Collect. Czech. Chem. Commun. 1991, 56, 1957-1962

Synthesis and biological activity in GPI test of scyliorhinin I and its analogues modified in position 8 by Leu, Sar and Pro residues

Krzysztof Rolkaa, Gotfryd Kupryszewskia, Piotr Janasb, Jarosław Myszorb and Zbigniew S. Hermanb

a Institute of Chemistry, University of Gdańsk, Sobieskiegi 18, 80-952 Gdańsk, Poland
b Department of Clinical Pharmacology, Silesian Academy of Medicine, Medyków 18, 40-752 Katowice, Poland


Three analogues of scyliorhinin I with Gly in position 8 substituted with Leu, Sar and Pro residues, were synthesized by the solid-phase method. The agonistic activity was determined on isolated guinea pig ileum. Analogues with Sar and Pro in position 8 appeared to be significantly more active than scyliorhinin I and the analogues with Leu in this position. For all analogues the Hill cooperativity coefficient is much lower than one suggesting that the interaction of these peptides with tachykinin receptor(s) in not a one-step reaction.