An internal standard for the quantification of dolasetron
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Unlabeled Version(s)
22234Dolasetron
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Dolasetron-d4

Item No. 33294

Technical Information
Formal Name
1H-indole-3-carboxylic acid-4,5,6,7-d4, octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, stereoisomer
Molecular Formula
C19H16D4N2O3
Formula Weight
Purity
≥99% deuterated forms (d1-d4)
Formulation
A solid
Acetone: solubleAcetonitrile: solubleDMSO: solubleMethanol: soluble
SMILES
O=C(C1=CNC2=C([2H])C([2H])=C([2H])C([2H])=C12)O[C@@H]3C[C@@]4([H])[N@](CC5=O)[C@](C3)([H])CC5C4
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+/i1D,2D,3D,4D
InChi Key
UKTAZPQNNNJVKR-MFXNJGBYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    Product Description

    Dolasetron-d4 is intended for use as an internal standard for the quantification of dolasetron (Item No. 22234) by GC- or LC-MS. 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-, and 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 alCharacterization 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 alPharmacological properties of dolasetron, a potent and selective antagonist at 5-HT3 receptors. Drug Develop. Res. 28(1), 87-93 (1993).