JNJ-61432059是具有口服活性的、选择性的AMPAR的负向调节剂，其对GluA1/γ-8的pIC50值为9.7。在老鼠的海马体中显示出具有时间和剂量依赖性的AMPA受体占用情况，在角膜点燃癫痫动物模型中显示出较强的保护作用。
CAS：2035814-50-5
分子式：C25H22FN5O2
分子量：443.47
纯度：98%
存储：Store at -20°C

Background:

JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models[1]. pIC50: 9.7 (AMPAR)[1].

[1]. Savall BM, et al. Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators. ACS Med Chem Lett. 2018 Dec 26;10(3):267-272.