Title

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

Document Type

Article

Abstract

Phellopterin, a naturally occurring furanocoumarin found in the roots of Angelica dahurica, inhibits [ H]diazepam and ethyl 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H- imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate ([ H]Ro 15-1788) binding to the benzodiazepine site of the rat brain γ-aminobutyric acid(A) (GABA(A)) receptor in vitro with IC values of 400 and 680 nM, respectively. Two other naturally occurring furanocoumarins, byakangelicol and imperatorin were significantly less potent, with IC values for inhibition of [ H]diazepam binding of 8.0 and 12.3 μM, 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. 3 3 3 50 50

Publication Date

11-29-1996

Publication Title

Neuroscience Letters

ISSN

03043940

Volume

219

Issue

3

First Page

151

Last Page

154

PubMed ID

8971802

Digital Object Identifier (DOI)

10.1016/S0304-3940(96)13183-9

https://doi.org/10.1016/S0304-3940(96)13183-9

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