Repinotan
- CAS No.
- 144980-29-0
- Chemical Name:
- Repinotan
- Synonyms
- Repinotan (BAYx3702);1,2-Benzisothiazol-3(2H)-one, 2-[4-[[[(2R)-3,4-dihydro-2H-1-benzopyran-2-yl]methyl]amino]butyl]-, 1,1-dioxide
- CBNumber:
- CB32520961
- Molecular Formula:
- C21H24N2O4S
- Molecular Weight:
- 400.49
- MDL Number:
- MOL File:
- 144980-29-0.mol
| Boiling point | 599.5±52.0 °C(Predicted) |
|---|---|
| Density | 1.284±0.06 g/cm3(Predicted) |
| pka | 9.20±0.20(Predicted) |
| FDA UNII | 05PB82Z52L |
Repinotan Chemical Properties,Uses,Production
Uses
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[1].
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[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].
IC 50
5-HT1A Receptor: 0.19 nM (Ki, In calf hippocampus); 5-HT1A Receptor: 0.25 nM (Ki, In rat and human cortex); 5-HT1A Receptor: 0.59 nM (Ki, In rat hippocampus); 5-HT7 Receptor: 6 nM (Ki)
References
[1] A C Berends, et al. A review of the neuroprotective properties of the 5-HT1A receptor agonist repinotan HCl (BAYx3702) in ischemic stroke. CNS Drug Rev. Winter 2005;11(4):379-402. DOI:10.1111/j.1527-3458.2005.tb00055.x
Repinotan Preparation Products And Raw materials
Raw materials
Preparation Products
Repinotan Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 32281 | 58 |
| Beijing HuaMeiHuLiBiological Chemical | 010-56205725 | waley188@sohu.com | China | 12335 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3467 | 58 |
| Shandong Territorial sea Biological Technology Co., LTD | 15092083467 | 18660263263@163.com | China | 2802 | 58 |
| Suzhou Zhixin Biotechnology Co., Ltd. | 0512-65118909 15162312715 | sales@szzxbio.com | China | 4726 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 20622 | 58 |
