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
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
收藏
页码:351 / 356
页数:6
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