A 5-HT3 receptor antagonist
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Labeled Version(s)
33294Dolasetron-d4
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Dolasetron

Item No. 22234

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1H-indole-3-carboxylic acid, octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, stereoisomer
CAS Number
115956-12-2
Synonyms
  • MDL 73147
Molecular Formula
C19H20N2O3
Formula Weight
324.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 33 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 16 mg/ml
λmax
213, 282 nm
SMILES
O=C1C2C[C@@](C[C@H](OC(C3=CNC4=C3C=CC=C4)=O)C[C@]5([H])C2)([H])[N@]5C1
InChi Code
InChI=1S/C19H20N2O3/c22-18-10-21-12-5-11(18)6-13(21)8-14(7-12)24-19(23)16-9-20-17-4-2-1-3-15(16)17/h1-4,9,11-14,20H,5-8,10H2/t11?,12-,13+,14+
InChi Key
UKTAZPQNNNJVKR-MMUVGSQPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

    $85

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    25 mg

    $197

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    50 mg

    $367

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    Product Description

    Dolasetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 20 nM).1 It is selective for 5-HT3 receptors over 5-HT1A, 5-HT1B, 5-HT2, dopamine D2, α1-, α2-, β-adrenergic, M1-5 muscarinic acetylcholine, and neurokinin-1 (NK1) receptors (IC50s = >10 µM for all).2 Dolasetron inhibits 5-HT-induced membrane currents in NG 108-15 cells (IC50 = 3.8 nM).1 It increases the latency to emesis and reduces the number of vomiting and retching episodes induced by cisplatin (Item No. 13119) in ferrets when administered at doses of 0.5 or 2 mg/kg.2 Formulations containing dolasetron have been used in the prevention of postoperative or chemotherapy-induced nausea.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Beoijinga, P.H., Galvan, M., Baron, B.M., et al. Characterization of the novel 5-HT3 antagonists MDL 73147EF (dolasetron mesilate) and MDL 74156 in NG108-15 neuroblastoma x glioma cells. Eur. J. Pharmacol. 219(1), 9-13 (1992).

    2. Miller, R.C., Galvan, M., Gittos, M.W., et al. Pharmacological properties of dolasetron, a potent and selective antagonist at 5-HT3 receptors. Drug Develop. Res. 28(1), 87-93 (1993).