Bemesetron-MDL-72222-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBemesetronCat. No.: HY-B1541CAS No.: 40796-97-2Synonyms: MDL 72222分式: CHClNO分量: 314.21作靶点: 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO

2、: 2 mg/mL (6.37 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1826 mL 15.9129 mL 31.8258 mL5 mM 0.6365 mL 3.1826 mL 6.3652 mL10 mM - - -请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Bemesetron (MDL 72222)种选择性 5-HT3 受体拮抗剂，IC50 为 0.33 nM 1。具有神经保护作 2。IC50

3、 & Target 5-HT3 Receptor0.33 nM (IC50)体外研究Blockade of 5-HT3 receptor with Bemesetron (MDL7222) reduces hydrogen peroxide-induced neurotoxicity1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEin cultured rat cortical cells. Bemesetron (0.01, 0.1 and 1 M, 15 hours) and Y25130 (0.05, 0.5 and 5 M)concen

4、tration-dependently reduce the H2O2-induced decrease of MTT reduction showing 74.92.4 and 79.02.5% with 1 M and 5 M, respectively, which are maximal effects 2.Pretreatment (20 minutes) with Bemesetron (1 M), Y25130 (5 M) or MK-801 (10 M) significantly, but notcompletely, inhibits the H2O2-induced el

5、evation of Ca2+c 2.Bemesetron (1 M, 15 hours) significantly blocks the H2O2-induced increase of caspase-3 immunoreactivity2.Cell Viability Assay 2Cell Line: Primary cortical neuronal cellsConcentration: 0.01-1 MIncubation Time: 20 minutes (pretreatment); 15 hours (post-incubation)Result: Concentrati

6、on-dependently reduced the H2O2-induced decrease of MTT reductionshowing 74.92.4% with 1 M, which was maximal effect.Western Blot Analysis 2Cell Line: Primary cortical neuronal cellsConcentration: 1 MIncubation Time: 15 hoursResult: Blocked significantly the H2O2-induced increase of caspase-3 immuno

7、reactivity.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 anysignificant change in catalepsy. However, Bemesetron (1 mg/kg) causes a significant reduction of catalepsy(from 90 min after Haloperidol), while 10 mg/kg significantly potentiate

8、s the phenomenon (from 60 min afterHaloperidol). The maximum inhibition of catalepsy (about 75%) occurs at 120 min, and the maximumpotentiation (about 4.5-times the control value) occurs at 60 min after Haloperidol 3.Animal Model: Male adult albino mice, weighing 26-36 g 3Dosage: 0.1-10 mg/kgAdminis

9、tration: Intraperitoneally injected, 20 min (pretreatment) +180 min (treatment)Result: Reduced catalepsy significantly at a dose of 1 mg/kg, whilst 10 mg/kg potentiated thephenomenon and 0.1 mg/kg was found to be without effect.REFERENCES1. Peters JA, et al. An electrophysiological investigation of

10、the properties of 5-HT3 receptors of rabbit nodose ganglion neurones in culture.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBr 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 ratcortical 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.McePdfHeightCaution: Product has not been