Dynorphin A (1-8) analog, E-2078, is stable in human and rhesus monkey blood

Jim Yu, Eduardo R. Butelman, James H. Woods, Brian T. Chait, Mary Jeanne Kreek

Research output: Contribution to journalArticlepeer-review

18 Scopus citations

Abstract

E-2078 is a dynorphin A (1-8) analog, [N-methyl-Tyr1, N-methyl-Arg7- D-Leu8] Dyn A (1-8) ethylamide. Its biochemical stability against enzymatic degradation in vitro in human and rhesus monkey blood, and in vivo in rhesus monkey blood was studied using matrix-assisted laser desorption/ionization mass spectrometry. In vitro studies were carried out in freshly drawn human and rhesus monkey blood, incubated at 37°C for various time periods. In vivo studies were conducted by E-2078 i.v. injection to rhesus monkeys, and blood samples were collected at various time points after the injection. It was found that E-2078 was stable against enzymatic degradation in vitro in freshly drawn human and rhesus monkey blood. Minor biotransformation products from E-2078, such as E (1-4), E (1-5) and E (3-6), were detected in vitro in some human and rhesus monkey blood, but they made up less than 5% of the total starting E-2078 peptide. No biotransformation products were detected in the blood samples from in vivo studies. The apparent half-life of elimination of E-2078 in vivo from the rhesus monkey blood was determined to be 44.0 min.

Original languageEnglish (US)
Pages (from-to)1147-1151
Number of pages5
JournalJournal of Pharmacology and Experimental Therapeutics
Volume280
Issue number3
StatePublished - Mar 1997
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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