An orally bioavailable 5-HT3 antagonist (Ki = 2.9 nM); selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both)

Azasetron (hydrochloride) – 50 mg

Brand:
Cayman
CAS:
123040-16-4
Storage:
-20
UN-No:
Non-Hazardous - /

Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).{47619,47620} It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.{47619}  

 

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Description

An orally bioavailable 5-HT3 antagonist (Ki = 2.9 nM); selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as D1, D2, α1-, and α2-adrenergic receptors (IC50s = >10 μM); binds to H1 receptors (IC50 = 4.4 μM); inhibits 5-HT-induced contractions in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06); inhibits cisplatin-induced emesis in dogs and doxorubicin/cyclophosphamide-induced emesis in ferrets at 1 mg/kg

Formal name: N-1-azabicyclo[2.2.2]oct-3-yl-6-chloro-3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzoxazine-8-carboxamide, monohydrochloride

Synonyms:  Y-25130

Molecular weight: 386.3

CAS: 123040-16-4

Purity: ≥98%

Formulation: A crystalline solid

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