Abstract
2-Oxo-2H-pyrimido[2,1-b]benzothiazole derivatives were found to inhibit the in vitro binding of <sup>3</sup>H-Ro 15-1788 (<sup>3</sup>H-flumazenil) to rat cortical benzodiazepine receptors with IC<sub>50</sub> 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 <sup>3</sup>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<sub>A</sub>/benzodiazepine receptors. Scatchard plot analysis showed that 2-oxo-4-phenyl-2H-pyrimido[2,1-b]benzothiazole is a competitive inhibitor of <sup>3</sup>H-Ro 15-1788 binding to rat brain cortical membrane preparations.
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