Antimigraine drug interactions with 5-hydroxytryptamine1A receptors.
The interactions of four antimigraine drugs with 5-hydroxytryptamine1A and beta-adrenergic receptors were analyzed in rat brain membranes. Methysergide, cyproheptadine, (-)propranolol, and pizotifen display similar affinities (IC50 values, 83 to 280 nM) for 5-hydroxytryptamine1A receptors labeled by [3H]8-hydroxy-N,N-dipropyl-2-aminotetralin. Cyproheptadine, pizotifen, and methysergide are essentially inactive at beta-adrenergic receptors labeled by [3H]dihydroalprenolol (IC50 values, 8,700 to 87,000 nM). By contrast, (-)propranolol is an extremely potent beta-adrenergic agent (IC50, 3 nM). These data indicate that the 5-hydroxytryptamine1A receptor is a common site of action for (-)propranolol and other antimigraine agents.
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000818:Animals; D001921:Brain / Q000187:drug effects*; D003533:Cyproheptadine / Q000494:pharmacology*; D004082:Dihydroalprenolol / Q000378:metabolism; D004347:Drug Interactions; D008784:Methysergide / Q000494:pharmacology*; D010918:Pizotyline / Q000494:pharmacology*; D011433:Propranolol / Q000494:pharmacology*; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000378:metabolism; D013876:Thiophenes / Q000494:pharmacology*
D011985:Receptors, Serotonin; D013764:Tetrahydronaphthalenes; D013876:Thiophenes; D010918:Pizotyline; D003533:Cyproheptadine; D004082:Dihydroalprenolol; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D011433:Propranolol; D008784:Methysergide