A 5-HT3 receptor antagonist (Ki = 3.9 nM) with antiemetic activity; selective for 5-HT3 over 5-HT4 receptors (Ki = >1

Granisetron (hydrochloride) – 1 g

Brand:
Cayman
CAS:
107007-99-8
Storage:
-20
UN-No:
Non-Hazardous - /

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 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 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.  

 

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Description

A 5-HT3 receptor antagonist (Ki = 3.9 nM) with antiemetic activity; selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM); increases the latency to first vomiting episodes and reduces the number of vomiting episodes in a canine model of cisplatin-induced emesis at 0.3, 1, and 3 mg/kg, p.o.; increases the latency to first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin and cyclophosphamide at 0.1, 0.3, and 1 mg/kg

Formal name: 1-methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide, monohydrochloride

Synonyms:  BRL 43694

Molecular weight: 348.9

CAS: 107007-99-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience

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