Synthesis and benzodiazepine receptor binding activity of 2, 9-disubstituted quinolino[2', 3'-5, 4](3-pyrazolino)[3, 2-b]purin-4-ones.
2, 9-Disubstituted quinolino[2', 3'-5, 4](3-pyrazolino)pyrimidin-2-ones and purin-4-ones were synthesized and their benzodiazepine receptor activity was evaluated for their ability to displace [(3)H]R015-1788 from its specific binding in bovine brain membranes. Compound 5c caused 83 +/- 8 %inhibition in [(3)H]R015-1788 specific benzodiazepine receptor binding followed by compounds 5f, 5h, and 5i while other analogs were inactive at 10 microM concentration.
El-Sayed
Ola A
OA
Pharmaceutical Chemistry Department, Faculty of Pharmacy, University of Alexandria, Egypt.
Habib
Nargues S
NS
Aboul-Enein
Hassan Y
HY
Costa
Barbara
B
Lucacchini
Antonio
A
Martini
Claudia
C
D000818:Animals; D001921:Brain / Q000378:metabolism; D002417:Cattle; D058787:GABA-A Receptor Antagonists; D011485:Protein Binding; D011688:Purinones / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D013329:Structure-Activity Relationship
D058787:GABA-A Receptor Antagonists; D011688:Purinones