A 5-HT3 receptor antagonist (Ki = 0.04 nM); selective for 5-HT3 over 5-HT1A

Palonosetron (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
135729-62-3
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

A 5-HT3 receptor antagonist (Ki = 0.04 nM); 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; inhibits 5-HT-induced contraction in isolated guinea pig ileum; inhibits cisplatin-induced emesis in ferrets (ID50 = 1.1 μg/kg, i.v.); inhibits emesis induced by cisplatin, dacarbazine, actinomycin D, and mechlorethamine in dogs (ID50s = 1.9, 4.1, 4.9, and 4.4 μg/kg, respectively)

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

Synonyms:  RS 25259-197

Molecular weight: 332.9

CAS: 135729-62-3

Purity: ≥98%

Formulation: A crystalline solid

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

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