Ceruletide (Caerulein) is a potent agonist of cholecystokinin receptor and it also is a safe and effective cholecystokinetic agent. It has a direct spasmogenic effect on the gallbladder muscle and bile ducts.

Ceruletide is the same as biologically and chemically to the human gastrointestinal hormones cholecystokinin-pancreozymin (CCK) and gastrin II. Ceruletide stimulates gallbladder contraction while delaying gastric emptying and inhibiting motility in the proximal duodenum [1]. Ceruletide in supramaximal but not in physiological doses activate NF-kappaB/Rel in vitro. This activation may induce a self-defending genetic program before the onset of cellular injury and may prevent higher degrees of damage of pancreatic acinar cells after secretagogue hyperstimulation [2].

Ceruletide (5-15 ng/kg, i.v.) shows a marked spasmogenic effect on the pylorus of rats. Ceruletide also reduces blood pressure in anesthetized dogs [1]. Ceruletide (0.4-0.5 mcg/kg, i.v.; 3-4 mcg/kg, s.c.) results in emesis and evacuation of the bowel in the intact conscious dog, and recovery is complete 15-30 min after i. v. administration and 2-4 hr after s.c. administration. Ceruletide SBA stimulation may perform as well as PP SBA stimulation in dogs with the portosystemic shunt and be more sensitive for the detection of hepatic dysfunction in dogs with the upper respiratory disease [3].