| 货号 | 21240-50mg |
| 描述 | Tropisetron is an orally-bioavailable antagonist of the serotonin (5-HT) receptor 5-HT3(Ki = 5.3 nM).1,2 Antagonists of 5-HT3, including tropisetron, have been shown to prevent nausea and emesis in patients undergoing chemotherapy in clinical trials.3,4 Tropisetron is also an antagonist of the α9 nicotinic acetylcholine receptor (nAChR; IC50 = 166 nM) and a partial agonist of α7 nAChR (Ki = 6.9 nM).5,6 |
| 别名 | ICS 205-930;SDZ-ICS 930; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Mawe, G.M.,Branchek, T.A. and Gershon, M.D. Peripheral neural serotonin receptors: Identification and characterization with specific antagonists and agonists. Proc. Natl. Acad. Sci. USA 83(24), 9799-9803 (1986). 2.Round, A. and Wallis, D.I. The depolarizing action of 5-hydroxytryptamine on rabbit vagal afferent and sympathetic neurones in vitro and its selective blockade by ICS 205-930. Br. J. Pharmacol. 88(2), 485-494 (1986). 3.Sorbe, B.G.,Höberg, T.,Glimelius, B., et al. A randomized, multicenter study comparing the efficacy and tolerability of tropisetron, a new 5-HT3 receptor antagonist, with a metoclopramide-containing antiemetic cocktail in the prevention of cisplatin-induced emesis. Cancer 73(2), 445-454 (1994). 4.Tricco, A.C.,Blondal, E.,Veroniki, A.A., et al. Comparative safety and effectiveness of serotonin receptor antagonists in patients undergoing chemotherapy: A systematic review and network meta-analysis. BMC Med. 14(1), 216 (2016). 5.Shiina, A.,Shirayama, Y.,Niitsu, T., et al. A randomised, double-blind, placebo-controlled trial of tropisetron in patients with schizophrenia. Ann. Gen. Psychiatry 9(27), (2010). 6.Rothlin, C.V.,Katz, E.,Verbitsky, M., et al. The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors. Mol. Pharmacol. 55(2), 248-254 (1999). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 320.8 |
| 分子式 | C17H20N2O2 • HCl |
| CAS号 | 105826-92-4 |
| 稳定性 | ≥ 2 years |
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