INTERACTION OF THE ALPHA-ADRENOCEPTOR AGONIST OXYMETAZOLINE WITH SEROTONIN 5-HT1A-RECEPTORS, 5-HT1B-RECEPTORS, 5-HT1C-RECEPTORS AND 5-HT1D-RECEPTORS

被引：38

作者：

SCHOEFFTER, P

HOYER, D

机构：

[1] Preclinical Research, Sandoz Pharma Ltd., CH-4002 Basel

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1991年 / 196卷 / 02期

关键词：

OXYMETAZOLINE; 5-HT; (5-HYDROXYTRYPTAMINE; SEROTONIN); 5-HT1A-RECEPTORS; 5-HT1B-RECEPTORS; 5-HT1C-RECEPTORS; 5-HT1D-RECEPTORS;

D O I：

10.1016/0014-2999(91)90432-P

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 < pK(B) < 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.

引用

页码：213 / 216

页数：4

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