贝美司琼

生物活性靶点体外研究体内研究贝美司琼试剂级价格

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

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.

安全信息

危险品标志 :T
危险类别码 :25
安全说明 :36
WGK Germany :3
RTECS号 :DG7580000

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 )

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.