Share this post on:

Ramosetron

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 PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18957445,20543426,18562677

Cas No.

132036-88-5

Purity

≥98%

Formula

C17H17N3O

Formula Wt.

279.34

IUPAC Name

(1-methylindol-3-yl)-[(5R)-4,5,6,7-tetrahydro-3H-benzimidazol-5-yl]methanone

Appearance

White to pale yellow crystalline powder

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.

Ro5126767