Structure-Activity Studies of Dermorphin. Synthesis and Some Pharmacological Data of Dermorphin and Its 1-Substituted Analogues

Krzysztof Darlak, Zbigniew Grzonka, Piotr Janicki, Andrzej Czlonkowski, S. Witold Gumulka

Research output: Contribution to journalArticle

25 Scopus citations

Abstract

Dermorphin and its analogues substituted at position 1 by N-acetyltyrosine, O-methyltyrosine, phenylalanine, D-phenylalanine, or alanine were obtained by solid-phase peptide synthesis. Their pharmacological effects were studied in vitro by the guinea pig ileum method and in vivo by the hot plate method, and the results were compared with those of morphine. The most pronounced activity was shown for dermorphin. A radioreceptor study showed a moderate affinity of dermorphin and its Tyr(Me) analogue for the opiate receptor sites from striatal homogenates.

Original languageEnglish (US)
Pages (from-to)1445-1447
Number of pages3
JournalJournal of Medicinal Chemistry
Volume26
Issue number10
DOIs
StatePublished - Oct 1983

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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