Interaction of the alpha-adrenoceptor agonist oxymetazoline with serotonin 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors.

Article Details

Citation

Schoeffter P, Hoyer D

Interaction of the alpha-adrenoceptor agonist oxymetazoline with serotonin 5-HT1A, 5-HT1B, 5-HT1C and 5-HT1D receptors.

Eur J Pharmacol. 1991 Apr 17;196(2):213-6. doi: 10.1016/0014-2999(91)90432-p.

PubMed ID
1678720 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
Oxymetazoline5-hydroxytryptamine receptor 1AProteinHumans
Unknown
Agonist
Details
Oxymetazoline5-hydroxytryptamine receptor 1BProteinHumans
Unknown
Agonist
Details
Oxymetazoline5-hydroxytryptamine receptor 1CProteinRat
Unknown
Partial agonist
Details
Oxymetazoline5-hydroxytryptamine receptor 1DProteinHumans
Unknown
Agonist
Details