新型胆囊收缩素类似物的药理学特性

Pharmacological characterization of new cholecystokinin analogues.

作者信息

Maletínská L, Lignon M F, Galas M C, Bernad N, Pírková J, Hlavácek J, Slaninová J, Martinez J

机构信息

Institute of Organic Chemistry and Biochemistry, Czechoslovak Academy of Sciences, Prague.

出版信息

Eur J Pharmacol. 1992 Nov 10;222(2-3):233-40. doi: 10.1016/0014-2999(92)90861-w.

DOI:10.1016/0014-2999(92)90861-w

PMID:1280592

Abstract

New analogues of cholecystokinin-7 (CCK-7) modified at amino acid residues 5 and 7 were assayed for their effect on gall bladder, pancreatic secretion, food intake (anorectic activity), amount of rearing (sedative activity) and analgesia, as well as their ability to inhibit 125I-CCK-8 binding to pancreatic cell membrane receptors and brain membrane receptors. The results were compared to the activities of standard compounds, CCK-8, cerulein, BOC-CCK-7 (BOC = tertbutyloxycarbonyl) and BOC-[Nle2,Nle5]CCK-7. All analogues exhibited agonistic effects. Their anorectic activity was significantly prolonged.

摘要

对在氨基酸残基5和7处进行修饰的胆囊收缩素-7（CCK-7）新类似物进行了检测，观察其对胆囊、胰腺分泌、食物摄取（厌食活性）、竖毛量（镇静活性）和镇痛的影响，以及它们抑制125I-CCK-8与胰腺细胞膜受体和脑膜受体结合的能力。将结果与标准化合物CCK-8、雨蛙肽、BOC-CCK-7（BOC = 叔丁氧羰基）和BOC-[Nle2,Nle5]CCK-7的活性进行比较。所有类似物均表现出激动作用。它们的厌食活性显著延长。