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The effect of p‐chloromercuribenzoate on structure‐binding relationships of muscarinic receptors in the rat 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.tb11066.x
Subject(s) - pirenzepine , muscarinic acetylcholine receptor , chemistry , pilocarpine , agonist , binding site , receptor , biophysics , oxotremorine , antagonist , cerebral cortex , pharmacology , biochemistry , endocrinology , neuroscience , biology , epilepsy
1 Muscarinic receptors in the rat cerebral cortex, reacted with p‐chloromercuribenzoate (PCMB) under different conditions (Phase I and II), have modified binding sites. 2 These exhibit remarkable changes in the structural dependence of the binding of drugs. 3 In Phase I, the structure‐binding profile of agonists for both the high and low affinity agonist sites are altered. 4 In Phase II, the structure‐binding profile of antagonists is also observed. 5 In Phase II, the ability of potent agonists to discriminate between sub‐classes of agonist binding sites is eliminated. There is also a loss of heterogeneity in the binding of the selective antagonist pirenzepine. 6 Of the 16 agonists examined, only pilocarpine has a heterogeneous binding profile in Phase II, the dispersity of binding being increased. 7 The changes in binding properties of the receptors are discussed in terms of general theories of drug‐receptor interactions.