CR1409拮抗缩胆囊素升高细胞内Ca^(2+)的作用  

ANTAGONISTIC EFFECT OF CR1409 ON CHOLECYSTOKININ-INDUCED INCREASE IN CYTOSOLIC CALCIUM CONCENTRATION

作　　者：陈蔚文[1] Cheret AM Abastado M Lewin MJM 

机构地区：[1]广州中医学院消化研究室,510407 [2]法国胃肠病学研究所

出　　处：《中国药理学通报》1991年第6期425-429,共5页Chinese Pharmacological Bulletin

摘　　要：CR1409是一种新合成的缩胆囊素(CCK)受体拮抗剂。本文使用荧光指示剂Fura-2作为细胞内钙离子的探测物,在离体的大白鼠胰腺细胞研究OR1409对CCK引起细胞内钙离子浓度升高的拮抗作用。结果表明:10μmol/L CR1409完全抑制1nmol/L CCK的作用,半效抑制浓度为0.37μmol/L,比另一种拮抗剂双丁酰环鸟嘌呤核苷(db cGMP)强100倍。随着CR1409浓度的递增,使CCK升高细胞内钙离子浓度的量效曲线右移,根据Schild方法计算,pA_2值为6.93(r=0.992)。CR1409对氯氨甲酰胆碱和蛙皮素无拮抗作用。实验结果证明CR1409是一种效力较强的、特异性的和竞争性的CCK受体拮抗剂。The glutaramic acid derivative cholecystokinin ( CCK ) receptor antagonist, CR1409 was tested for its ability to inhibit CCK induced increase in cytosolic calcium concentration in isolated rat pancreatic acinar cells using fura-2 as calcium probe. Preaddition of 10μmol/L CR1409 completely inhibited the increase of cytosolic calcium concertration induced with 1 nmol/L CCK, but had no antagonistic effect on carbacholine bombesin-induced increase in cytosolic calcium concentration. The half maximal inhibition ...

关 键 词：细胞内钙离子 缩胆囊素 CR1409 Fura 2/AM 离体细胞 量效曲线 量—效反应曲线 

分 类 号：R96[医药卫生—药理学]