Description
Ramosetron is an inhibitor of 5-HT3 receptors that is currently in clinical trials as a treatment for chemotherapeutic-induced or postoperative nausea and vomiting; it also treats inflammatory bowel syndrome (IBS). Ramosetron exhibits antiemetic and anti-inflammatory activities. Ramosetron inhibits 5-fluorouracil-induced inflammation and mucositis, decreasing expression of IL-6, TNF-α, and IL-1β, decreasing activation of caspases 3 and 8, and preventing apoptosis; this results in decreased body weight loss and disease severity. This compound also allows gastrointestinal transit and inhibits stress-induced abnormal defecation in vivo.
References
Kim WJ, Kang H, Shin HY, et al. Ramosetron, midazolam, and combination of ramosetron and midazolam for prevention of postoperative nausea and vomiting: a prospective, randomized, double-blind study. J Int Med Res. 2013 Aug;41(4):1203-13. PMID: 23766412.
Park YM, Lee YJ, Lee YH, et al. Effects of ramosetron on gastrointestinal transit of Guinea pig. J Neurogastroenterol Motil. 2013 Jan;19(1):36-41. Erratum in: J Neurogastroenterol Motil. 2013;19(2):275. PMID: 23350045.
Yasuda M, Kato S, Yamanaka N, et al. 5-HT3 receptor antagonists ameliorate 5-fluorouracil-induced intestinal mucositis by suppression of apoptosis in murine intestinal crypt cells. Br J Pharmacol. 2013 Mar;168(6):1388-400. PMID: 23072534.
