MDL 72222|40796-97-2|-陌孚医药/Medlife

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MDL 72222

目录号: PC11067 纯度: ≥98%

CAS No. :40796-97-2

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中文名称

MDL 72222

中文别名

3-托烷-3,5-二氯苯甲酸;贝美司琼

英文名称

Benzoic acid,3,5-dichloro-, (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester

英文别名

Benzoic acid,3,5-dichloro-, (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester;1aH,3a,5a,H-tropan-3-yl-3,5-dichloro-benzoate;3-TROPANYL-3,5-DICHLOROBENZOATE;MDL 72222;8-methyl-8-azabicyclo<3.2.1>oct-3-yl 3,5-dichlorobenzoate;bemesetron;Benesetron;TROPANYL 3,5-DICHLOROBENZOATE;tropine 3,5-dichlorobenzoate;tropyl3,5-dichlorobenzoate

Cas No.

40796-97-2

分子式

C₁₅H₁₇NO₂Cl₂

分子量

314.21

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Bemesetron (MDL 72222) is a selective 5-HT₃ receptor antagonist with an IC₅₀ of 0.33 nM. Neuroprotective effect.

性状

Solid

IC50 & Target[1][2]

5-HT₃ Receptor

0.33 nM (IC₅₀)

体外研究(In Vitro)

Blockade of 5-HT₃ 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 H₂O₂-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 H₂O₂-induced elevation of [Ca]_c.
Bemesetron (1 μM, 15 hours) significantly blocks the H₂O₂-induced increase of caspase-3 immunoreactivity.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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 H₂O₂-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 H₂O₂-induced increase of caspase-3 immunoreactivity.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Peters JA, et al. An electrophysiological investigation of the properties of 5-HT₃ receptors of rabbit nodose ganglion neurones in culture. Br J Pharmacol. 1993 Oct;110(2):665-76. [Information]

[2]. Lee HJ, et al. Blockade of 5-HT(3) receptor with MDL7222 and Y25130 reduces hydrogen peroxide-induced neurotoxicity in cultured rat cortical cells. Life Sci. 2005 Dec 5;78(3):294-300. [Information]

[3]. Silva SR, et al. Effects of 5-HT₃ receptor antagonists on neuroleptic-induced catalepsy in mice. Neuropharmacology. 1995 Jan;34(1):97-9. [Information]

溶解度数据

体外研究:

DMSO : 2 mg/mL (6.37 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1826 mL	15.9129 mL	31.8258 mL
5 mM	0.6365 mL	3.1826 mL	6.3652 mL
10 mM	---	---	---

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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