Alosetron - CAS 122852-42-0
Catalog number:
122852-42-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C17H18N4O
Molecular Weight:
294.36
COA:
Inquire
Targets:
5-HT Receptor
Description:
Alosetron, an effective 5-HT3 receptor antagonist, could be commonly used against irritable bowel syndrome.
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Purity:
95%
Appearance:
crystalline powder
Synonyms:
ALOSETRON;ALOSETRON2,3,4,5-Tetrahydro-5-methyl-2-((5-methyl-1H-imidazol-4-yl)methyl)-1H-pyrido(4,3-b)indol-1-one
Solubility:
10 mM in DMSO
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
Alosetron is an effective 5-HT3 receptor antagonist and could be commonly used against irritable bowel syndrome.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Grams-Kilos
Boiling Point:
648.1ºC at 760 mmHg
Density:
1.34 g/cm3
InChIKey:
JSWZEAMFRNKZNL-UHFFFAOYSA-N
InChI:
InChI=1S/C17H18N4O/c1-11-13(19-10-18-11)9-21-8-7-15-16(17(21)22)12-5-3-4-6-14(12)20(15)2/h3-6,10H,7-9H2,1-2H3,(H,18,19)
Canonical SMILES:
CC1=C(N=CN1)CN2CCC3=C(C2=O)C4=CC=CC=C4N3C
1.Diagnosis and treatment of diarrhea-predominant irritable bowel syndrome.
Lacy BE1. Int J Gen Med. 2016 Feb 11;9:7-17. doi: 10.2147/IJGM.S93698. eCollection 2016.
Irritable bowel syndrome (IBS) is one of the most common gastrointestinal disorders worldwide. The economic impact of IBS on the health care system is substantial, as is the personal impact on patients. Patients with diarrhea-predominant IBS (IBS-D) comprise a substantial proportion of the overall IBS population. Primary care providers are often the first point of contact for patients with IBS-D and can accurately diagnose IBS after a careful history and examination without extensive diagnostic tests. Several pharmacologic treatments (eg, loperamide, alosetron, and antidepressants) and non-pharmacologic treatments (eg, dietary modification and probiotics) are available for IBS-D, but restrictions on use (eg, alosetron) or the lack of controlled trial data showing reductions in both global and individual IBS-D symptoms (eg, bloating, pain and stool frequency) emphasize the need for alternative treatment options. Two newer medications (eluxadoline and rifaximin) were approved in May 2015 for the treatment of IBS-D, and represent new treatment options for this common gastrointestinal condition.
2.Sex-related differences in small intestinal transit and serotonin dynamics in high-fat-diet-induced obesity in mice.
France M1, Skorich E1, Kadrofske M2, Swain GM1,3, Galligan JJ1,4. Exp Physiol. 2016 Jan 1;101(1):81-99. doi: 10.1113/EP085427. Epub 2015 Oct 28.
NEW FINDINGS: What is the central question of this study? Are the sex differences in the effects of obesity on serotonin signaling mechanisms in the small intestine? What is the main finding and its importance? We demonstrate that small intestinal transit is altered in male and female obese mice. We found sex differences in intestinal 5-HT signalling in the jejunum of male and female obese mice that may underlie the altered intestinal transit. Our results reveal important sex differences in 5-HT-linked intestinal dysfunction in obesity. Obesity alters gastrointestinal (GI) motility and 5-HT signalling. Altered 5-HT signalling disrupts control of GI motility. Levels of extracellular 5-HT depend on enterochromaffin (EC) cell release and serotonin transporter (SERT) uptake. We assessed GI transit and 5-HT signalling in the jejunum of normal and obese mice. Male and female mice were fed a control diet (CD; 10% of kilocalories as fat) or a high-fat diet (HFD; 60% of kilocalories as fat).
3.Novel Therapies in IBS-D Treatment.
Nee J1, Zakari M2, Lembo AJ2. Curr Treat Options Gastroenterol. 2015 Dec;13(4):432-40. doi: 10.1007/s11938-015-0068-5.
OPINION STATEMENT: Irritable bowel syndrome (IBS) is a common gastrointestinal disease characterized by abdominal pain and change in bowel habits. IBS diarrhea predominant (IBS-D), which is arguably the most common subset of IBS, is also associated with rectal urgency, increased frequency, abdominal bloating, and loose to watery stools. Current treatments for diarrhea include mu-opioid agonists (i.e., loperamide, lomotil) and bile acid sequestrants (i.e., cholestyramine) while treatments for abdominal pain include antispasmodics (i.e., hyoscyamine, dicyclomine) and tricyclic antidepressants (i.e., amitriptyline). There are currently 3 FDA-approved treatments for IBS-D, which have been shown to improve both abdominal pain and diarrhea. Alosetron was initially approved by FDA 2000; however, its use is now limited to women with severe IBS-D symptoms refractory to other treatment. Eluxadoline, a mixed mu-opioid agonist, and rifaximin, a broad spectrum gut specific antibiotic, were both FDA approved in 2015.
4.Ramosetron Reduces Symptoms of Irritable Bowel Syndrome With Diarrhea and Improves Quality of Life in Women.
Fukudo S1, Kinoshita Y2, Okumura T3, Ida M4, Akiho H5, Nakashima Y6, Nishida A7, Haruma K8. Gastroenterology. 2016 Feb;150(2):358-366.e8. doi: 10.1053/j.gastro.2015.10.047. Epub 2015 Nov 6.
BACKGROUND & AIMS: Previous studies have indicated that serotonin-3-receptor antagonists might have a sex-specific effect in patients with irritable bowel syndrome with diarrhea (IBS-D). Alosetron has been approved for the treatment of only women, and ramosetron has been approved for the treatment for only men. We performed a randomized, placebo-controlled, phase 3 study to determine whether ramosetron reduces symptoms of IBS-D in women.
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CAS 122852-42-0 Alosetron

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