常用名 盐酸托烷司琼
英文名 Tropisetron hydrochloride
CAS号 105826-92-4
沸点 448.5ºC at 760 mmHg
熔点 283-285ºC
分子式 C17H21ClN2O2
分子量 320.814
闪点 225ºC
精确质量 320.129150
PSA 41.90000
LogP 2.83000
外观性状 固体;White to Light yellow powder to crystal
蒸汽压 3.09E-08mmHg at 25°C
储存条件 2-8°C
水溶解性 可溶于:甲醇
"Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
IC50 value: 70.1 ± 0.9 nM
Target: 5-HT3 receptor; α7-nicotinic receptor
in vitro: Retinal ganglion cells(RGCs) pretreated with 100 nM tropisetron before glutamate increased cell survival to an average of 105% compared to controls. Inhibition studies using the alpha7 nAChR antagonist, MLA (10 nM), support the hypothesis that tropisetron is an effective neuroprotective agent against glutamate-induced excitotoxicity; mediated by α7 nAChR activation. Tropisetron had no discernible effects on pAkt levels but significantly decreased p38 MAPK levels associated with excitotoxicity from an average of 15 ng/ml to 6 ng/ml [2]. Tropisetron, but not granisetron, significantly inhibits the phosphatase activity of calcineurin, over-expresses the CB(1) receptors at both transcriptional and protein levels, and reduces cAMP content in cerebellar granule neurons (CGNs) [4].
in vivo: Animals were treated intracerebroventricularly with tropisetron, mCPBG (selective 5-HT3 receptor agonist) or mCPBG plus tropisetron on days 1, 3, 5 and 7. Tropisetron significantly diminished the elevated levels of these markers and reversed the cognitive deficit. Interestingly, tropisetron was also found to be a potent inhibitor of calcineurin phosphatase activity [1]. tropisetron (5mg/kg/day) plus mCPBG (10mg/kg/day), and granisetron (5mg/kg/day) intraperitoneally on days 3-35 post-immunization. Treatment with tropisetron and granisetron markedly suppressed the clinical symptoms of EAE (p<0.001) and reduced leukocyte infiltration as well as demyelination in the spinal cord (p<0.05) [3]."
包装:100mg,500mg,1g,10g,100g以及kg级别等公斤级大包装
纯度:99%
配送:惯例下常温**
包装:袋装
厂家:西安齐岳生物科技有限公司
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