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Synthesis of 1,5-diaryl-3-methyl-1 H-pyrazolo[4,5-c]isoquinolines and studies of binding to specific peripheral benzodiazepine binding sites

✍ Scribed by Lucia Cecchi; Vittoria Colotta; Fabrizio Melani; Giovanna Palazzino; Guido Filacchioni; Claudia Martini; Gino Giannaccini; Antonio Lucacchini


Book ID
102916159
Publisher
John Wiley and Sons
Year
1989
Tongue
English
Weight
563 KB
Volume
78
Category
Article
ISSN
0022-3549

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✦ Synopsis


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.


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## Abstract Two benzodiazepines, Diazepam and Flunitrazepam, labeled with carbon‐14 in position 5 of the diazepine ring have been synthesized. Use of a condensation between iminochlorides and ^14^C‐benzonitriles, followed by exhaustive methylation of the resulting quinazolines and hydrolyses is des