PMID: 6979043Mar 1, 1982Paper

Reciprocal modulation of agonist and antagonist binding to muscarinic cholinergic receptor by guanine nucleotide

Proceedings of the National Academy of Sciences of the United States of America
E BurgisserR J Lefkowitz

Abstract

The ability of guanine nucleotide to decrease the binding affinity of agonists but not antagonists has been documented in a number of hormone and neurotransmitter receptor systems. By contrast, recent reports indicate that both agonist and antagonist binding to the muscarinic cholinergic receptors appear to be regulated in a reciprocal fashion by guanine nucleotide. We document two forms of the muscarinic cholinergic receptor in frog heart, which are present in approximately equal proportions and which display high-agonist/low antagonist and low-agonist/high-antagonist affinities, respectively. Guanine nucleotide appears to convert the former type of site into the latter type. These observations can be interpreted in terms of a model for two interconvertible forms of the muscarinic cholinergic receptor reciprocally favored by agonists and antagonists. This model has implications both for the understanding of neurotransmitter-receptor interactions generally and for the nature of the biological effects of receptor antagonists.

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Citations

Jun 11, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·G SimonisR H Strasser
Sep 23, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Massimo IbbaDavid G Lambert
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