化合物 Epinastine T60366

Product Introduction
Bioactivity


英文名: Epinastine

描述: Epinastine (WAL801) 是一种抗组胺剂和肥大细胞稳定剂。Epinastine 是一种有效的，选择性的，口服活性的组胺 H1 受体 (histamine H1 receptor) 拮抗剂。Epinastine 还抑制人嗜酸性粒细胞释放 IL-8 并具有抗过敏作用。

体外活性: Epinastine can displace specific [ 3 H]NC-5Z binding at low concentrations in the locust nervous tissue. Epinastine binds to the honey bees neuronal octopamine receptor with K i of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain [2]. Epinastine results in an inhibition of histamine release from rat peritoneal mast cells induced by both antigen-antibody reaction and compound 48/80. Epinastine is similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. Epinastine is effective in inhibiting not only Ca 2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca 2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance P [3]. Epinastine shows a dose- and time-dependent suppressive effect on IL-8, one of the chemokines for eosinophils, released from eosinophils isolated from atopic diseases [4].

体内活性: In receptor binding studies, Epinastine shows a high affinity to H1-receptors in the guinea pig ileum. Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途