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The effects of p ‐chloromercuribenzoate on muscarinic receptors in the cerebral cortex
Author(s) -
Birdsall N.J.M.,
Burgen A.S.V.,
Hulme E.C.,
Wong E.H.F.
Publication year - 1983
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1983.tb11065.x
Subject(s) - dithiothreitol , muscarinic acetylcholine receptor , pirenzepine , chemistry , binding site , receptor , agonist , biophysics , ligand (biochemistry) , biochemistry , biology , enzyme
1 The action of p ‐chloromercuribenzoate (PCMB) on the ligand binding properties of the muscarinic receptors in the rat cerebral cortex has been examined. 2 At low concentrations, PCMB produces a selective change in the binding of agonists without any effect on the binding of antagonists. 3 At higher concentrations, the structure‐binding profile for binding antagonists is changed. The affinity of agonists is greatly reduced and the heterogeneity of binding eliminated. 4 The effects of both high and low concentrations of PCMB can be reversed by dithiothreitol. 5 Inactivation of receptors proceeds in parallel and is kinetically complex. It can only be partially reversed by dithiothreitol. 6 Evidence is presented connecting the low affinity agonist binding site with the high affinity pirenzepine binding site. 7 The changes produced by PCMB have been interpreted in terms of the modification of receptor conformation.