Zetler G
Peptides. 1984 Jul-Aug;5(4):729-36. doi: 10.1016/0196-9781(84)90014-7.
The smooth muscle stimulatory effects of cholecystokinin octapeptide (CCK-8), ceruletide (CER), ten analogues of CER, and carbachol were studied in isolated organs of the guinea pig and the mouse (stomach, ileum, duodenum, colon and gallbladder). On a molar basis, CCK-8 and CER had in all organs except stomach greater potency (lower EC50) than carbachol. The effectiveness (Emax) of CCK-8 and CER was in the gut less than that of carbachol, in the guinea pig gallbladder equal with and in the mouse gallbladder superior to that of carbachol. The alteration of peptide structure was virtually without influence on effectiveness; however, it greatly modified the potency and the organ selectivity of the effect. There was no clear-cut correlation between the potency to stimulate smooth muscle and to alter the behavior of the mouse.
在豚鼠和小鼠的离体器官(胃、回肠、十二指肠、结肠和胆囊)中研究了八肽胆囊收缩素(CCK-8)、蛙皮素(CER)、CER的十种类似物以及卡巴胆碱对平滑肌的刺激作用。在摩尔基础上,CCK-8和CER在除胃以外的所有器官中比卡巴胆碱具有更高的效力(更低的EC50)。CCK-8和CER的效能(Emax)在肠道中低于卡巴胆碱,在豚鼠胆囊中与卡巴胆碱相当,在小鼠胆囊中高于卡巴胆碱。肽结构的改变对效能几乎没有影响;然而,它极大地改变了效力和效应的器官选择性。刺激平滑肌的效力与改变小鼠行为之间没有明确的相关性。