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  • Title: Dual effect of N-ethylmaleimide on agonist binding to bovine heart muscarinic receptors.
    Author: Vauquelin G, Vanderheyden P, Ebinger G.
    Journal: Arch Int Pharmacodyn Ther; 1990; 307():5-10. PubMed ID: 2095714.
    Abstract:
    M2-Muscarinic acetylcholine receptors are identified in membrane preparations from calf heart by binding of [3H]quinuclidinyl benzilate. The alkylating reagent N-ethylmaleimide provokes two major changes in the competition binding characteristics of the agonist carbachol. At low temperature (0 degrees C), the reagent provokes a rightward shift and steepening of the competition curve in a GTP-like manner. This can be attributed to alkylation of the adenylate cyclase-regulating component Gi. At 30 degrees C, the reagent also increases the affinity of the agonist for the receptor, presumably by direct alkylation of the receptor.
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