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Interactions between gallamine and muscarinic receptors: allosterism and subpopulation specificity are separate phenomena.

Abstract：

:The quaternary antagonist gallamine discriminates subpopulations of muscarinic receptors in the forebrain and brainstem of the rat and also modulates the binding of other muscarinic ligands via an allosteric mechanism in both brain regions. The calcium channel antagonist verapamil exhibits a similar allosteric effect in both regions (at 100 microM) but does not differentiate the subpopulations that are defined by gallamine. On the other hand, N-methylatropine does not produce the allosteric effect at 100 microM, but shows a high degree of selectivity (about 1,000-fold) for the gallamine-defined subpopulations. These studies indicate that the allosterism and subpopulation specificity of gallamine are separate phenomena and may be examined in isolation by appropriate ligands.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Ellis J,Seidenberg M

doi

10.1016/0014-2999(87)90006-9

subject

Has Abstract

pub_date

1987-11-24 00:00:00

pages

39-44

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(87)90006-9

journal_volume

144

pub_type

杂志文章

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