2376841-54-0

2376841-54-0 structure
2376841-54-0 structure
  • Name: GABAA receptor agent 8
  • Chemical Name: GABAA receptor agent 8
  • CAS Number: 2376841-54-0
  • Molecular Formula: C19H16N4O
  • Molecular Weight: 316.36
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
  • Create Date: 2022-06-25 22:33:38
  • Modify Date: 2024-01-06 21:15:55
  • 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].

Name GABAA receptor agent 8
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
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.

Molecular Formula C19H16N4O
Molecular Weight 316.36