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在离体正常和炎性胆囊,甲基莲心碱(Nef)明显抑制K+所致收缩,其IC(50)分别为120μmol/L和5μmol/L,表明Nef对炎性胆囊抑制作用较强。Nef和维拉帕米(Ver)可抑制K ̄+所致Oddi括约肌两相收缩,Ver主要抑制持久相收缩,而Nef以抑制时相收缩为强。Nef和Ver非竞争性拮抗组织胺(Hist)所致胆囊收缩,其PD′_2值分别为5.01和5.38。提示Nef对胆道平滑肌的抑制作用与其抗内钙释放有关。
In isolated normal and inflammatory gallbladder, neferine significantly inhibited the contraction caused by K+, and its IC (50) was 120 μmol/L and 5 μmol/L, respectively, indicating that Nef has a strong inhibitory effect on inflammatory gallbladder. Nef and verapamil (Ver) inhibited the contraction of Oddi’s sphincter contraction caused by K ̄ + , Ver inhibited the contraction of the permanent phase, and Nef suppressed the contraction of the time phase. Nef and Ver non-competitively antagonized the contraction of the gallbladder caused by histamine (Hist) with PD’2 values of 5.01 and 5.38, respectively. It is suggested that the inhibitory effect of Nef on bile duct smooth muscle is related to its resistance to internal calcium release.