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本文介绍的H_1受体新拮抗剂setastine,仅对中枢神经系统具有较小的镇静作用。合成氯苯与苯甲酰氯进行Friedel Crafts酰基化反应后产物与溴化甲基镁经Grignard反应,得4-氯-α-甲基二苯基甲醇(Ⅰ)。Ⅰ与N-(2-氯乙基)环六亚甲亚胺在苯、氨基钠和氯化氢存在下,进行烷基化反应,得到本品的盐酸盐[DE 2528194;JP1063525]。药理作用以吡咯醇胺为标准品对本品进行了药理学研究。豚鼠经皮下注射本品后,其防止组胺引起的死亡与吡咯醇胺相当(ED_(50)=0.10～0.12mg/kg),口服本品,其作用为标准品的1.5至2.5倍(ED_(50)=0.10～0.22 mg/kg,取决于预先给药的间期)。
This article describes the H_1 receptor antagonist setastine, which has only a minor sedative effect on the central nervous system. The synthesis of chlorobenzene and benzoyl chloride by Friedel Crafts acylation reaction with methyl magnesium bromide by Grignard reaction to give 4-chloro-α-methyldiphenylcarbinol (Ⅰ). I and N- (2-chloroethyl) -cyclic hexamethylene imine in the presence of benzene, sodium amide and hydrogen chloride, to give the hydrochloride salt [DE 2528194; JP 1063525]. Pharmacological effects Pyrrolnolamine as a standard product of this pharmacological study. Guinea pigs after subcutaneous injection of this product, to prevent the death caused by histamine and pyrrologolamine equivalent (ED_ (50) = 0.10 ~ 0.12mg / kg), oral administration of this product, its role as a standard 1.5 to 2.5 times (50) = 0.10 to 0.22 mg / kg, depending on the preadministration interval).