A 5-HT3 receptor antagonist
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Alosetron (hydrochloride)

Item No. 22434

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,3,4,5-tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-1H-pyrido[4,3-b]indol-1-one, monohydrochloride
CAS Number
122852-69-1
Synonyms
  • GR 68755
Molecular Formula
C17H18N4O • HCl
Formula Weight
330.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mlEthanol: 0.5 mg/ml
λmax
218, 259, 294 nm
SMILES
CN(C1=C2C=CC=C1)C3=C2C(N(CC4=C(C)NC=N4)CC3)=O.Cl
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
InChi Key
FNYQZOVOVDSGJH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    25 mg

    $28

    Add

    50 mg

    $44

    Add

    100 mg

    $66

    Add

    250 mg

    $152

    Add
    Product Description

    Alosetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Kis = 0.3 and 0.4 nM for the rat cortical and human recombinant receptors, respectively).1 It is selective for 5-HT3 over 5-HT2 and 5-HT1A receptors (Kis = 6.3 and >100 µM, respectively), as well as α1-, β1-, and β2- adrenergic, M1, M2, and M3 muscarinic, GABAA, dopamine D2, and nicotinic receptors at 10 μM.2 Alosetron (0.3-10 nM) inhibits 5-HT-induced depolarization of isolated rat vagus nerve.1 It reduces wrap restraint stress-induced defecation and the number of abdominal muscle contractions in a rat model of irritable bowel syndrome with diarrhea (IBS-D) when administered at a dose of 0.1 mg/kg.3 Formulations containing alosetron have been used in the treatment of diarrhea-predominant irritable bowel syndrome in women.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Humphrey, P.P., Bountra, C., Clayton, N., et al. Review article: the therapeutic potential of 5-HT3 receptor antagonists in the treatment of irritable bowel syndrome. Ailment Pharmacol. Ther. 13(Suppl 2), 31-38 (1999).

    2. Kilpatrick, G.J., Hagan, R.M., Butler, A., et al. GR68755, a potent and selective antagonist of 5-HT3 receptors. Glaxo Grp. Res. Ltd. 259P (1991).

    3. Taquichi, R., Shilkata, K., Furuya, Y., et al. Selective corticotropin-releasing factor 1 receptor antagonist E2508 reduces restraint stress-induced defecation and visceral pain in rat models. Psychoneuroendocrinology 75, 110-115 (2017).