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LIGAND BINDING TO MUSCARINIC RECEPTORS IN INTACT LONGITUDINAL MUSCLE STRIPS FROM GUINEA‐PIG INTESTINE
Author(s) -
WARD DAWN,
YOUNG J.M.
Publication year - 1977
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.1476-5381.1977.tb08404.x
Subject(s) - muscarinic acetylcholine receptor , oxotremorine , guinea pig , receptor , ligand (biochemistry) , binding site , antagonist , biophysics , chemistry , endocrinology , medicine , biochemistry , biology
1 The binding of ligands to muscarinic receptors in intact longitudinal muscle strips from guinea‐pig small intestine has been determined by measuring the inhibition of the irreversible binding of [ 3 H]‐propylbenzilylcholine mustard ([ 3 H]‐PrBCM). 2 The IC 50 values for inhibition of [ 3 H]‐PrBCM binding by a given ligand were generally higher in intact strips than those reported for broken‐cell preparations. This effect is probably due, at least in part, to the presence of an access‐limitation factor in the kinetics of the irreversible binding of [ 3 H]‐PrBCM to the intact tissue. 3 The mean Hill coefficients for antagonist binding approached unity, but those for strong agonists were significantly less than unity. There was, with the possible exceptions of hexyltrimethylammonium and oxotremorine, reasonably good agreement with the Hill coefficients reported for brain homogenates.