IMIDAZO[1,2-B]PYRIDAZINES - SYNTHESES AND INTERACTION WITH CENTRAL AND PERIPHERAL-TYPE (MITOCHONDRIAL) BENZODIAZEPINE RECEPTORS

The fundamental chemistry of pyridazines, the syntheses of substituted imidazo[1,2-b]pyridazines (1) (and some related compounds) and the in teraction of the products with central benzodiazepine receptors (CBR) and peripheral-type (mitochondrial) benzodiazepine receptors (PBR) are described. Some of these imidazo[1,2-b]pyridazines had high selective affinity for the central benzodiazepine receptors and others had high selectivity for the peripheral-type (mitochondrial) benzodiazepine re ceptors. The results of structure-activity studies and molecular model ing will be reported. In vivo tests of some compounds which interacted strongly with the central benzodiazepine receptors revealed reasonabl y potent anticonvulsant/anticonflict activity, and some of those which bind selectively to the peripheral-type (mitochondrial) benzodiazepin e receptors are being examined as possible radiopharmaceuticals for im aging of tumors (and other disease states).