贝美司琼
|
|
|
- CAS号:
- 40796-97-2
- 英文名:
- 3-TROPANYL-3,5-DICHLOROBENZOATE
- 英文别名:
- MDL-72222;MLD-72222;bemesetron;Benesetron;Bemesetron (MDL 72222);tropyl3,5-dichlorobenzoate;MNJNPLVXBISNSX-WDNDVIMCSA-N;tropine 3,5-dichlorobenzoate;TROPANYL 3,5-DICHLOROBENZOATE;3-TROPANYL-3,5-DICHLOROBENZOATE
- 中文名:
- 贝美司琼
- 中文别名:
- 贝美司琼;化合物 T14526;3-托烷-3,5-二氯苯甲酸;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
- CBNumber:
- CB2317210
- 分子式:
- C15H17Cl2NO2
- 分子量:
- 314.21
- MOL File:
- 40796-97-2.mol
|
|
|
贝美司琼化学性质
-
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: 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
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。
|
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.
|
贝美司琼
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-B1541 | Bemesetron | | 1 mg | 300元 |
| 2024/01/25 | HY-B1541 | Bemesetron | | 5 mg | 750元 |
贝美司琼
生产厂家
全球有 66家供应商
贝美司琼国内生产厂家
40796-97-2, 贝美司琼 相关搜索:
- Serotonin receptor
- 药靶配体
- Chromatography
- Drug Standards
- Forensic and Veterinary Standards
- Analytical Chromatography Product Catalog
- Analytical Standards
- C15H17Cl2NO2
- 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
- 化合物 T14526
- 3-托烷-3,5-二氯苯甲酸
- 贝美司琼
- 40796-97-2
- rel-(1R,5R)-8-Methyl-8-azabicyclo[3.2.1]octan-3-yl 3,5-dichlorobenzoate
- Endo-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 3,5-dichlorobenzoate
- Bemesetron (Synonyms: MDL 72222)
- Bemesetron (MDL 72222)
- MNJNPLVXBISNSX-WDNDVIMCSA-N
- (1R,3r,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 3,5-dichlorobenzoate
- Benzoic acid, 3,5-dichloro-, (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
- MLD-72222
- Benesetron
- 3,5-Dichlorobenzoic acid (1β,5β)-8-methyl-8-azabicyclo[3.2.1]octan-3α-yl ester
- (1β,5β)-Tropane-3α-ol 3,5-dichlorobenzoate
- tropine 3,5-dichlorobenzoate
- tropyl3,5-dichlorobenzoate
- endo-8-methyl-8-azabicyclo(3.2.1)oct-3-yl3,5-dichlorobenzoate
- bemesetron
- 3,5-dichloro-benzoicaci(3-endo)-8-methyl-8-azabicyclo(3.2.1)oct-3-yles
- 3,5-dichloro-,8-methyl-8-azabicyclo(3.2.1)oct-3-ylester,endo-benzoicaci
- TROPANYL 3,5-DICHLOROBENZOATE
- MDL-72222
- 3-TROPANYL-3,5-DICHLOROBENZOATE