VUF-K-8788

VUF-K-8788 is a periphery-selective histamine H1 receptor antagonist developed for its anti-allergic and anti-pruritic activities. It demonstrates potent inhibition of histamine-induced responses in vitro and in vivo, including blocking [3H]-mepyramine binding to lung parenchyma membranes (Ki = 5.0 nM) and inhibiting histamine-induced contraction of isolated guinea pig ileum without affecting contractions induced by other agents such as acetylcholine or serotonin. In animal models, VUF-K-8788 reduces vascular permeability increases caused by histamine and passive cutaneous anaphylaxis (PCA), inhibits both immediate and late-phase asthmatic reactions, suppresses eosinophil and macrophage infiltration into bronchoalveolar lavage fluid, and completely blocks PCA-induced scratching behavior without central nervous system side effects at tested doses. These properties suggest potential utility in treating allergic disorders such as atopic dermatitis, eczema, and bronchial asthma[1][2][3][4][5][9].

Other names

7-[3-[4-(2-quinolinylmethyl)-1-piperazinyl]-propoxy]-2,3-dihydro-4H-1,4-benzothiazin-3-one