GABAA receptor agent 7

Names

[ Name ]:
GABAA receptor agent 7

Biological Activity

[Description]:

GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 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

[In Vitro]

GABAA receptor agent 7 (compoud 5c) shows anticonvulsant activity with an IC50 of 0.452 µM in 4-AP induced hyper-excitability Model[1]. GABAA receptor agent 7 (0.01-100 µM; 0-140 s) increases GABA-induced activation of GABAA1 receptor in a dose-dependent manner with EC50 3.08 µM[1].

[In Vivo]

GABAA receptor agent 7 shows anticonvulsant activity in mice with an ED50 of 31.81 mg/kg and an TD50 of 547.89 mg/kg[1]. GABAA receptor agent 7 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 ]:
C₁₈H₁₃ClN₄O

[ Molecular Weight ]:
336.78

Related Compounds

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