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.

Azasetron (hydrochloride)

Item No. 28383

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-1-azabicyclo[2.2.2]oct-3-yl-6-chloro-3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzoxazine-8-carboxamide, monohydrochloride
CAS Number
123040-16-4
Synonyms
  • Y-25130
Molecular Formula
C17H20ClN3O3 • HCl
Formula Weight
386.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
λmax
221, 307 nm
SMILES
O=C(C1=C(OCC(N2C)=O)C2=CC(Cl)=C1)NC3C4CCN(CC4)C3.Cl
InChi Code
InChI=1S/C17H20ClN3O3.ClH/c1-20-14-7-11(18)6-12(16(14)24-9-15(20)22)17(23)19-13-8-21-4-2-10(13)3-5-21;/h6-7,10,13H,2-5,8-9H2,1H3,(H,19,23);1H
InChi Key
DBMKBKPJYAHLQP-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

    10 mg

    $107

    Add

    25 mg

    $240

    Add

    50 mg

    $371

    Add

    100 mg

    $688

    Add
    Product Description

    Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).1,2 It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Haga, K., Inaba, K., Shoji, H., et al. The effects of orally administered Y-25130, a selective serotonin3-receptor antagonist, on chemotherapeutic agent-induced emesis. Jpn. J. Pharmacol. 63(3), 377-383 (1993).

    2. Sato, N., Sakamori, M., Haga, K., et al. Antagonistic activity of Y-25130 on 5-HT3 receptors. Jpn. J. Pharmacol. 59(4), 443-448 (1992).