Interaction of the alpha-adrenoceptor agonist oxymetazoline with serotonin 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors.
Oxymetazoline was recognized with nanomolar affinity by 5-HT1A, 5-HT1B and 5-HT1D binding sites and mimicked the effects of 5-hydroxytryptamine with about the same potency and intrinsic activity as the endogenous amine in the corresponding functional tests. At 5-HT1C receptors, oxymetazoline behaved as a mixed agonist-antagonist. Clonidine had minimal activity. Methiothepin antagonized the effects of oxymetazoline (7.4 less than pKB less than 8.8). Thus, oxymetazoline is a full and potent agonist at 5-HT1A, 5-HT1B and 5-HT1D receptors and a partial agonist at 5-HT1C receptors.
Preclinical Research, Sandoz Pharma Ltd., Basel, Switzerland.
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Schoeffter
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Hoyer
D000316:Adrenergic alpha-Agonists / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002417:Cattle; D003000:Clonidine / Q000494:pharmacology; D066298:In Vitro Techniques; D007700:Kinetics; D008719:Methiothepin / Q000494:pharmacology; D010109:Oxymetazoline / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology*; D010646:Phentolamine / Q000494:pharmacology; D051381:Rats; D011985:Receptors, Serotonin / Q000145:classification / Q000187:drug effects* / Q000378:metabolism; D013552:Swine
D000316:Adrenergic alpha-Agonists; D011985:Receptors, Serotonin; D008719:Methiothepin; D010109:Oxymetazoline; D003000:Clonidine; D010646:Phentolamine