Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Repinotan (BAY x 3702 free base) is an effective, selective, blood-brain barrier permeable, oral active 5-HT1A receptor agonist. The Ki values of Repinotan are 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex) and 0.59 nM (rat hippocampus). Repinotan shows pronounced neuroprotective effect.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | In stock | $ 1,520.00 | |
50 mg | In stock | $ 1,980.00 | |
100 mg | In stock | $ 2,500.00 |
Description | Repinotan (BAY x 3702 free base) is an effective, selective, blood-brain barrier permeable, oral active 5-HT1A receptor agonist. The Ki values of Repinotan are 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex) and 0.59 nM (rat hippocampus). Repinotan shows pronounced neuroprotective effect. |
In vitro | Repinotan exhibits differential affinity across several receptor types, demonstrating lower binding affinities to 5-HT7 (K i = 6 nM), α1- and α2 adrenergic receptors (K i = 6 nM and 7 nM, respectively), 5-HT1D (36 nM), dopamine D2 and D4 receptors (48 nM and 91 nM, respectively), σ sites (176 nM), and 5-HT2C receptors (310 nM) [1]. In experiments, repinotan has shown protective effects against apoptosis in rat cortical and hippocampal neuron cultures exposed to 25 nM Staurosporine. Specifically, at concentrations ranging from 50 pM to 1 μM, repinotan effectively reduces lactate dehydrogenase release, DNA fragmentation, and apoptotic body formation in a concentration-dependent manner following Staurosporine-induced apoptosis [1]. |
In vivo | Repinotan, administered in doses ranging from 1-100 μg/kg, induces significant, dose-dependent reductions in infarcts across models of permanent and transient middle cerebral artery occlusion, as well as in traumatic brain injury paradigms. Notably, Repinotan exhibits a relatively short half-life in plasma (t1/2 = 0.6 hours in rats; 0.4 hours in rhesus monkeys) and undergoes extensive metabolism. |
Molecular Weight | 400.49 |
Formula | C21H24N2O4S |
CAS No. | 144980-29-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Repinotan 144980-29-0 inhibitor inhibit