Peptides containing N-allyl or N, N-diallyl groups at the N-terminus have been synthesized as potential opioid antagonists. A number of analogues with an amide bond replaced by a thiomethylene group have also been prepared. In brain binding assays and in guinea-pig ileum and mouse vas deferens preparations, the analogues generally displayed low affinity for μ- and δ-receptors as well as agonist activities in in vitro tests. N,N-Diallyl-Phe-D-Ala-Phe-Gly- NH2 (28) was found to be a moderately potent but highly selective antagonist at δ opiate receptors.

Opioid agonists and antagonists. Peptides containing N-terminal allyl groups and/or a thiomethylene linkage in place of a peptide bond

SALVADORI, Severo;MARASTONI, Mauro;TOMATIS, Roberto;BOREA, Pier Andrea;BIANCHI, Clementina
1988

Abstract

Peptides containing N-allyl or N, N-diallyl groups at the N-terminus have been synthesized as potential opioid antagonists. A number of analogues with an amide bond replaced by a thiomethylene group have also been prepared. In brain binding assays and in guinea-pig ileum and mouse vas deferens preparations, the analogues generally displayed low affinity for μ- and δ-receptors as well as agonist activities in in vitro tests. N,N-Diallyl-Phe-D-Ala-Phe-Gly- NH2 (28) was found to be a moderately potent but highly selective antagonist at δ opiate receptors.
1988
Balboni, G.; Salvadori, Severo; Marastoni, Mauro; Tomatis, Roberto; Borea, Pier Andrea; Bianchi, Clementina
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/460556
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