Binding studies on two functional cardioselective antimuscarinic compounds.
Vecuronium and himbacine are antimuscarinic compounds which in functional studies exhibited a ca 6- and 10-fold higher potency at cardiac muscarinic receptors than at ileal muscarinic receptors. However in binding studies both compounds failed to differentiate between [3H](-)-QNB binding sites in guinea-pig atrial and ileal muscle homogenates. In the latter experiments, the dissociation constants of vecuronium in atria and ileum and that of himbacine in ileum were lower than the values determined functionally. The basis for the lack of cardioselectivity in binding studies is not known. These compounds add to the list of functional cardioselective muscarinic receptor antagonists that failed to display selectivity in binding studies with [3H](-)-QNB.
D000470:Alkaloids / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D005663:Furans; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects*; D006325:Heart Atria / Q000378:metabolism; D007082:Ileum / Q000378:metabolism; D066298:In Vitro Techniques; D009281:Naphthalenes; D010276:Parasympatholytics / Q000378:metabolism* / Q000494:pharmacology; D010880:Piperidines; D014673:Vecuronium Bromide / Q000378:metabolism* / Q000494:pharmacology
D000470:Alkaloids; D005663:Furans; D009281:Naphthalenes; D010276:Parasympatholytics; D010880:Piperidines; D014673:Vecuronium Bromide; C048172:himbacine