Alosetron HCl - CAS 122852-69-1
Catalog number: 122852-69-1
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C17H18N4O. HCl
Molecular Weight:
330.81
COA:
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Targets:
5-HT Receptor
Description:
The hydrochloride salt form of Alosetron which is an effective 5-HT3 receptor antagonist and could be commonly used against irritable bowel syndrome.
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Purity:
> 95%
Appearance:
White to Pale Yellow Solid
Synonyms:
2,3,4,5-Tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-1H-pyrido[4,3-b]indol-1-one Hydrochloride;
Solubility:
DMSO:> 3 mg/ml; methanol: > 3 mg/ml
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
The hydrochloride salt form of Alosetron which 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:
Milligrams-Grams
Melting Point:
>270 ˚C
InChIKey:
FNYQZOVOVDSGJH-UHFFFAOYSA-N
InChI:
InChI=1S/C17H18N4O.ClH/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);1H
Canonical SMILES:
CC1=C(N=CN1)CN2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl
1.Development of a Forced Degradation Profile of Alosetron by Single Mode Reversed-Phase HPLC, LC-MS, and its Validation.
Karthik Y1, Babu B1, Meyyanathan SN1. Sci Pharm. 2014 Dec 29;83(2):311-20. doi: 10.3797/scipharm.1411-07. eCollection 2015.
Determination of alosetron in the presence of its degradation products was studied and validated by a novel HPLC method. The separation of the drug and its degradation products was achieved with the Jones Chromatography C18 analytical column (150 mm x 4.6 mm; 3 µm) with a stationary phase in isocratic elution mode. The mobile phase used was 0.01 M ammonium acetate, pH-adjusted to 3.5 with glacial acetic acid and acetonitrile in the ratio of 75:25 (V/V) at a flow rate of 1 ml/min and UV detection was carried out at 217 nm. Further, the drug was subjected to stress studies for acidic, basic, neutral, oxidative, and thermal degradations as per ICH guidelines and the drug was found to be labile in base hydrolysis and oxidation, while stable in acid, neutral, thermal, and photolytic degradation conditions. An MS study has been performed on the major degradation products to predict the degradation pathway of alosetron. The method provided linear responses over the concentration range of 100-1500 ng/ml and regression analysis showed a correlation coefficient value (r(2)) of 0.
2.Novel pharmacological therapies for irritable bowel syndrome.
Corsetti M1, Whorwell P2. Expert Rev Gastroenterol Hepatol. 2016 Mar 18:1-9. [Epub ahead of print]
Irritable bowel syndrome (IBS) is a prevalent functional gastrointestinal disorder, which represents a major cost to healthcare services. Current pharmacological treatment includes fibre supplements, antispasmodics, laxatives, loperamide and antidepressants. This article reviews the novel pharmacological treatments already or recently approved for patients with IBS-C (lubiprostone, linaclotide) and IBS-D (alosetron, ramosetron, rifaximin, eluxadoline). Furthermore, results for drugs in development (plecanatide, ibudutant and ebastine) or used in chronic constipation or for other indications, with potential application in IBS (prucalopride, elobixibat, mesalazine, ondansetron and colesevelam) are also reviewed.
3.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.
4.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.
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Chemical Structure

CAS 122852-69-1 Alosetron HCl

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