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.
1985
Baraldi, Pier Giovanni; Manfredini, Stefano; Periotto, Vittorio; Simoni, Daniele; Guarneri, Mario; Borea, Pier Andrea
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/460358
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