| CAS |
89565-68-4 |
| Chinese Name |
托烷司琼 |
| English Name |
Tropisetron |
| Synonyms |
ICS 205-930;Tropisetronum;SDZ-ICS-930 free base |
| Molecular Formula |
C17H20N2O2 |
| Molecular Weight |
284.35 |
| Solubility |
Soluble in Water/DMSO(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00864399 |
| SMILES |
CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 |
| InChIKey |
ZNRGQMMCGHDTEI-FUNVUKJBSA-N |
| InChI |
InChI=1S/C17H20N2O2/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/t11-，12+，13? |
| PubChem CID |
656665 |
| Target Point |
5-HT Receptor;nAChR |
| Passage |
Neuronal Signaling；GPCR & G Protein;Membrane Transporter&Ion Channel |
| Background |
It is a 5-HT3 receptor antagonist and also an α7-nicotinic receptor agonist. |
| Biological Activity |
Tropisetron 是一种α7烟碱受体激动剂，同时也是5-羟色胺（5-HT）3 受体拮抗剂，IC50为70.1 nM，具有镇痛和抗炎活性。[1] |
| IC50 |
5-HT3 Receptor：70.1μM(IC50)[1] |
| In Vitro |
Tropisetron specifically inhibited both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibited both the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is a potent inhibitor of PMA plus ionomycin-induced NF-(kappa)B activation.[2] The anti-inflammatory effects of the 5-HT receptor antagonist tropisetron，are mediated by a selective inhibition of pro-inflammatory cytokines at the post-transcriptional level. Tropisetron prevents the phosphorylation and thus activation of the p38 MAPK.[3] |
| In Vivo |
Tropisetron failed to reduce cerebral infarction. Animals receiving tropisetron showed a significant increase(p < 0.05)in neurological deficits and mortality rate. Blockade of 5-HT3 receptors with tropisetron worsens ischemic brain injury induced by pMCAO.[4] |
| Animal Experiment |
Two different doses of tropisetron(5 and 10 mg/kg)or vehicle were administered intraperitoneally 30 min before pMCAO. Neurological deficit scores，mortality rate and infarct volume were determined 24 h after permanent focal cerebral ischemia.[4] |
| Data Literature Source |
[1]. Macor JE，et al. The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist. Bioorg Med Chem Lett. 2001 Feb 12;11(3):319-21.
[2]. Vega Lde L，et al. The 5-HT3 receptor antagonist tropisetron inhibits T cell activation by targeting the calcineurin pathway. Biochem Pharmacol. 2005 Aug 1;70(3):369-80.
[3]. Stratz C，et al. The anti-inflammatory effects of the 5-HT receptor antagonist tropisetron are mediated by the inhibition of p38 MAPK activation in primary human monocytes. Int Immunopharmacol. 2012 Aug;13(4):398-402.
[4]. Candelario-Jalil E，et al. Detrimental effects of tropisetron on permanent ischemic stroke in the rat. BMC Neurosci. 2008 Feb 6;9:19. doi: 10.1186/1471-2202-9-19. |
| Unit |
Bottle |
| Specification |
5mg |
English
中文
Manual Download
