A 5-HT3 receptor antagonist
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Labeled Version(s)
29049Palonosetron-d3 (hydrochloride)
Metabolite(s)
34212Palonosetron N-oxide
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Palonosetron (hydrochloride)

Item No. 16752

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3aS,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one, monohydrochloride
CAS Number
135729-62-3
Synonyms
  • RS 25259-197
Molecular Formula
C19H24N2O • HCl
Formula Weight
332.9
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
210, 239 nm
SMILES
O=C(N([C@H]1C(CC2)CCN2C1)C3)C4=CC=CC5=C4[C@]3([H])CCC5.Cl
InChi Code
InChI=1S/C19H24N2O.ClH/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20;/h2,4,6,13,15,17H,1,3,5,7-12H2;1H/t15-,17-;/m1./s1
InChi Key
OLDRWYVIKMSFFB-SSPJITILSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    50 mg

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    Product Description

    Palonosetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 0.04 nM).1 It is selective for 5-HT3 over 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors (Kis = ≥15.85 μM for all), as well as a panel of additional neurotransmitter receptors. Palonosetron inhibits 5-HT-induced contraction in isolated guinea pig ileum. It inhibits cisplatin-induced emesis in ferrets (ID50 = 1.1 μg/kg, i.v.) as well as emesis induced by cisplatin (Item No. 13119), dacarbazine (Item No. 21877), actinomycin D (Item No. 11421), and mechlorethamine in dogs (ID50s = 1.9, 4.1, 4.9, and 4.4 μg/kg, respectively).2 Formulations containing palonosetron have been used in the treatment of postoperative or chemotherapy-induced nausea and vomiting.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wong, E.H., Clark, R., Leung, E., et al. The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro. Br. J. Pharmacol. 114(4), 851-859 (1995).

    2. Eglen, R.M., Lee, C.H., Smith, W.L., et al. Pharmacological characterization of RS 25259-197, a novel and selective 5-HT3 receptor antagonist, in vivo. Br. J. Pharmacol. 114(4), 860-866 (1995).