Journal article

An imidazole based H-Phe-Phe-NH2 peptidomimetic with anti-allodynic effect in spared nerve injury mice

Anna Skogh, Anna Lesniak, Christian Skold, Maria Karlgren, Fabienne Z Gaugaz, Richard Svensson, Shanti Diwakarla, Anna Jonsson, Rebecca Fransson, Fred Nyberg, Mathias Hallberg, Anja Sandstrom

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | PERGAMON-ELSEVIER SCIENCE LTD | Published : 2018

Abstract

The dipeptide amide H-Phe-Phe-NH2 (1) that previously was identified as a ligand for the substance P 1-7 (SP1-7) binding site exerts intriguing results in animal models of neuropathic pain after central but not after peripheral administration. The dipeptide 1 is derived from stepwise modifications of the anti-nociceptive heptapeptide SP1-7 and the tetrapeptide endomorphin-2 that is also binding to the SP1-7 site. We herein report a strong anti-allodynic effect of a new H-Phe-Phe-NH2 peptidomimetic (4) comprising an imidazole ring as a bioisosteric element, in the spare nerve injury (SNI) mice model after peripheral administration. Peptidomimetic 4 was stable in plasma, displayed a fair membr..

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University of Melbourne Researchers