5,6,7,8,9,10-Hexahydro-2-(4-methoxyphenyl)cyclohepta[b]pyrazolo[3,4-d]pyridin-3(2H)-one

Uses

CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 can be used for the research of pentylenetetrazol-induced seizures[1].

Definition

ChEBI: LSM-3520 is a member of pyrazoles and a ring assembly.

Biological Activity

Selective, partial agonist for the benzodiazepine binding site of the GABA A receptor. Potently inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors (IC 50 = 1.3 nM) and displays weak affinity for peripheral benzodiazepine (IC 50 = 0.68 - 2.25 μ M) and GABA binding sites (IC 50 > 10000 μ M). Displays anxiolytic activity in vivo following oral administration.

References

[1] Williams M, et al. CGS 20625, a novel pyrazolopyridine anxiolytic. J Pharmacol Exp Ther. 1989 Jan;248(1):89-96. PMID:2563294