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Vol. 282, Issue 1, 278-285, 1997
Department of Pharmaceutical Biology and Pharmacology,
Victorian College of Pharmacy (Monash University), Parkville, Victoria,
Australia, 3052
Functional studies were conducted on guinea pig atrial muscarinic
acetylcholine M2 receptors with the allosteric
modulators heptane-1,7-bis(dimethyl-3
-phthalimidopropyl)ammonium
bromide (C7/3-phth), gallamine and alcuronium to determine
whether these ligands are able to recognize a common accessory site.
The three modulators inhibited the negative inotropic response to
carbachol in this tissue. When used in combination,
C7/3-phth and gallamine or C7/3-phth and
alcuronium gave dose ratios that were either additive or underadditive.
In contrast, the combinations of C7/3-phth or alcuronium
with the competitive antagonists, N-methylscopolamine or atropine,
yielded supra-additive dose ratios. The data could be reconciled with a
model involving a ternary complex between (1) the receptor, (2)
carbachol, N-methylscopolamine or atropine acting at the orthosteric
binding site and (3) C7/3-phth, alcuronium or gallamine
acting at a common, allosteric site with varying degrees of
heterotropic cooperativity.
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