CAS NO: | 40796-97-2 |
包装: | 10mg |
市场价: | 1080元 |
Cas No. | 40796-97-2 |
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 |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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: |