BENZODIAZEPINE RECEPTOR LIGANDS - SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF 3-SUBSTITUTED, 7-SUBSTITUTED AND 8-SUBSTITUTED [5,1-C][1,2,4]BENZOTRIAZINES AND 5-OXIDE DERIVATIVES .1.

A new series of 3-, 7- and 8-substituted pyrazolo[5,1-c][1,2,4]benzotr iazine 5-oxides and a series of pyrazolo[5,1-c][1,2,4]benzotriazines w ere synthesized and their benzodiazepine receptor affinities were eval uated in vitro. A study of structure-affinity relationships within the series is briefly discussed, considering the role of various substitu ents at the 3-, 7- and 8-positions and the role of N-5-oxide. Compound s 1b, 1c, 1cR, 4c, 4cR, 9d, 12d and 12dR were evaluated in vivo for th eir anticonvulsant effects.