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Effects on Inflammation of Newly-Synthesized Hexapeptide with Affinity to Opioid and Nociceptin Receptors

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Abstract

Following the discovery of the N/OFQ/NOP system and its modulatory role in physiological and pathophysiological processes, intensive study has started to find selective NOP ligands with hypothetic therapeutic potential. Among the agonists, a hexapeptide Ac-RYYRWK-NH2 has been identified. It expresses high NOP receptor affinity and selectivity. Its molecule was used as a template, in which Tyr5 was substituted by original β2-tryptophan analogue (S)-2-(1-methyl-1H-indol-3-yl)propionic residue (compound HP3) The new compound activates both NOP and opioid receptors. Having in mind that classical opioids, as well as nociceptin, are involved in modulating pain and inflammation, we examined the anti-inflammatory effect of newly-synthesized peptide HP3 on carrageenan-induced peripheral inflammation, and compared it with that of indomethacin (3 mg/kg). It was found that HP3 in dose 40 μg/kg exerts weaker anti-inflammatory action in the first 180 min of the experiment, but is equally effective with indomethacin 3 mg/kg at the end of the observation. The HP3 effect is due mainly of the activation of opioid receptors.

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Acknowledgments

The study was supported by Grant DTK 02/61 of the National Research Fund, Sofia, Bulgaria.

Conflict of interest

Rositsa Zamfirova, Polina Mateeva, Nikola Pavlov, and Emilia Naydenova declare that they have no conflict of interests.

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Authors and Affiliations

  1. Institute of Neurobiology, Bulgarian Academy of Sciences, 23 Acad. G. Bonchev str., 1113, Sofia, Bulgaria

    R. N. Zamfirova & P. I. Mateeva

  2. Department of Organic Chemistry, University of Chemical Technologies and Metallurgy, Sofia, Bulgaria

    N. D. Pavlov & E. D. Naydenova

Authors
  1. R. N. Zamfirova
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  2. P. I. Mateeva
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  3. N. D. Pavlov
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  4. E. D. Naydenova
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Correspondence to R. N. Zamfirova.

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Zamfirova, R.N., Mateeva, P.I., Pavlov, N.D. et al. Effects on Inflammation of Newly-Synthesized Hexapeptide with Affinity to Opioid and Nociceptin Receptors. Int J Pept Res Ther 20, 385–389 (2014). https://doi.org/10.1007/s10989-014-9401-4

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  • DOI: https://doi.org/10.1007/s10989-014-9401-4

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