Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the μ-selective opioid receptor antagonist cyprodime

Helmut Schmidhammer, Angelika Stangl, Zsuzsanna Fürst, Eva Szabó, A. Borsodi, Dinesh Patel, John R. Traynor

Research output: Contribution to journalArticle

Abstract

The N-phenethyl analogue (compound 4) of the μ-selective opioid antagonist cyprodime (1) has been prepared and evaluated in radioligand binding, bioassays (guinea-pig ileum myenteric plexus and mouse vas deferens preparations) and the rat tail flick test. It was found to possess remarkable affinity and high preference for μ opioid receptors and high antinociceptive potency which is comparable to its N-methyl analogue 3.

Original languageEnglish
Pages (from-to)1923-1926
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume5
Issue number17
DOIs
Publication statusPublished - Sep 7 1995

Fingerprint

Myenteric Plexus
Vas Deferens
Narcotic Antagonists
Bioassay
Opioid Receptors
Ileum
Biological Assay
Tail
Rats
Guinea Pigs
cyprodime

ASJC Scopus subject areas

  • Biochemistry
  • Clinical Biochemistry
  • Molecular Biology
  • Molecular Medicine
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the μ-selective opioid receptor antagonist cyprodime. / Schmidhammer, Helmut; Stangl, Angelika; Fürst, Zsuzsanna; Szabó, Eva; Borsodi, A.; Patel, Dinesh; Traynor, John R.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 5, No. 17, 07.09.1995, p. 1923-1926.

Research output: Contribution to journalArticle

Schmidhammer, Helmut ; Stangl, Angelika ; Fürst, Zsuzsanna ; Szabó, Eva ; Borsodi, A. ; Patel, Dinesh ; Traynor, John R. / Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the μ-selective opioid receptor antagonist cyprodime. In: Bioorganic and Medicinal Chemistry Letters. 1995 ; Vol. 5, No. 17. pp. 1923-1926.
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