r-43512

Tecastemizole (R 43512) is a selective antagonist of H1 receptor and a major metabolite of astemizole with anti-inflammatory effects.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

Astemizole (Standard) is a reference standard for quantitative analysis, quality control, and biochemical experiments. Astemizole (Laridal) is a long-acting, non-sedating antihistamine. It acts as a histamine H1 receptor antagonist (IC50 = 4 nM) and an hERG K+ channel blocker (IC50 = 0.9 nM), exhibiting anticholinergic and antipruritic effects. It is indicated for inflammatory conditions such as rhinitis and asthma.