Formulation: A solid
Formal Name: 1-(methyl-d3)-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C18H21D3N4O
Formula Weight: 315,4
Shelf life (days): 1460
CAS Number: 1224925-76-1
Notes: Granisetron-d3 is intended for use as an internal standard for the quantification of granisetron (Item No. 21239) by GC- or LC-MS. Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 3.9 nM) with antiemetic activity.{23960,47619} It is selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM).{23960} Granisetron (0.3, 1, and 3 mg/kg, p.o.) increases the latency to a first vomiting episode and reduces the number of vomiting episodes in a canine model of emesis induced by cisplatin (Item No. 13119).{47619} It also increases the latency to a first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin (Item No. 15007) and cyclophosphamide (Item No. 13849) when administered at doses of 0.1, 0.3, and 1 mg/kg. Formulations containing granisetron have been used in the prevention of nausea and vomiting associated with chemotherapy.