昂丹司琼
更新时间：2022-07-27 14:43:59
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常用名 |
昂丹司琼 |
CAS号 |
99614-02-5 |
| 价钱 |
￥需询单/10mg ￥需询单/25mg ￥需询单/50mg ￥需询单/100mg |
纯度 |
99.9% |
| 备货期 |
需询单 |
库存 |
现货 |
产物详情（用途，包装等）
用途：
Ondansetron(GR38032) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.IC50 Value: Target: 5- HT3 Receptorin vitro: 5-HT evoked transient inward currents (EC50 = 3.4 microM; Hill coefficient = 1.8) that were blocked by the 5-HT3 receptor antagonist ondansetron (IC50 = 103 pM) [1]. The 5-HT3A receptor antagonist ondansetron (0.3 nM) reversibly inhibited the 5-HT (30 microM) signal by 70% and at 3 nM it abolished the response [2].in vivo: Acute ondansetron administration at the lowest dose (0.1 mg/kg, IP) tested had no effect, while other doses (0.33 and 1 mg/kg, IP) produced improvements in auditory gating [3]. Different doses of ondansetron were injected intraperitoneally (i.p.) at fixed times during the day to determine both the sublethal (TD50) and lethal (LD50) doses, which were, respectively, 3.7 +/- 0.6 mg/kg and 4.6 +/- 0.5 mg/kg [4]. ondansetron (0.25-1.0 mg/kg, subcutaneously) given before the challenge dose of ethanol (2.4 g/kg, intraperitoneally) injection, significantly and dose dependently attenuated the expression of sensitization. In addition, ondansetron (1.0 mg/kg, subcutaneously) given before ethanol injection on days 1, 4, 7, and 10 significantly blocked the development (days 1, 4, 7, and 10), and expression (day 15) of sensitization to the locomotor stimulant effect of ethanol injection [5]. Toxicity: Ondansetron may be safe in lower doses used to prevent nausea and vomiting in radiation treatment or postoperatively. However, as there is a report that a lower dose of ondansetron prolonged the QT interval in healthy volunteers, this needs to be clarified by the FDA [6].
作用：
本品为一种高度选择性的5-羟色胺3（5-HT3）受体拮抗剂，能抑制由化疗和放疗引起的恶心吐逆，其作用机制尚不完全清晰。一样平常以为，化疗和放疗可引起小肠的嗜铬细胞释放5-HT3，并通过5-HT3受体引起迷走传着迷经兴奋从而导致吐逆反射，而昂丹司琼可阻断这一反射发生。 昂丹司琼本品不影响行为效率，无镇静作用，且不改变血浆催乳素水平。口服吸收迅速，单剂量8mg，tmax为1.5小时，Cmax为30ng/ml，口服生物行使度约为60%；Vd约为140L，t1/2β约3小时；血浆卵白连系率为70%～76%。主要自肝脏代谢，代谢产物主要自粪和尿渗出，50%以内的本品以真相自尿倾轧。暮年人由于代谢减慢，服用本品后消除半衰期延伸（5小时），同时口服生物行使度提高（65%）；严重肝功效障碍患者系统祛除率可显著削减，消除半衰期可延伸至15～32小时，同时口服生物行使度可靠近100%。 本品是强效、高选择性的5—HT3受体拮抗剂，有强镇吐作用。化疗药物和放射治疗可造成小肠释放5—HT，经由5—HT3受体激活迷走神经的传入支，触发吐逆反射。本品能阻断这一反射的触发。迷走神经传入支的激动也可引起位于第四脑室底部Postrema区的5—HT释放，从而经由中枢机制而增强。本品对化疗、放疗引起的恶心、吐逆,系通过拮抗位于周围和中枢神经局部的神经原的5—HT受体而施展止吐作用。手术后恶心、吐逆的作用机制未明，但可能类似细胞毒类致恶心、吐逆的配合途径而诱发。本品尚能抑制因阿片诱导的恶心，其作用机理尚不清晰。由于本品的高选择性作用，因而不具有其他止吐药的副作用，如锥体外系反映、太过镇静等。
物理化学性子：
CAS号：99614-02-5
常用中文名：昂丹司琼
常用英文名：Ondansetron
分子式：C18H19N3O
分子量：293.363
密度：1.3±0.1 g/cm3
沸点：546.0±30.0 °C at 760 mmHg
熔点：231 - 232ºC
闪点：284.0±24.6 °C
储存条件：−20°C |
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