Title

2-Oxo-2H-pyrimido[2,1-b]benzothiazoles inhibit brain benzodiazepine receptor binding in vitro

Document Type

Article

Abstract

2-Oxo-2H-pyrimido[2,1-b]benzothiazole derivatives were found to inhibit the in vitro binding of H-Ro 15-1788 ( H-flumazenil) to rat cortical benzodiazepine receptors with IC values in the range of 0.7-13 μmol/l. The most potent compound, 2-oxo-4-phenyl-2H-pyrimido[2,1-b]benzothiazole showed a similar potency to inhibit H-Ro 15-1788 binding to membrane preparations of rat brain cortex, cerebellum and hippocampus as well as to various subunit combinations of recombinant human γ-aminobutyric acid(A)/benzodiazepine receptors. Scatchard plot analysis showed that 2-oxo-4-phenyl-2H-pyrimido[2,1-b]benzothiazole is a competitive inhibitor of H-Ro 15-1788 binding to rat brain cortical membrane preparations. Copyright (C) 2000 S. Karger AG, Basel. 3 3 3 3 50

Publication Date

1-1-2000

Publication Title

Pharmacology

ISSN

00317012

Volume

60

Issue

4

First Page

175

Last Page

178

PubMed ID

10828741

Digital Object Identifier (DOI)

10.1159/000028366

https://doi.org/10.1159/000028366

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