| CAS |
No.105826-92-4 |
| 中文名称 |
盐酸托烷司琼 |
| 英文名称 |
Tropisetron Hydrochlorid |
| 别名 |
盐酸托烷司琼;DOPET;3，4-Dihydroxyphenethylalcohol;3-Hydroxytyrosol |
| 分子式 |
C17H21ClN2O2 |
| 分子量 |
320.81 |
| 溶解性 |
Soluble in Water/DMSO(Need ultrasonic) |
| 纯度 |
≥98% |
| 外观(性状) |
Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD02313825 |
| SMILES |
CN1[C@@H]2CC[C@H]1CC(C2)OC(=O)C3=CNC4=CC=CC=C43.Cl |
| InChIKey |
XIEGSJAEZIGKSA-KOQCZNHOSA-N |
| InChI |
InChI=1S/C17H20N2O2.ClH/c1-19-11-6-7-12(19)9-13(8-11)21-17(20)15-10-18-16-5-3-2-4-14(15)16;/h2-5，10-13，18H，6-9H2，1H3;1H/t11-，12+，13 ; |
| PubChem CID |
656664 |
| 靶点 |
5-HT Receptor;α7nAChR |
| 通路 |
Neuronal Signaling;GPCR & G Protein;Membrane Transporter&Ion Channel |
| 背景说明 |
是5-HT3受体拮抗剂和α7-烟碱受体激动剂。 |
| 生物活性 |
Tropisetron， a selective 5-HT3 receptor antagonist.[1] |
| In Vitro |
RGCs pretreated with 100 nM tropisetron before glutamate increased cell survival to an average of 105% compared to controls. 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] |
| In Vivo |
Seven days following Aβ inoculation， control Animals displayed dramatic increase in TNF-α， COX-2， iNOS， NF-κB， active Caspase 3， cytochrome c release and calcineurin Phosphatase activity in the hippocampus. Tropisetron significantly diminished the elevated levels of these markers and reversed the cognitive deficit. Tropisetron was also found to be a potent inhibitor of calcineurin Phosphatase activity. Tropisetron protects against Aβ-induced neurotoxicity in vivo through both 5-HT3 receptor-dependent and independent pathways.[1] |
| 细胞实验 |
Adult pig RGCs were isolated from all other retinal tissue using a two-step panning technique. Once isolated， RGCs were cultured for 3 days under control untreated conditions， in the presence of 500 μM glutamate to induce excitotoxicity， and when tropisetron was applied before glutamate to induce neuroprotection.[2] |
| 动物实验 |
Aβ (1-42) was injected into the hippocampus of male rats. Animals were treated intracerebroventricularly with tropisetron， mCPBG (selective 5-HT3 receptor agonist) or mCPBG plus tropisetron on days 1， 3， 5 and 7. Seven days following Aβ administration， inflammatory markers (TNF-α， COX-2， iNOS and NF-κB)， apoptotic markers (Caspase 3 cytochrome c release) and calcineurin Phosphatase activity were assessed in hippocampus.[1] |
| 数据来源文献 |
[1]. Rahimian R， et al. Tropisetron attenuates amyloid-beta-induced inflammatory and apoptotic responses in rats. Eur J Clin Invest. 2013 Oct;43(10):1039-51.
[2]. Swartz MM， et al. Tropisetron as a neuroprotective agent against glutamate-induced excitotoxicity and mechanisms of action. Neuropharmacology. 2013 Oct;73:111-21. |
| 规格 |
5mg 10mg 25mg 50mg 100mg 200mg |
| 单位 |
瓶 |
中文
英语
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