Design and synthesis of cholecystokinin-4 dipeptide analogues with anxiolytic and anxiogenic activities |
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| Authors: | T. A. Gudasheva E. P. Kir’yanova L. G. Kolik M. A. Konstantinopol’skii S. B. Seredenin |
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| Affiliation: | (1) Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya ul. 8, Moscow, 125315, Russia |
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| Abstract: | A new series of dipeptide analogues of the general formula Ph(CH2) n CO-NH(CH2) m CO-Trp-NH2 (n = 1, 3–5; m = 1–3) was designed based on the structure of the endogenous tetrapeptide cholescystokinin-4 (CCK-4) and the topochemical Shemyakin-Ovchinnikov-Ivanov principle. The L-tryptophan derivatives exhibited anxiolytic properties and the D-tryptophan derivatives, anxiogenic properties. The dipeptide Ph(CH2)5CO-Gly-L-Trp-NH2 (GB-115) with the activity in rats of 0.05–0.2 mg/kg after oral and intraperitoneal administration was chosen for further studies as a promising anxiolytic agent. |
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| Keywords: | anxiolytic activity CCK-4 CCK-4 analogues cholecystokinin design dipeptides |
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