Description
Tropisetron is an antagonist at 5-HT3 receptors and partial agonist at α7 nicotinic acetylcholine receptors (nAChRs) that exhibits antiemetic, analgesic, anti-inflammatory, nephroprotective, neuroprotective, and anti-fibrotic activities. In animal models of nephrotoxicity, tropisetron decreases levels of TNF-α, IL-1β, and iNOS and improves renal pathology. Additionally, tropisetron increases survival of glutamatergic neurons by decreasing levels of p38 MAPK and inducing NMDA receptor internalization in vitro. Tropisetron also inhibits collagen synthesis and fibrosis in animal models of scleroderma.
References
Zirak MR, Rahimian R, Ghazi-Khansari M, et al. Tropisetron attenuates cisplatin-induced nephrotoxicity in mice. Eur J Pharmacol. 2014 Jun 4. [Epub ahead of print]. PMID: 24905858.
Swartz MM, Linn DM, Linn CL. Tropisetron as a neuroprotective agent against glutamate-induced excitotoxicity and mechanisms of action. Neuropharmacology. 2013 Oct;73:111-21. PMID: 23727438.
Stegemann A, Sindrilaru A, Eckes B, et al. Tropisetron suppresses collagen synthesis in skin fibroblasts via α7 nicotinic acetylcholine receptor and attenuates fibrosis in a scleroderma mouse model. Arthritis Rheum. 2013 Mar;65(3):792-804. PMID: 23440693.
Bandschapp O, Filitz J, Urwyler A, et al. Tropisetron blocks analgesic action of acetaminophen: a human pain model study. Pain. 2011 Jun;152(6):1304-10. PMID: 21420788.
Hsu ES. A review of granisetron, 5-hydroxytryptamine3 receptor antagonists, and other antiemetics. Am J Ther. 2010 Sep-Oct;17(5):476-86. PMID: 20844345.
