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Functional and direct binding studies using subtype selective muscarinic receptor antagonists
Author(s) -
Kunysz E.L.,
Michel Anton D.,
Whiting Roger L.
Publication year - 1988
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.1476-5381.1988.tb10303.x
Subject(s) - pirenzepine , muscarinic acetylcholine receptor , muscarinic acetylcholine receptor m1 , carbachol , muscarinic acetylcholine receptor m2 , muscarinic acetylcholine receptor m3 , muscarinic antagonist , muscarinic acetylcholine receptor m4 , muscarinic acetylcholine receptor m5 , chemistry , muscarinic agonist , endocrinology , oxotremorine , medicine , pharmacology , receptor , biology , biochemistry
1 Muscarinic receptor antagonists were examined in direct binding studies on guinea‐pig cardiac and cortical muscarinic receptors. Pirenzepine, dicyclomine and hexahydroadiphenine were shown to be selective ligands for the putative M 1 ‐muscarinic receptor. 2 Functional affinity estimates of the muscarinic ligands studied was determined from their ability to inhibit carbachol‐stimulated inositol phosphate (IP) accumulation in guinea‐pig cortical slices. 3 The affinity estimates for the inhibition of muscarinic agonist‐stimulated IP accumulation were better correlated with affinity estimates obtained from binding studies on the M 1 than the M 2 muscarinic receptor. 4 These data provide additional evidence, both from direct binding and functional studies, for the presence of M 1 and M 2 muscarinic receptor subtypes.