 2*- nAChR availability is not associated with changes in 2*-nAChR mRNA (Marks et al., 1992; Peng et al., 1994; Zhang et al., 1994) protein synthesis (Buisson and Bertrand, 2001), rate of receptor internalization, postendocytic trafficking, or lysosomal degradation (Darsow et al., 2005), but…”
BackgroundKe, L., Eisenhour, C. M., Bencherif, M., & Lukas, R. J. (1998) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)37658-x · Cited by 136 · see citing works
Sallette, J., Bohler, S., Benoit, P., Soudant, M., Pons, S., Le Novère, N., Changeux, J.-P., & Corringer, P. J. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m308260200 · Cited by 80 · see citing works
Whiteaker, P., Sharples, C. G. V., & Wonnacott, S. (1998) · Molecular Pharmacology · doi:10.1016/s0026-895x(24)13263-4 · Cited by 152 · see citing works
Harkness, P. C., & Millar, N. S. (2002) · The Journal of Neuroscience · doi:10.1523/jneurosci.22-23-10172.2002 · Cited by 74 · see citing works
- Authors
- Zhang, X., Gong, Z.-H., Hellström-Lindahl, E., & Nordberg, A.
- Affiliations
- Karolinska Institutet (SE)
- Venue
- Neuroreport
- Published
- 1995-01
- Volume
- 6
- Issue
- 2
- Pages
- 313-317
- ISSN
- 0959-4965 (ISSN-L)
- OpenAlex
- W1985242427
- Cited by
- 36
- References
- 0
- Citations by year
- 2015: 2
- FWCI
- 1.49
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Neuroreport (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Health Sciences › Medicine › Physiology › Smoking Behavior and Cessation
- Keywords
- α4β2 nicotinic acetylcholine receptor, receptor regulation, nicotine, cytisine, tubocurarine, hexamethonium, dihydro-beta-erythroidine, receptor up-regulation
- MeSH terms
- Quinolizidine Alkaloids, Alkaloids, Animals, Azocines, Cell Line, Dihydro-beta-Erythroidine, Models, Biological, Nicotine, Quinolizines, Receptors, Nicotinic, Tubocurarine, Hexamethonium, Mice
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