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MedKoo Cat#: 317171 | Name: Alosetron HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Alosetron is a potent and selective 5-HT3 receptor antagonist. Alosetron blocks the actions of serotonin at 5-HT3 sites in the peripheral nervous system, particularly on enteric and nociceptive sensory neurons, thereby affecting the regulation of visceral pain, decreasing gastrointestinal contraction and motility, and decreasing gastrointestinal secretions. This agent is used to treat diarrhea-predominant irritable bowel syndrome in women only.

Chemical Structure

Alosetron HCl
Alosetron HCl
CAS#122852-69-1 (HCl)

Theoretical Analysis

MedKoo Cat#: 317171

Name: Alosetron HCl

CAS#: 122852-69-1 (HCl)

Chemical Formula: C17H19ClN4O

Exact Mass: 294.1481

Molecular Weight: 330.82

Elemental Analysis: C, 61.72; H, 5.79; Cl, 10.72; N, 16.94; O, 4.84

Price and Availability

Size Price Availability Quantity
50mg USD 350.00 2 Weeks
100mg USD 550.00 2 Weeks
250mg USD 1,050.00 2 Weeks
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Related CAS #
122852-42-0 (free base) 122852-69-1 (HCl)
Synonym
Alosetron HCl; Alosetron hydrochloride; Lotronex; GR68755; GR-68755; GR 68755;
IUPAC/Chemical Name
5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one hydrochloride
InChi Key
FNYQZOVOVDSGJH-UHFFFAOYSA-N
InChi Code
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
SMILES Code
O=C1N(CC2=C(C)NC=N2)CCC(N3C)=C1C4=C3C=CC=C4.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 330.82 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Alosetron. 2019 Feb 7. PMID: 30222295. 2: Balfour JA, Goa KL, Perry CM. Alosetron. Drugs. 2000 Mar;59(3):511-8; discussion 519-20. doi: 10.2165/00003495-200059030-00008. PMID: 10776833. 3: Butt I, Kasmin F. Alosetron. 2022 Dec 5. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan–. PMID: 31971721. 4: Mucke H, Cole P, Rabasseda X. Alosetron. Drugs Today (Barc). 2000 Sep;36(9):595-607. doi: 10.1358/dot.2000.36.9.593776. PMID: 12847565. 5: Mayer EA, Bradesi S. Alosetron and irritable bowel syndrome. Expert Opin Pharmacother. 2003 Nov;4(11):2089-98. doi: 10.1517/14656566.4.11.2089. PMID: 14596662. 6: Bleser S. Alosetron for severe diarrhea-predominant irritable bowel syndrome: improving patient outcomes. Curr Med Res Opin. 2011 Mar;27(3):503-12. doi: 10.1185/03007995.2010.547933. Epub 2011 Jan 6. PMID: 21208139. 7: Lembo A, Sultan S, Chang L, Heidelbaugh JJ, Smalley W, Verne GN. AGA Clinical Practice Guideline on the Pharmacological Management of Irritable Bowel Syndrome With Diarrhea. Gastroenterology. 2022 Jul;163(1):137-151. doi: 10.1053/j.gastro.2022.04.017. PMID: 35738725. 8: Camilleri M. Pharmacology and clinical experience with alosetron. Expert Opin Investig Drugs. 2000 Jan;9(1):147-59. doi: 10.1517/13543784.9.1.147. PMID: 11060667. 9: Savarino E, Zingone F, Barberio B, Marasco G, Akyuz F, Akpinar H, Barboi O, Bodini G, Bor S, Chiarioni G, Cristian G, Corsetti M, Di Sabatino A, Dimitriu AM, Drug V, Dumitrascu DL, Ford AC, Hauser G, Nakov R, Patel N, Pohl D, Sfarti C, Serra J, Simrén M, Suciu A, Tack J, Toruner M, Walters J, Cremon C, Barbara G. Functional bowel disorders with diarrhoea: Clinical guidelines of the United European Gastroenterology and European Society for Neurogastroenterology and Motility. United European Gastroenterol J. 2022 Jul;10(6):556-584. doi: 10.1002/ueg2.12259. Epub 2022 Jun 13. PMID: 35695704; PMCID: PMC9278595. 10: Hyman PE, Garvey TQ 3rd. Return of alosetron. Expert Opin Drug Saf. 2002 May;1(1):1-4. doi: 10.1517/14740338.1.1.1. PMID: 12904154. 11: Gunput MD. Review article: clinical pharmacology of alosetron. Aliment Pharmacol Ther. 1999 May;13 Suppl 2:70-6. doi: 10.1046/j.1365-2036.1999.00009.x. PMID: 10429744. 12: Black CJ, Ford AC. Best management of irritable bowel syndrome. Frontline Gastroenterol. 2020 May 28;12(4):303-315. doi: 10.1136/flgastro-2019-101298. PMID: 34249316; PMCID: PMC8231425. 13: Lembo A, Weber HC, Farraye FA. Alosetron in irritable bowel syndrome: strategies for its use in a common gastrointestinal disorder. Drugs. 2003;63(18):1895-905. doi: 10.2165/00003495-200363180-00002. PMID: 12930162. 14: Moynihan R. Alosetron: a case study in regulatory capture, or a victory for patients' rights? BMJ. 2002 Sep 14;325(7364):592-5. doi: 10.1136/bmj.325.7364.592. PMID: 12228140; PMCID: PMC1124108. 15: Andresen V, Hollerbach S. Reassessing the benefits and risks of alosetron: what is its place in the treatment of irritable bowel syndrome? Drug Saf. 2004;27(5):283-92. doi: 10.2165/00002018-200427050-00001. PMID: 15061683. 16: Linezolid, Alosetron, Levetiracetam. Am J Health Syst Pharm. 2000 Aug 15;57(16):1480-4. PMID: 10965393. 17: Gallo-Torres H, Brinker A, Avigan M. Alosetron: ischemic colitis and serious complications of constipation. Am J Gastroenterol. 2006 May;101(5):1080-3. doi: 10.1111/j.1572-0241.2006.00650.x. PMID: 16696787. 18: Chang L, Chey WD, Harris L, Olden K, Surawicz C, Schoenfeld P. Incidence of ischemic colitis and serious complications of constipation among patients using alosetron: systematic review of clinical trials and post-marketing surveillance data. Am J Gastroenterol. 2006 May;101(5):1069-79. doi: 10.1111/j.1572-0241.2006.00459.x. PMID: 16606352. 19: Audolfsson G, Bayguinov O, Yamamoto T, Somogyi GT, Schraut WH, Sanders KM, Bauer AJ. Review article: effects of the 5-HT3 receptor antagonist alosetron on neuromuscular transmission in canine and human intestinal muscle. Aliment Pharmacol Ther. 1999 May;13 Suppl 2:39-47. PMID: 10429739. 20: Lièvre M. Alosetron for irritable bowel syndrome. BMJ. 2002 Sep 14;325(7364):555-6. doi: 10.1136/bmj.325.7364.555. PMID: 12228116; PMCID: PMC1124090.