Further characterization of hemopressin peptide fragments in the opioid and cannabinoid systems

Eszter Szlavicz, Pannilage Shiromi Perera, C. Tömböly, Z. Helyes, Ferenc Zador, S. Benyhe, A. Borsodi, Engin Bojnik

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

BACKGROUND: Hemopressin, so-called because of its hypotensive effect, belongs to the derivatives of the hemoglobin α-chain. It was isolated from rat brain membrane homogenate by the use of catalytically inactive forms of endopeptidase 24.15 and neurolysin. Hemopressin has antihyperalgesic features that cannot be prevented by the opioid receptor antagonist, naloxone. METHODS: In the present study, we investigated whether hemopressin (PVNFKFLSH) and its C-terminally truncated fragment hemopressin 1-7 (PVNFKFL) have any influence on opioid-dependent signaling. Peptides have been analyzed using G-protein-stimulating functional and receptor bindings in this experimental setup. RESULTS: These 2 compounds efficiently activated the G-proteins, and naloxone slightly blocked this stimulation. At the same time, they were able to displace radiolabeled [3H]DAMGO, a selective ligand for μ-opioid system, at micromolar concentrations. Displacement caused by the heptapeptide was more modest compared with hemopressin. Experiments performed on cell lines overexpressing μ-opioid receptors verified the opioid activity of both hemopressins. Moreover, the CB1 cannabinoid receptor antagonist, AM251, significantly decreased their G-protein stimulatory effect. CONCLUSIONS: Here, we further confirm that hemopressins can modulate CB1 receptors and can have a slight modulatory effect on the opioid system.

Original languageEnglish
Pages (from-to)1488-1494
Number of pages7
JournalAnesthesia and Analgesia
Volume121
Issue number6
DOIs
Publication statusPublished - Dec 1 2015

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Peptide Fragments
Cannabinoids
Opioid Analgesics
GTP-Binding Proteins
Naloxone
neurolysin
thimet oligopeptidase
Cannabinoid Receptor Antagonists
Ala(2)-MePhe(4)-Gly(5)-enkephalin
Cannabinoid Receptor CB1
Narcotic Antagonists
hemopressin
Opioid Receptors
Hemoglobins
Ligands
Cell Line
Peptides
Membranes
Brain

ASJC Scopus subject areas

  • Anesthesiology and Pain Medicine

Cite this

Further characterization of hemopressin peptide fragments in the opioid and cannabinoid systems. / Szlavicz, Eszter; Perera, Pannilage Shiromi; Tömböly, C.; Helyes, Z.; Zador, Ferenc; Benyhe, S.; Borsodi, A.; Bojnik, Engin.

In: Anesthesia and Analgesia, Vol. 121, No. 6, 01.12.2015, p. 1488-1494.

Research output: Contribution to journalArticle

Szlavicz, Eszter ; Perera, Pannilage Shiromi ; Tömböly, C. ; Helyes, Z. ; Zador, Ferenc ; Benyhe, S. ; Borsodi, A. ; Bojnik, Engin. / Further characterization of hemopressin peptide fragments in the opioid and cannabinoid systems. In: Anesthesia and Analgesia. 2015 ; Vol. 121, No. 6. pp. 1488-1494.
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