Tropisetron(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
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. We also observed that tropisetron is a potent inhibitor of PMA plus ionomycin-induced NF-(kappa)B activation but in contrast TNF(alpha)-mediated NF-(kappa)B activation was not affected by this antagonist. Tropisetron prevents the phosphorylation and thus activation of the p38 MAPK, which is involved in post-transcriptional regulation of various cytokines.
in vivo: 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.

5-HT Receptor
Setiptiline
Sumatriptan succinate
Tandospirone
Tianeptine
Tianeptine sodium
Trazodone
Tropisetron
Urapidil
Venlafaxine
Vilazodone
Vortioxetine
WAY-100635
Ziprasidone
Zolmitriptan