Formulation: A solid
Formal Name: (S)-2-((S)-quinuclidin-3-yl-3-d)-2,3,3a,4,5,6-hexahydro-1H-benzo[de]isoquinolin-1-one-3,3-d2, monohydrochloride
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C19H21D3N2O • HCl
Formula Weight: 335,9
Shelf life (days): 1460
Notes: Palonosetron-d3 is intended for use as an internal standard for the quantification of palonosetron (Item No. 16752) by GC- or LC-MS. Palonosetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 0.04 nM).{27432} 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).{27431} Formulations containing palonosetron have been used in the treatment of postoperative or chemotherapy-induced nausea and vomiting.
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