| 产品描述: | Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM. Neuroprotective effect |
| 靶点: |
5-HT3 Receptor:0.33 nM (IC50) |
| 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. |
| 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. 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. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.183 ml |
15.913 ml |
31.826 ml |
| 5 mM |
0.637 ml |
3.183 ml |
6.365 ml |
| 10 mM |
0.318 ml |
1.591 ml |
3.183 ml |
| 50 mM |
0.064 ml |
0.318 ml |
0.637 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |