Opioid peptides. Structure-activity relationships of dermorphin endothiotetrapeptides. VII.
Severo Salvadori, Mauro Marastoni, Gianfranco Balboni, Roberto Tomatis, Gian Pietro Sarto
Abstract
Severo Salvadori, Mauro Marastoni, Gianfranco Balboni, Roberto Tomatis, Gian Pietro Sarto
Abstract
We describe the synthesis and preliminary in vitro and in vivo pharmacological tests of five endothiotetrapeptide analogues of the opioid heptapeptide dermorphin H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser.-NH2. The modification obtained by substituting Phet for Phe3 or Glyt for Gly4 provided further analogues with significant opioid activity.
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We describe the synthesis and preliminary in vitro and in vivo pharmacological tests of five endothiotetrapeptide analogues of the opioid heptapeptide dermorphin H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser.-NH2. The modification obtained by substituting Phet for Phe3 or Glyt for Gly4 provided further analogues with significant opioid activity.
Key concepts: Dermorphin, Opioid, Opioid peptide, In vivo, Chemistry, Pharmacology, Stereochemistry, In vitro