A 5-HT3 receptor antagonist
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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
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
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    25 mg

    $28

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    50 mg

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    100 mg

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    250 mg

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    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).