Tropisetron

Description

Tropisetron is an orally active 5-HT3R antagonist Ki = 5.3 nM as well as being a potent and selective ?7 nicotinic partial agonist EC50 = 1.3 ?M . Tropisetron prevents phosphorylation and activation of the p38 MAPK. Tropisetron inhibits both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibits the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is anti-inflammatory and antiemetic. Tropisetron has antitumor and neuroprotective effects. Tropisetron can be studied in research for diseases including hemorrhagic cystitis, chronic joint inflammation, lung cancer and chronic cerebral hypoperfusion.