Biological activity of cholecystokinin (30–33) tetrapeptide analogues

Analogues of the endogenous peptide corresponding to the 30-33 sequence of cholecystokinin (Trp-Met-Asp-Phe-NH sub(2)) were synthesized, and their biological activity was studied. It was shown that, in rats, the N-succinylated Nle super(2) analogue of this tetrapeptide exhibits increased anxiolytic...

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Bibliographic Details
Published in:Russian journal of bioorganic chemistry 2005-03, Vol.31 (2), p.119-127
Main Authors: Proskuryakova, T. V., Bespalova, Zh. D., Pal’keeva, M. E., Petrichenko, O. B., Pankratova, N. V., Shokhonova, V. A., Anokhina, I. P.
Format: Article
Language:English
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Summary:Analogues of the endogenous peptide corresponding to the 30-33 sequence of cholecystokinin (Trp-Met-Asp-Phe-NH sub(2)) were synthesized, and their biological activity was studied. It was shown that, in rats, the N-succinylated Nle super(2) analogue of this tetrapeptide exhibits increased anxiolytic properties in the dark-light chamber test and an enhanced alcohol intake by both the control animals and the alcohol-dependent animals under the conditions of free choice. Introduction of an isopropyl residue into the C-terminal amide of the Nle super(2) analogue resulted in the appearance of anxiogenic 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 for cholecystokinin receptors.
ISSN:1068-1620
1573-9163
1608-330X
DOI:10.1007/s11171-005-0016-6