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Ramosetron hydrochloride

Ramosetron hydrochloride structure

CAS No:
132907-72-3
Formula:
C17H18ClN3O
Chemical Name:
Ramosetron hydrochloride
Synonyms:
Methanone,(1-Methyl-1H-indol-3-yl)[(6R)-4,5,6,7-tetrahydro-1H-benziMidazol-6-yl]-,hydrochloride (1:1);(R)-5-[(1-Methyl-3-indolyl)carbonyl]-4,5,6,7-tetrahydro-1H-benzimidazole hydrochloride;(1-methylindol-3-yl)-[(5r)-4,5,6,7-tetrahydro-3h-benzimidazol-5-yl]methanone hydrochloride;RAMOSETRON HYDROCHLORIDE;(1-methyl-1h-indol-3-yl)(4,5,6,7-tetrahydro-1h-benzimidazol-5-yl)-methanon;(r)-5-((1-methyl-3-indolyl)carbonyl)-4,5,6,7-tetrahydro-1h-benzimidazolehydr;(r)-monohydrochlorid;ym060
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

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.

White Solid

ChEBI: Ramosetron hydrochloride is a member of indoles.

Ramosetron hydrochloride Basic Attributes

Molecular Weight：

315.8

Exact Mass：

315.1138399

UNII：

9551LHD87E

DSSTox ID：

DTXSID3021223

NCI Thesaurus Code：

C88299

Color/Form：

white to beige

Characteristics

Melting Point：

244-246°C

Water Solubility：

H2O: 20mg/mL, clear

Toxicity：

dog,LD,intravenous,> 30mg/kg (30mg/kg),SENSE ORGANS AND SPECIAL SENSES: CONJUNCTIVE IRRITATION: EYE,Oyo Yakuri. Pharmacometrics. Vol. 47, Pg. 117, 1994.

Critical Temperature & Pressure：

-20°C

Safety Information

wgk germany：

hazard class code：

Hazard Statements：

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 39 companies from 1 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

Drugs used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)|Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS. (See all compounds classified as Serotonin Antagonists.)

MeSH Entry Terms：

5-((1-methyl-3-indolyl)carbonyl)-4,5,6,7-tetrahydro-1H-benzimidazol

Ramosetron hydrochloride Use and Manufacturing

Ramosetron Hydrochloride is a selective serotonin 5-HT3 receptor antagonist and has structurally different from Ondansetron (O655000), Granisetron (G780000). It controls excessive bowel movement and diarrhea by inhibiting 5-HT3 receptors in the intestinal tract. Ramosetron Hydrochloride was approved as film-coated tablets in July 2008 and as orally disintegrating tablets in August 2013 for the indication of treatment of male patients with diarrhea-predominant irritable bowel syndrome.

Drug Function and Efficacy

1. 5-HT3 receptor antagonism: In the 5-hydroxytryptamine-induced guinea pig isolated colon contraction experiment and rat and ferret heart rate slowing reflex (Bezold-Jarisch reflex) experiment, it showed 5-HT3 receptor antagonism; 2. Anti-malignant tumor drug-induced vomiting inhibition: The vomiting of ferrets induced by cisplatin was inhibited by giving this product before or after the first vomiting. Cisplatin and other anti-malignant tumor drugs can free 5-hydroxytryptamine from the chromaffin cells in the digestive tract, and 5-hydroxytryptamine binds to the 5-HT3 receptors present in the gastrointestinal mucosa and the vagus nerve endings.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Ramosetron Hydrochloride Injection
Ingredients	Ramosetron Hydrochloride
Indication	This drug may react with mannitol injection, bumetanide injection, furosemide injection, etc., so do not use them together. However, it can be used by adding 200ml of normal saline to furosemide injection containing 20mg of furanilamide and mixing with one ampoule of this drug.
Specifications	2ml:0.3mg
Manufacturer	Cisen Pharmaceutical Co., Ltd.

Ramosetron Hydrochloride Injection
Ingredients	Ramosetron Hydrochloride
Indication	This drug may react with mannitol injection, bumetanide injection, furosemide injection, etc., so do not use them together. However, it can be used by adding 200ml of normal saline to furosemide injection containing 20mg of furanilamide and mixing with one ampoule of this drug.
Specifications	2ml:0.3mg
Manufacturer	ZHONGFU Pharmaceutical Co., Ltd.

Ramosetron Hydrochloride for Injection
Ingredients	The main ingredient of this product is ramosetron hydrochloride, and its chemical name is: (-)-5-(R)-(1-methyl-indole-3-carbonyl)-4,5,6,7-tetrahydro-benzimidazole hydrochloride.
Indication	This drug may react with mannitol injection, bumetanide injection, furosemide injection, etc., so do not use them together. However, it can be used by adding 200 ml of normal saline to furosemide injection containing 20 mg of furanilic acid and mixing with one ampoule of this drug.
Specifications	0.3mg
Manufacturer	Zhejiang Yatai Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

Yuanda Life Sciences (Shandong) Co., Ltd.

China
Active
ZHONGFU Pharmaceutical Co., Ltd.

China
Active
Jiangsu Shenlong Pharmaceutical Co., Ltd.

China
Active

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