Diphenylalkylamine calcium antagonists interact with alpha-adrenoceptor binding sites in aortic membranes.
Some interactions of calcium antagonists with [3H]prazosin and [3H]yohimbine binding sites were investigated in bovine aorta membranes. Diphenylalkylamines (flunarizine, cinnarizine and bepridil) acted as competitors of the two ligands with Ki values in the microM range. With the exception of verapamil, reference compounds (nifedipine, Bay-K 8644, diltiazem) and the peripheral benzodiazepine receptor antagonist PK 11195 did not displace the ligands. The apparent affinity of the diphenylalkylamines for alpha-adrenoceptor was consistent with the concentrations producing vasodilatation.
D000818:Animals; D001013:Aorta, Thoracic / Q000378:metabolism; D015764:Bepridil; D001667:Binding, Competitive / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D002417:Cattle; D002936:Cinnarizine / Q000031:analogs & derivatives* / Q000494:pharmacology; D066298:In Vitro Techniques; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D009131:Muscle, Smooth, Vascular / Q000378:metabolism*; D011224:Prazosin / Q000378:metabolism; D011759:Pyrrolidines / Q000494:pharmacology; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects* / Q000378:metabolism; D015016:Yohimbine / Q000378:metabolism
D002121:Calcium Channel Blockers; D011759:Pyrrolidines; D011942:Receptors, Adrenergic, alpha; D015016:Yohimbine; D002936:Cinnarizine; D015764:Bepridil; D011224:Prazosin