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Contribution of opioid and neurotensin receptors in the anti‐inflammatory activity of PK20 hybrid compound in murine airways
Author(s) -
Russjan Ewelina,
Zając Dominika,
Sulejczak Dorota,
Kleczkowska Patrycja,
Kaczyńska Katarzyna
Publication year - 2021
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/1440-1681.13505
Subject(s) - neurotensin , receptor , opioid , pharmacology , chemistry , medicine , neuropeptide
PK20 is an anti‐inflammatory hybrid compound, composed of an endomorphin‐2‐like and neurotensin‐like fragments. The aim of the present study is to assess the contribution of particular pharmacophores to the activity of the hybrid tested. For this purpose, airway hyperresponsiveness, accumulation of inflammatory cells in bronchoalveolar lavage fluid (BALF), concentration of mouse mast cell protease, malondialdehyde and secretory phospholipase 2 activity in lung tissue, as well as production of pro‐inflammatory cytokines in BALF and lung were determined by using murine model of non‐atopic asthma. Blocking either neurotensin receptors or mu opioid receptors did not alter the potential of PK20 in reducing airway hyperresponsiveness. In studies of inflammatory cells, the beneficial effect of the entire peptide occurs to be mediated by the stimulation of neurotensin receptors. However, regarding cytokine and biochemical assays, pretreatment with both receptor antagonists resulted in a different effect on its activity depending on the parameter studied. To conclude, the activation of both the opioid and neurotensin receptors seems to be necessary to induce the full anti‐inflammatory activity of the hybrid compound.