LDN-212320 是兴奋性氨基酸转运体 2(EAAT2)/谷氨酸转运体(GLT-1)的激活剂。它通过上调海马和 ACC 星形胶质细胞 GLT-1 的水平来预防伤害性疼痛。

LDN-212320 is a glutamate transporter EAAT2 activator. It also enhances EAAT2 levels by >6 fold at concentrations< 5 μM after 24 h.

LDN/OSU-0212320 enhanced EAAT2 protein levels and glutamate uptake function but did not affect EAAT1 or EAAT3 protein levels and it also increased EAAT2 protein levels in a dose-dependent (EC50: 1.83 ± 0.27 μM) and time-dependent manner. LDN/OSU-0212320 treatment markedly prevented neuronal loss and degeneration, as assessed by MAP2 immunostaining [2].

After LDN/OSU-0212320(a single i.p.; 40-mg/kg) treatment, EAAT2 protein levels and associated glutamate uptake increased by approximately 1.5- to 2-fold at 2 hours and by approximately 2- to 3-fold between 8 and 24 hours after injection. Even 72 hours after injection, an approximately 1.5-fold increase in EAAT2 protein levels could still be detected (data not shown). LDN/OSU-0212320–induced EAAT2 protein levels and glutamate uptake was dose-dependent [2].

894002-50-7

C17H15N3S

293.39

OSU-0212320;LDN-0212320;LDN/OSU-0212320

DMSO:45 mg/mL (153.38 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years