Description
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.
Product information
CAS Number: 144980-29-0
Molecular Weight: 400.49
Formula: C21H24N2O4S
Chemical Name: 2-[4-({[(2R)-3,4-dihydro-2H-1-benzopyran-2-yl]methyl}amino)butyl]-2,3-dihydro-1λ⁶,2-benzothiazole-1,1,3-trione
Smiles: O=C1C2=CC=CC=C2S(=O)(=O)N1CCCCNC[C@H]1CCC2=CC=CC=C2O1
InChiKey: YGYBFMRFXNDIPO-QGZVFWFLSA-N
InChi: InChI=1S/C21H24N2O4S/c24-21-18-8-2-4-10-20(18)28(25,26)23(21)14-6-5-13-22-15-17-12-11-16-7-1-3-9-19(16)27-17/h1-4,7-10,17,22H,5-6,11-15H2/t17-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
In Vivo:
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.
Products are for research use only. Not for human use.
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