A series of isomeric title compds. I (R = H, halo, Me, NO2, Ph, MeO) were prepd. by reaction of the appropriate α-aminophenyl ketone with 2,7-dimethyl-3,8-dinitrodipyrazolo[1,5-a:1',5'-d]pyrazine-4,9-dione [80030-73-5] and tested for their ability to bind to benzodiazepine receptors of rat cerebral cortex synaptic membranes. All I displayed affinities for the benzodiazepine receptors in the micromolar range; in particular I (R = H) [94993-75-6] displayed an affinity for the receptors which was practically comparable to its structural isomer ripazepam, and to that of chlordiazepoxide, although the potency of binding was 2 orders of magnitude less than that of diazepam.
Synthesis and Interaction of 5-(Substituted-phenyl)-3-methyl-6, 7-dihydropyrazolo[4, 3-e][1, 4]diazepin-8(7H)-ones with Benzodiazepine Receptors in Rat Cerebral Cortex
BARALDI, Pier Giovanni;MANFREDINI, Stefano;SIMONI, Daniele;BOREA, Pier Andrea
1985
Abstract
A series of isomeric title compds. I (R = H, halo, Me, NO2, Ph, MeO) were prepd. by reaction of the appropriate α-aminophenyl ketone with 2,7-dimethyl-3,8-dinitrodipyrazolo[1,5-a:1',5'-d]pyrazine-4,9-dione [80030-73-5] and tested for their ability to bind to benzodiazepine receptors of rat cerebral cortex synaptic membranes. All I displayed affinities for the benzodiazepine receptors in the micromolar range; in particular I (R = H) [94993-75-6] displayed an affinity for the receptors which was practically comparable to its structural isomer ripazepam, and to that of chlordiazepoxide, although the potency of binding was 2 orders of magnitude less than that of diazepam.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
