Conversion between configurational states of the muscarinic receptor in rat brain

European Journal of Pharmacology
R S AronstamL G Abood

Abstract

Reductive alkylation of neural membranes by N-ethyl maleimide (NEM) converts muscarinic acetylcholine receptors from a state of low to high affinity for receptor agonists. Interactions of muscarinic antagonists with the receptor are unaffected by this treatment. Muscarinic receptors from the rat telencephalon in the high agonist affinity state are increased from 34.2 to 53.4% of the total receptor population and the Ki for carbamylcholine inhibition of 3-quinuclidinyl benzilate binding is decreased from 1.2 X 10(-4) to 6.9 X 10(-5) M by NEM treatment.

References

Jan 1, 1976·Annual Review of Physiology·S H Snyder, J P Bennett
Sep 15, 1977·Biochemical Pharmacology·R S AronstamJ Baumgold
Jul 1, 1976·Journal of Neurochemistry·N J Birdsall, E C Hulme
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May 1, 1974·Proceedings of the National Academy of Sciences of the United States of America·H I Yamamura, S H Snyder

Citations

Jan 1, 1988·Pharmacology & Therapeutics·F Mitchelson
Jul 1, 1981·Proceedings of the National Academy of Sciences of the United States of America·R S Aronstam, B Witkop
Jul 13, 2013·Journal of Biomedical Science·Tso-Hao TangRobert S Aronstam
May 1, 1979·Toxicology and Applied Pharmacology·R S Aronstam, M E Elderfrawi
Jun 1, 1984·Journal of Autonomic Pharmacology·H SiegelD J Triggle
Oct 16, 1980·Biochemical and Biophysical Research Communications·D Gurwitz, M Sokolovsky
Feb 13, 1980·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·N J BirdsallA S Burgen
Sep 1, 1982·Journal of Neurochemistry·H SoreqM Sokolovsky
Jun 15, 1982·European Journal of Biochemistry·G VauquelinA D Strosberg
Jan 1, 1980·Journal of Supramolecular Structure·F J EhlertH I Yamamura
Sep 1, 1983·British Journal of Pharmacology·N J BirdsallE H Wong
Jul 18, 2002·The Journal of Biological Chemistry·Chi Shing SumJames W Wells

Related Concepts

Metazoa
Brain
Carboptic
Ethylmaleimide
Tissue Membrane
Microsomes
Cholinergic Receptors
Muscarinic Acetylcholine Receptor
Synaptosomes
Rats, Laboratory

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