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MDL 72222 Sale

(Synonyms: 贝美司琼,MDL 72222) 目录号 : GC14083

MDL 72222 (MDL 72222) 是一种选择性 5-HT3 受体拮抗剂,IC50 为 0.33 nM。

MDL 72222 Chemical Structure

Cas No.:40796-97-2

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10 mg
¥1,080.00
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产品描述

Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM[1]. Neuroprotective effect[2].

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[2]. 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 [Ca2+]c[2]. Bemesetron (1 μM, 15 hours) significantly blocks the H2O2-induced increase of caspase-3 immunoreactivity[2].

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[3].

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

Chemical Properties

Cas No. 40796-97-2 SDF
别名 贝美司琼,MDL 72222
化学名 (1R,3s,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 3,5-dichlorobenzoate
Canonical SMILES ClC1=CC(Cl)=CC(C(O[C@H]2C[C@H]3N(C)[C@@H](C2)CC3)=O)=C1
分子式 C15H17Cl2NO2 分子量 314.21
溶解度 Soluble to 100 mM in DMSO 储存条件 Store at RT
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1 mM 3.1826 mL 15.9129 mL 31.8258 mL
5 mM 0.6365 mL 3.1826 mL 6.3652 mL
10 mM 0.3183 mL 1.5913 mL 3.1826 mL
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