产品
编 号：F167020
分子式：C21H24N2O4S
分子量：400.49
分子式：C21H24N2O4S
分子量：400.49
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CAS No: 144980-29-0
产品详情
生物活性：
Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki 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.
体内研究：
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.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.
体外研究：
Repinotan binds with lower affinity to 5-HT7 (Ki = 6 nM), α1- and α2 adrenergic (Ki = 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. 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.
Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki 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.
体内研究：
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.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.
体外研究：
Repinotan binds with lower affinity to 5-HT7 (Ki = 6 nM), α1- and α2 adrenergic (Ki = 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. 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.
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