The opiate-like activity of six newly synthesized dermorphin-related tetrapeptides was determined in guinea pig ileum, mouse vas deferens and mouse tail-flick tests. Naloxone was a powerful antagonist of all compounds. Moreover, the biological activities of the compounds under examination were correlated in a statistically significant way to the lipophilic character of the C-terminal substituents and to an indicator variable taking into account the presence of an amidic group at the C-terminus. © 1984 S. Karger AG, Basel.
Structure activity relationship for dermophin related tetrapeptides
SARTO, Gianpietro;BOREA, Pier Andrea;SALVADORI, Severo;TOMATIS, Roberto
1984
Abstract
The opiate-like activity of six newly synthesized dermorphin-related tetrapeptides was determined in guinea pig ileum, mouse vas deferens and mouse tail-flick tests. Naloxone was a powerful antagonist of all compounds. Moreover, the biological activities of the compounds under examination were correlated in a statistically significant way to the lipophilic character of the C-terminal substituents and to an indicator variable taking into account the presence of an amidic group at the C-terminus. © 1984 S. Karger AG, Basel.File in questo prodotto:
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