PMID: 3755789Sep 29, 1986Paper

Effects of N-ethylmaleimide on muscarinic acetylcholine receptor subtype autoradiography and inositide response in rat brain

Life Sciences
E HorváthD G Spencer

Abstract

Chemical modification of brain muscarinic acetylcholine receptors (mAChr) with N-ethylmaleimide (NEM) has been employed to investigate mAChr-subtype distribution and mediation of the inositide response. 3H-Pirenzepine and 3H-oxotremorine-M were used to autoradiographically localize the M1- and M2-AChr subtypes, respectively, in brain slices. M1- and M2-AChr distribution were observed to be distinct from each other. The presence of 1 mM NEM selectively reduced the labeling of M2-, but not of M1-AChr. These data support the notion that NEM converts the high-affinity M2-AChr to a lower affinity state, without affecting the affinity of the M1-AChr. Also, regional analysis indicated that the M1- and M2-AChr subtypes were not interconvertible by NEM. NEM at 30 microM enhanced the carbamylcholine stimulated labeling of phosphatidic acid from 32Pi in nerve endings from rat forebrain, suggesting that the low affinity M2-AChr may mediate at least a part of the inositide response to cholinergic stimulation.

References

Jan 1, 1976·Journal of Supramolecular Structure·N J BirdsallE C Hulme
Feb 1, 1985·Journal of Neurochemistry·L A Van RooijenB W Agranoff
Jun 1, 1984·The Biochemical Journal·M J Berridge
May 16, 1983·Biochemical and Biophysical Research Communications·L A Van RooijenB W Agranoff
Oct 14, 1983·European Journal of Pharmacology·E C HulmeJ M Stockton
Oct 14, 1983·Biochemical and Biophysical Research Communications·T W VickroyW R Roeske
Jul 17, 1981·European Journal of Pharmacology·E C HulmeA S Burgen

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