贝美司琼
| 中文名称 | 贝美司琼 |
|---|---|
| 中文同义词 | 贝美司琼;3-托烷-3,5-二氯苯甲酸;化合物 T14526;REL-(1R,5R)-8-甲基-8-氮杂双环[3.2.1]辛-3-基 3,5-二氯本甲酸酯 |
| 英文名称 | 3-TROPANYL-3,5-DICHLOROBENZOATE |
| 英文同义词 | 3-TROPANYL-3,5-DICHLOROBENZOATE;MDL-72222;TROPANYL 3,5-DICHLOROBENZOATE;3,5-dichloro-,8-methyl-8-azabicyclo(3.2.1)oct-3-ylester,endo-benzoicaci;3,5-dichloro-benzoicaci(3-endo)-8-methyl-8-azabicyclo(3.2.1)oct-3-yles;bemesetron;endo-8-methyl-8-azabicyclo(3.2.1)oct-3-yl3,5-dichlorobenzoate;tropyl3,5-dichlorobenzoate |
| CAS号 | 40796-97-2 |
| 分子式 | C15H17Cl2NO2 |
| 分子量 | 314.21 |
| EINECS号 | |
| 相关类别 | Serotonin receptor |
| Mol文件 | 40796-97-2.mol |
| 结构式 |  |
贝美司琼 性质
| 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：微溶 |
| 形态 | 固体 |
| 酸度系数(pKa) | 9.89±0.40(Predicted) |
| 颜色 | 白色 |
| 水溶解性 | Soluble to 100 mM in DMSO. Insoluble in water. Sparingly soluble in chloroform, and ethanol. |
|
5-HT 3 Receptor 0.33 nM (IC 50 ) |
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. |
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. |