GABAA receptor agent 8 

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].

GABAA receptor^[1]

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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

316.36

C₁₉H₁₆N₄O

2376841-54-0

O=C1C=C(CC2=CC=CC=C2)N=C3N1NC(C4=CC=C(C)C=C4)=N3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]