A histamine H3 receptor antagonist (Ki = 0.5 nM for inhibition of histamine release in rat synaptosomal preparations); selective for histamine H3 over histamine H1 and H2

Ciproxifan (maleate) – 5 mg

Brand:
Cayman
CAS:
184025-19-2
Storage:
-20
UN-No:
Non-Hazardous - /

Ciproxifan is a histamine H3 receptor antagonist (Ki = 0.5 nM for inhibition of histamine release in rat synaptosomal preparations).{54037} It is selective for histamine H3 over histamine H1 and H2, M3 muscarinic, and α1D- and β1-adrenergic receptors (Kis = 3.15-25 µM), as well as the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT2A, 5-HT3, and 5-HT4 (Kis = 1.58-15 µM) in radioligand binding assays. Ciproxifan (3-300 nM) inhibits relaxation in precontracted isolated guinea pig ileal longitudinal muscle induced by R-(–)-α-methylhistamine (Item No. 25601). In vivo, ciproxifan reduces R-(–)-α-methylhistamine-induced water consumption in rats (ED50 = 0.09 mg/kg). It increases wake episode duration and latency to fall asleep in rats when administered at a dose of 2 mg/kg.  

 

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Description

A histamine H3 receptor antagonist (Ki = 0.5 nM for inhibition of histamine release in rat synaptosomal preparations); selective for histamine H3 over histamine H1 and H2, M3 muscarinic, and α1D- and β1-adrenergic receptors (Kis = 3.15-25 µM), as well as 5-HT1B, 5-HT2A, 5-HT3, and 5-HT4 (Kis = 1.58-15 µM) in radioligand binding assays; inhibits R-(–)-α-methylhistamine-induced relaxation in precontracted isolated guinea pig ileal longitudinal muscle from 3-300 nM; reduces R-(–)-α-methylhistamine-induced water consumption in rats (ED50 = 0.09 mg/kg); increases wake episode duration and latency to fall asleep in rats when administered at a dose of 2 mg/kg

Formal name: cyclopropyl[4-[3-(1H-imidazol-4-yl)propoxy]phenyl]-methanone (2Z)-2-butenedioate

Synonyms:  FUB-359

Molecular weight: 386.4

CAS: 184025-19-2

Purity: ≥98%

Formulation: A crystalline solid

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