6-BROMO-3'-NITROFLAVONE, A NEW HIGH-AFFINITY BENZODIAZEPINE RECEPTOR AGONIST RECOGNIZES 2 POPULATIONS CEREBRAL CORTICAL BINDING-SITES

The synthesis and biochemical characterization of 6-bromo-3'-nitroflav one (1) is presented. Compound 1 has higher affinity for cerebellar an d cerebral cortical than for striatal, hippocampal, or spinal cord ben zodiazepine receptors (BDZ-Rs). In the cerebra) cortex it recognizes t wo populations of binding sites (K(i)s 1.2 nM and 15.5 nM, respectivel y), and at doses of 0.01 to 0.3 mg/kg, ip produces anxiolytic effects in mice. (C) 1997, Elsevier Science Ltd.