Formulation: A solid
Formal Name: 1-[(4-fluorophenyl)methyl]-N-4-piperidinyl-1H-benzimidazol-2-amine
Purity: ≥98%
Formula Markup: C19H21FN4
Formula Weight: 324,4
Shelf life (days): 1460
CAS Number: 75970-99-9
Notes: Norastemizole is a histamine H1 receptor antagonist (IC50 = 4.1 nM) and an active metabolite of the histamine H1 receptor antagonist and ether-a-go-go (ERG) channel blocker astemizole (Item No. 16967).{67881,67882} It is formed from astemizole by the cytochrome P450 (CYP) isoform 3A4 (CYP3A4).{67882} Norastemizole also inhibits currents in a whole-cell patch-clamp assay using HEK293 cells expressing human-ether-a-go-go (hERG), also known as Kv11.1 (IC50 = 27.7 nM).{67883} It prevents IL-1β-induced increases in the levels of intracellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) in human umbilical vein endothelial cells (HUVECs) when used at a concentration of 100 µM.{67884} Norastemizole (1 mg/kg) inhibits passive cutaneous anaphylaxis induced by ovalbumin (OVA) or the biogenic amine histamine (Item No. 33828), but not by bradykinin, in guinea pigs. It inhibits eosinophil infiltration into the lungs of mice in a mouse model of OVA-induced asthma when administered at a dose of 1 mg/kg.
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