Abstract
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.
MeSH terms
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Adrenergic alpha-Agonists / metabolism
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Adrenergic alpha-Agonists / pharmacology*
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Animals
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Brain / drug effects
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Brain / metabolism
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Cattle
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Clonidine / pharmacology
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In Vitro Techniques
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Kinetics
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Methiothepin / pharmacology
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Oxymetazoline / antagonists & inhibitors
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Oxymetazoline / metabolism
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Oxymetazoline / pharmacology*
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Phentolamine / pharmacology
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Rats
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Receptors, Serotonin / classification
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Receptors, Serotonin / drug effects*
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Receptors, Serotonin / metabolism
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Swine
Substances
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Adrenergic alpha-Agonists
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Receptors, Serotonin
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Methiothepin
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Oxymetazoline
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Clonidine
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Phentolamine