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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。
CR1409 is a newly synthesized cholecystokinin (CCK) receptor antagonist. In this paper, fluorescent indicator Fura-2 as a detection of intracellular calcium ions in rat pancreatic cells in vitro study of OR1409 CCK caused by increased intracellular calcium concentration antagonism. The results showed that 10 μmol / L CR1409 completely inhibited the effect of 1 nmol / L CCK with a half-inhibitory concentration of 0.37 μmol / L, which was 100-fold stronger than that of the other antagonist, dibutyrylguanosine (db cGMP). With the increase of CR1409 concentration, the dose-response curve of increasing intracellular calcium concentration of CCK shifted to the right. According to Schild’s method, the pA_2 value was 6.93 (r = 0.992). CR1409 has no antagonistic effect on the carbachol and bombesin. Experimental results show that CR1409 is a more potent, specific and competitive CCK receptor antagonist.