The effect of p-chloromercuribenzoate on structure-binding relationships of muscarinic receptors in the rat cerebral cortex.

Abstract:

:Muscarinic receptors in the rat cerebral cortex, reacted with p-chloromercuribenzoate (PCMB) under different conditions (Phase I and II), have modified binding sites. These exhibit remarkable changes in the structural dependence of the binding of drugs. In Phase I, the structure-binding profile of agonists for both the high and low affinity agonist sites are altered. In Phase II, the structure-binding profile of antagonists is also observed. 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. Of the 16 agonists examined, only pilocarpine has a heterogeneous binding profile in Phase II, the dispersity of binding being increased. The changes in binding properties of the receptors are discussed in terms of general theories of drug-receptor interactions.

journal_name

Br J Pharmacol

authors

Birdsall NJ,Burgen AS,Hulme EC,Wong EH

doi

10.1111/j.1476-5381.1983.tb11066.x

subject

Has Abstract

pub_date

1983-09-01 00:00:00

pages

197-204

issue

1

eissn

0007-1188

issn

1476-5381

journal_volume

80

pub_type

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