Eletriptan (UK-116044) 是一种高选择性和口服活性的血清素 5-HT1B 和 5-HT1D 受体激动剂，pKi 值分别为 8.0 和 8.9。
| Cas No. | 143322-58-1 |
| 别名 | 依来曲普坦,UK-116044 |
| Canonical SMILES | CN(CCC1)[C@H]1CC2=CNC3=CC=C(CCS(C4=CC=CC=C4)(=O)=O)C=C32 |
| 分子式 | C22H26N2O2S |
| 分子量 | 382.5 |
| 溶解度 | DMF: 10 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 10 mg/ml,Ethanol: 0.1 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Eletriptan is an agonist of the serotonin (5-HT) receptor types 5-HT1B and 5-HT1D. It inhibits forskolin-induced cAMP accumulation in and induces vasoconstriction of isolated rabbit common carotid artery rings (pD2s = 7.6 and 4.9, respectively), an effect that can be blocked by the 5-HT1B antagonist SB216641 but not the 5-HT1D antagonist BRL15572. Eletriptan preferentially induces constriction of isolated human cerebral over coronary arteries (EC50s = 15.8 and 1,995 nM, respectively). Formulations containing eletriptan have been used in the treatment of migraine headache. |
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