A 5-HT3 receptor antagonist
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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
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
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    10 mg

    $107

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    25 mg

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    50 mg

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    100 mg

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    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).