Synthesis of 1,5-diaryl-3-methyl-1H-pyrazolo[4,5-c]isoquinolines and studies of binding to specific peripheral benzodiazepine binding sites.
Some 1,5-diaryl-3-methyl-1H-pyrazolo[4,5-c]isoquinolines were synthesized and tested for their ability to displace [3H]clonazepam or [3H]Ro 5-4864 from their specific binding on the central and peripheral benzodiazepine receptors. None of the tested compounds showed any activity as central binding inhibitors, while most of them were specific as peripheral binding inhibitors, although they were not very potent.
Cecchi
L
L
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
Colotta
V
V
Melani
F
F
Palazzino
G
G
Filacchioni
G
G
Martini
C
C
Giannaccini
G
G
Lucacchini
A
A
D000818:Animals; D001570:Benzodiazepinones / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003292:Convulsants / Q000494:pharmacology; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000378:metabolism; D008297:Male; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000378:metabolism; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*
D001570:Benzodiazepinones; D003292:Convulsants; D007546:Isoquinolines; D011720:Pyrazoles; D011963:Receptors, GABA-A; C028513:4'-chlorodiazepam