[Biological activity of cholecystokinin-(30-33) tetrapeptide analogs].
Analogues of the endogenous peptide corresponding to the 30-33 sequence of cholecystokinin (Trp-Met-Asp-Phe-NH2) were synthesized, and their biological activity was studied. It was shown that, in rats, the N-succinylated Nle2 analogue of this tetrapeptide exhibits increased anxiolytic properties in the dark-bright chamber test and an enhanced alcohol intake by both the control animals and the long-time alcohol-dependent animals under the conditions of free choice. Introduction of an isopropyl residue into the C-terminal amide of the Nle2 analogue resulted in the appearance of anxiolytic and antialcohol activity and the ability to increase the morphine analgesic effect in the tail-flick test on rats. The two synthesized analogues retained an affinity to cholecystokinin receptors.
Proskuriakova
T V
TV
Bespalova
Zh D
ZhD
Pal'keeva
M E
ME
Petrichenko
O B
OB
Pankratova
N V
NV
Shokhonova
V A
VA
Anokhina
I P
IP
D000428:Alcohol Drinking / Q000188:drug therapy*; D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001007:Anxiety / Q000139:chemically induced; D001522:Behavior, Animal / Q000187:drug effects*; D001921:Brain / Q000378:metabolism; D004357:Drug Synergism; D066298:In Vitro Techniques; D009020:Morphine / Q000494:pharmacology; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D010179:Pancreas / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D043886:Receptor, Cholecystokinin A / Q000378:metabolism; D043887:Receptor, Cholecystokinin B / Q000378:metabolism; D013329:Structure-Activity Relationship; D013758:Tetragastrin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D014364:Tryptophan / Q000737:chemistry
D000700:Analgesics; D014151:Anti-Anxiety Agents; D009842:Oligopeptides; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D013758:Tetragastrin; D009020:Morphine; D014364:Tryptophan