贝美司琼
- CAS号:40796-97-2
- 英文名:3-TROPANYL-3,5-DICHLOROBENZOATE
- 中文名:贝美司琼
- CBNumber:CB2317210
- 分子式:C15H17Cl2NO2
- 分子量:314.21
- MOL File:40796-97-2.mol
- 熔点 :165 °C
- 沸点 :406.5±45.0 °C(Predicted)
- 密度 :1.34±0.1 g/cm3(Predicted)
- 储存条件 :Sealed in dry,2-8°C
- 溶解度 :0.1 M HCl: slightly soluble
- 形态 :solid
- 酸度系数(pKa) :9.89±0.40(Predicted)
- 颜色 :white
- 水溶解性 :Soluble to 100 mM in DMSO. Insoluble in water. Sparingly soluble in chloroform, and ethanol.
贝美司琼性质、用途与生产工艺
- 生物活性 Bemesetron (MDL 72222) 是一种选择性 5-HT3 受体拮抗剂，IC50 为 0.33 nM 。具有神经保护作用。
-
靶点
5-HT 3 Receptor
0.33 nM (IC 50 )
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体外研究
Blockade of 5-HT 3 receptor with Bemesetron (MDL7222) reduces hydrogen peroxide-induced neurotoxicity in cultured rat cortical cells. Bemesetron (0.01, 0.1 and 1 μM, 15 hours) and Y25130 (0.05, 0.5 and 5 μM) concentration-dependently reduce the H 2 O 2 -induced decrease of MTT reduction showing 74.9±2.4 and 79.0 ±2.5% with 1 μM and 5 μM, respectively, which are maximal effects.
Pretreatment (20 minutes) with Bemesetron (1 μM), Y25130 (5 μM) or MK-801 (10 μM) significantly, but not completely, inhibits the H 2 O 2 -induced elevation of [Ca 2+ ] c .
Bemesetron (1 μM, 15 hours) significantly blocks the H 2 O 2 -induced increase of caspase-3 immunoreactivity.
Cell Viability Assay
Cell Line: Primary cortical neuronal cells Concentration: 0.01-1 μM Incubation Time: 20 minutes (pretreatment); 15 hours (post-incubation) Result: Concentration-dependently reduced the H 2 O 2 -induced decrease of MTT reduction showing 74.9±2.4% with 1 μM, which was maximal effect. Western Blot Analysis
Cell Line: Primary cortical neuronal cells Concentration: 1 μM Incubation Time: 15 hours Result: Blocked significantly the H 2 O 2 -induced increase of caspase-3 immunoreactivity. -
体内研究
Bemesetron (0.1, 1 and 10 mg/kg; i.p.) is used in male adult albino mice. The lowest dose do not cause any significant change in catalepsy. However, Bemesetron (1 mg/kg) causes a significant reduction of catalepsy (from 90 min after Haloperidol), while 10 mg/kg significantly potentiates the phenomenon (from 60 min after Haloperidol). The maximum inhibition of catalepsy (about 75%) occurs at 120 min, and the maximum potentiation (about 4.5-times the control value) occurs at 60 min after Haloperidol.
Animal Model: Male adult albino mice, weighing 26-36 g Dosage: 0.1-10 mg/kg Administration: Intraperitoneally injected, 20 min (pretreatment) +180 min (treatment) Result: Reduced catalepsy significantly at a dose of 1 mg/kg, whilst 10 mg/kg potentiated the phenomenon and 0.1 mg/kg was found to be without effect.
- 更新日期：2024/11/08
- 产品编号：HY-B1541
- 产品名称：Bemesetron
- CAS编号：
- 包装：5 mg
- 价格：400元
- 更新日期：2024/11/08
- 产品编号：HY-B1541
- 产品名称：贝美司琼 Bemesetron
- CAS编号：40796-97-2
- 包装：10mg
- 价格：650元
- 公司名称：TOCRIS-US
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- 国家：英国
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