The affinity to the brain dopamine D-1 receptor in vitro of triprenyl phenols isolated from the fruit bodies of Albatrellus ovinus

被引：15

作者：

Dekermendjian, K ^{[1
]}

Shan, R ^{[1
]}

Nielsen, M ^{[1
]}

Stadler, M ^{[1
]}

Sterner, O ^{[1
]}

Witt, MR ^{[1
]}

机构：

[1] LUND UNIV, DIV ORGAN CHEM 2, S-22100 LUND, SWEDEN

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1997年 / 32卷 / 04期

关键词：

CNS; dopamine D-1 receptor; Albatrellus ovinus; triprenyl phenol;

D O I：

10.1016/S0223-5234(97)89088-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Six triprenyl phenols that inhibit the in vitro binding of H-3-SCH 23390 to the dopamine D-1 receptor subfamily in rat striatal brain membranes were isolated from extracts of the edible mushroom Albatrellus ovinus. The compounds, of which scutigeral 1a, ilicicolin B 3, neogrifolin 5a and grifolin 6 are known while ovinal 2 and ovinol 4a are new, were isolated by chromatography and their structures were determined by spectroscopic techniques The IC50 values of the most potent compound, scutigeral 2a, is 2.6 mu M and it was shown that it decreases the binding affinity of H-3-SCH 23390 in a competitive manner. Compounds 1-5 showed no inhibition on the binding of H-3-spiperone to the dopamine D-2 receptor subfamily, indicating that these compounds interact selectively with the dopamine D-1 receptor subfamily.

引用

页码：351 / 356

页数：6

共 14 条

[1] INHIBITION OF KAINIC ACID-BINDING TO GLUTAMATE RECEPTORS BY EXTRACTS OF GASTRODIA [J].