2-Oxo-2H-pyrimido[2,1-b]benzothiazoles inhibit brain benzodiazepine receptor binding in vitro
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
Digital Object Identifier (DOI)
Ai, Jinglu; Wang, Xiaomei; Wahe, Helen; Tanee Fomum, Zacharias; Sterner, Olov; Nielsen, Mogens; and Witt, Michael Robin, "2-Oxo-2H-pyrimido[2,1-b]benzothiazoles inhibit brain benzodiazepine receptor binding in vitro" (2000). Neurobiology. 1016.