Pharmacological characterization of new cholecystokinin analogues.
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.
D000681:Amylases / Q000378:metabolism*; D000698:Analgesia; D000818:Animals; D000855:Anorexia / Q000139:chemically induced*; D002766:Cholecystokinin / Q000031:analogs & derivatives* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005704:Gallbladder / Q000187:drug effects; D006168:Guinea Pigs; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D010179:Pancreas / Q000187:drug effects*; D051381:Rats; D017208:Rats, Wistar; D011949:Receptors, Cholecystokinin / Q000187:drug effects
D011949:Receptors, Cholecystokinin; D002766:Cholecystokinin; D000681:Amylases