Ceruletide, ceruletide analogues and cholecystokinin octapeptide (CCK-8): effects on isolated intestinal preparations and gallbladders of guinea pigs and mice.
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.
D000818:Animals; D002108:Ceruletide / Q000031:analogs & derivatives / Q000494:pharmacology*; D003106:Colon / Q000187:drug effects*; D004386:Duodenum / Q000187:drug effects; D005704:Gallbladder / Q000187:drug effects*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects*; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects* / Q000502:physiology; D009928:Organ Specificity; D012844:Sincalide / Q000494:pharmacology*; D013270:Stomach / Q000187:drug effects; D013329:Structure-Activity Relationship
D002108:Ceruletide; D012844:Sincalide