GABAA receptor agent 8

Names

[ CAS No. ]:
2376841-54-0

[ Name ]:
GABAA receptor agent 8

Biological Activity

[Description]:

GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

GABAA receptor[1]


[In Vitro]

GABAA receptor agent 8 (compoud 5e) shows anticonvulsant activity with an IC50 of 0.334 µM in 4-AP induced hyper-excitability Model[1]. GABAA receptor agent 8 (0.01-100 µM; 0-140 s) increases GABA-induced activation of GABAA1 receptor in a dose-dependent manner with EC50 12.02 µM.

[In Vivo]

GABAA receptor agent 8 (compoud 5e) shows anticonvulsant activity in mice with an ED50 of 40.95 mg/kg and an TD50 of 372.39 mg/kg[1]. GABAA receptor agent 8 specifically attenuates PTZ-induced seizures but not MES-induced seizures in mice[1].

[References]

[1]. Huang L, et al. Discovery of [1,2,4]-triazolo [1,5-a]pyrimidine-7(4H)-one derivatives as positive modulators of GABAA1 receptor with potent anticonvulsant activity and low toxicity. Eur J Med Chem. 2020 Jan 1;185:111824.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H16N4O

[ Molecular Weight ]:
316.36

Related Compounds