1135278-54-4
中文名稱
化合物 T10781
英文名稱
CGP 78608 hydrochloride
CAS
1135278-54-4
分子式
C11H14BrClN3O5P
分子量
414.58
MOL 文件
1135278-54-4.mol
1135278-54-4 結(jié)構(gòu)式
常見(jiàn)問(wèn)題列表
生物活性
CGP 78608 hydrochlorid 是 NMDA 受體甘氨酸結(jié)合位點(diǎn)的一種高效選擇性拮抗劑，IC50 為 6 nM。CGP 78608 作為 GluN1/GluN3A 介導(dǎo)的甘氨酸電流的增強(qiáng)劑，EC50 值為 26.3 nM。具有抗驚厥活性。體外研究
CGP-78608 hydrochloride decreases glycine sensitivity of GluN1/GluN3A receptors through an inter-subunit allosteric effect between GluN1 and GluN3A agonist-binding domain (ABD) sites.
CGP 78608 hydrochloride reduces or abolishes ammonia-dependent cGMP synthesis which is a causative factor of ammonia neurotoxicity.
體內(nèi)研究
CGP-78608 hydrochloride displays potent anticonvulsant effects after i.p. administration in the electroshock-induced convulsions assay in mice.