Synthesis and Infarction-Limiting Properties of Peptide Agonists of Opioid Receptors

S. Yu Tsibul’nikov*, A. V. Mukhomedzyanov, L. N. Maslov, M. V. Ovchinnikov, M. V. Sidorova, E. V. Kudryavtseva, Yu V. Bushov, Yu B. Lishmanov, I. Khaliulin

*Corresponding author for this work

Research output: Contribution to journalArticle (Academic Journal)peer-review

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Abstract

Three structurally different peptide agonists of opioid receptors, i.e., gludalan, deltolei, and dalargin, were synthesized and assessed for infarction-limiting effects in rats with coronary occlusion (45 min) and reperfusion (2 h). The opioid peptides dalargin and gludalan (0.1 mg/kg) and deltolei (0.03, 0.1, and 0.2 mg/kg) were injected 5 min before reperfusion. It was found that gludalan and deltolei at a dose of 0.1 mg/kg decreased the ratio of infarction size to the area at risk (IS/AAR) whereas dalargin did not affect the IS. The infarction-limiting effect of deltolei disappeared if the peptide dose was decreased (0.03 mg/kg) or increased (0.2 mg/kg). The opioid receptor antagonists naltrexone (5 mg/kg) or naloxone methiodide (5 mg/kg), which does not penetrate the blood—brain barrier, eliminated the infarction-limiting effect of gludalan.

Original languageEnglish
Pages (from-to)291-293
Number of pages3
JournalPharmaceutical Chemistry Journal
Volume52
Issue number4
Early online date16 Jul 2018
DOIs
Publication statusPublished - Jul 2018

Keywords

  • heart
  • opioids
  • postconditioning
  • reperfusion

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