Repinotan (BAY x 3702 free base) 是一种有效的、选择性的、可透过血脑屏障，并具有口服活性的5-HT1A受体激动剂，Ki值为 0.19 nM (小牛海马)， 0.25 nM (大鼠和人类皮层) 和 0.59 nM (大鼠海马)。Repinotan 对其他相关受体的亲和力较弱。Repinotan 具有强效的神经保护作用。

Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with K i values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects [1].

Repinotan binds with lower affinity to 5-HT7 (K i = 6 nM), α1- and α2 adrenergic (K i = 6 nM and 7 nM, respectively), 5-HT1D (36 nM), dopamine D2 and D4 (48 nM and 91 nM, respectively), σ sites (176 nM) and 5-HT2C (310 nM) receptors [1]. Exposure to repinotan protects rat cortical and hippocampal neurons in cultures from apoptosis induced by 25 nM Staurosporine. After Staurosporine-induced apoptosis, Repinotan, at 50 pM to 1 μM, reduces the release of lactate dehydrogenase, DNA fragmentation, and apoptotic body formation in a concentration-dependent manner [1].

Repinotan (1-100 μg/kg) causes strong, dose-dependent infarct reductions in permanent middle cerebral artery occlusion, transient middle cerebral artery occlusion, and traumatic brain injury paradigms [1]. The half-life of Repinotan in plasma is relatively short (t1/2 = 0.6 h in rat; 0.4 h in rhesus monkeys), and Repinotan is extensively metabolized [1].

144980-29-0

C21H24N2O4S

400.49

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years