In vitro and in vivo pharmacology of novel naltrindole-related compounds

A. Z. Ronai, K. Gyires, H. Schmidhammer, S. Hosztafi, A. Borsodi, M. Spetea, T. Friedmann, P. Riba, Z. Furst

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2 Citations (Scopus)

Abstract

The pharmacological and receptor binding properties of some novel naltrindole (NTI) and naltrexone benzofurane (NTB) derivatives, modified at positions 3, 5, 14 and 17 were studied. Of the N-(17)-methyl NTI-derivatives, the 14-O-methyl derivative was a potent, highly selective δ opioid agonist whereas the 5-methyl derivative of the latter was a moderately potent μ agonist. Of the N-(17)-methyl NTB derivatives the 3,14-OH compound was a potent δ antagonist whereas the 3-O-methyl, 14-OH derivative was a moderately potent mixed agonist/antagonist at the same receptor. The N-methyl, 14-O-methyl NTI derivative ('morphindole') had in vivo a potent gastroprotective effect in rats in the ethanol-induced ulcer model.

Original languageEnglish
Pages (from-to)1-5
Number of pages5
JournalMedical Science Monitor
Volume3
Issue number1
Publication statusPublished - Jan 1 1997

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Keywords

  • N-methyl naltrexone-benzofurane derivatives
  • N-methyl naltrindole-derivatives (morphindoles)
  • gastroprotective effect
  • isolated organs

ASJC Scopus subject areas

  • Medicine(all)

Cite this

Ronai, A. Z., Gyires, K., Schmidhammer, H., Hosztafi, S., Borsodi, A., Spetea, M., Friedmann, T., Riba, P., & Furst, Z. (1997). In vitro and in vivo pharmacology of novel naltrindole-related compounds. Medical Science Monitor, 3(1), 1-5.