Ramosetron hydrochloride

Ramosetron hydrochloride is a member of indoles.|Ramosetron Hydrochloride is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity. Upon administration, ramosetron selectively binds to and blocks the activity of 5-HT subtype 3 (5-HT3) receptors located in the vagus nerve terminal and in the vomiting center in the central nervous system (CNS), suppressing chemotherapy-induced nausea and vomiting.
Ramosetron Hydrochloride is the only currently available drug indicated for the treatment of male patients with IBS-D in Japan. Ramosetron Hydrochloride was approved in July 1996 under a brand name of Nasea Injection 0.3 mg and in June 1998 under a brand name of Nasea OD tablets 0.1 mg for the treatment of gastrointestinal symptoms (nausea and vomiting) associated with therapy with antineoplastic drugs (e.g., cisplatin).Nasea was launched in Japan for chemotherapy-induced emesis. Nasea was prepared by a four step sequence via the Vilsmeier-type coupling of 1-methylindole and 5-( 1- pyrrolidoncarbonyl)-4,5,6,7-tetrahydro-Hl-benzimidazole hydrochloride. The antiemetic activity arises because it is a potent 5-HT3 receptor antagonist that is i.v. and orally active. The (R)-isomer was found to be 100 times more potent than the (S)-isomer. It was able to inhibit cisplatin-induce emesis and was 8670 times more potent than netoclopramide.
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ChEBI: Ramosetron hydrochloride is a member of indoles.