Identification of Dmt-D-Lys-Phe-Phe-OH as a highly antinociceptive tetrapeptide metabolite of the opioid-neurotensin hybrid peptide PK20.
Journal Title: Pharmacological Reports - Year 2013, Vol 65, Issue 4
Abstract
Recently, we presented a novel compound (PK20, Dmt-D-Lys-Phe-Phe-Lys-Lys-Pro-Phe-Tle-Leu-OH) that targets single entity opioid and neurotensin pharmacophores. This endomorphin-2-like opioid peptide was introduced as a highly active analgesic because it elicited a strong dose- and time-dependent antinociceptive response when administered centrally and peripherally. Its pain-relieving activity was observed as rapidly as 5 min after drug injection. Such promising results led us to perform further studies, such as determining the resistance to enzymatic degradation, which resulted in obtaining a very stable opioid pharmacore PK20 metabolite.
Authors and Affiliations
Patrycja Kleczkowska, Engin Bojnik, Anna Leśniak, Piotr Kosson, Isabelle Van den Eynde, Steven Ballet, Sandor Benyhe, Dirk Tourwé, Andrzej Lipkowski
Keywords
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