Characterisation of the furanocoumarin phellopterin as a rat brain benzodiazepine receptor partial agonist in vitro

被引：24

作者：

Dekermendjian, K ^{[1
]}

Ai, JL ^{[1
]}

Nielsen, M ^{[1
]}

Sterner, O ^{[1
]}

Shan, RD ^{[1
]}

Witt, MR ^{[1
]}

机构：

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

来源：

NEUROSCIENCE LETTERS | 1996年 / 219卷 / 03期

关键词：

central nervous system; gamma-aminobutyric acid(A) benzodiazepine receptors; partial agonist; furanocoumarins; phellopterin;

D O I：

10.1016/S0304-3940(96)13183-9

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Phellopterin, a naturally occurring furanocoumarin found in the roots of Angelica dahurica, inhibits [H-3]diazepam and ethyl 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate ([H-3]Ro 15-1788) binding to the benzodiazepine site of the rat brain gamma-aminobutyric acid(A) (GABA(A)) receptor in vitro with IC50 values of 400 and 680 nM, respectively. Two other naturally occurring furanocoumarins, byakangelicol and imperatorin were significantly less potent, with IC50 values for inhibition of [H-3]diazepam binding of 8.0 and 12.3 mu M, respectively. Scatchard plot analysis showed that the inhibitory activity of phellopterin was due to competitive inhibition of the benzodiazepine ligand binding. The results of GABA- and t-butylbicyclophosphorothionate (TBPS)-shift assays suggest that phellopterin is a partial agonist of the central benzodiazepine receptors in vitro.

引用

页码：151 / 154

页数：4

共 14 条

[1] LIGANDS FOR BENZODIAZEPINE RECEPTORS WITH POSITIVE AND NEGATIVE EFFICACY [J].