GABAA receptor agent 8_product_DataBase

Bioactivity	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].
Target	GABAA receptor
Invitro	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].
Name	GABAA receptor agent 8
CAS	2376841-54-0
Formula	C19H16N4O
Molar Mass	316.36
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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