Regulation of alpha 4 beta 2 nicotinic acetylcholine receptors in M10 cells following treatment with nicotinic agents. 1995

X Zhang, and Z H Gong, and E Hellström-Lindahl, and A Nordberg
Department of Clinical Neuroscience and Family Medicine, Karolinska Institute, Huddinge University Hospital, Sweden.

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.

UI MeSH Term Description Entries
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D009538 Nicotine Nicotine is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke. Nicotine Bitartrate,Nicotine Tartrate
D011807 Quinolizines
D011978 Receptors, Nicotinic One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors. Nicotinic Acetylcholine Receptors,Nicotinic Receptors,Nicotinic Acetylcholine Receptor,Nicotinic Receptor,Acetylcholine Receptor, Nicotinic,Acetylcholine Receptors, Nicotinic,Receptor, Nicotinic,Receptor, Nicotinic Acetylcholine,Receptors, Nicotinic Acetylcholine
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D004079 Dihydro-beta-Erythroidine Dihydro analog of beta-erythroidine, which is isolated from the seeds and other plant parts of Erythrina sp. Leguminosae. It is an alkaloid with curarimimetic properties. Dihydro beta Erythroidine,Erythroidine, Dihydro beta,beta Erythroidine, Dihydro
D000470 Alkaloids Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed) Alkaloid,Plant Alkaloid,Plant Alkaloids,Alkaloid, Plant,Alkaloids, Plant
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001392 Azocines
D014403 Tubocurarine A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae. Tubocurare,Tubocurarine Chloride,d-Tubocurare,d-Tubocurarine

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