A Nonpeptide Oxytocin Receptor Agonist for a Durable Relief of Inflammatory Pain

Authors
H Louis, Q Zhao, K Damien, I Perrine, A Virginie et al

Lab
Centre National de la Recherche Scientifique and University of Strasbourg, UPR3212 Institute of Cellular and Integrative Neurosciences, Strasbourg, France

Journal
Scientific Reports

Abstract
Oxytocin possesses several physiological and social functions, among which an important analgesic effect. For this purpose, oxytocin binds mainly to its unique receptor, both in the central nervous system and in the peripheral nociceptive terminal axon in the skin. However, despite its interesting analgesic properties and its current use in clinics to facilitate labor, oxytocin is not used in pain treatment. Indeed, it is rapidly metabolized, with a half-life in the blood circulation estimated at five minutes and in cerebrospinal fluid around twenty minutes in humans and rats. Moreover, oxytocin itself suffers from several additional drawbacks: a lack of specificity, an extremely poor oral absorption and distribution, and finally, a lack of patentability. Recently, a first non-peptide full agonist of oxytocin receptor (LIT-001) of low molecular weight has been synthesized with reported beneficial effect for social interactions after peripheral administration. In the present study, we report that a single intraperitoneal administration of LIT-001 in a rat model induces a long-lasting reduction in inflammatory pain-induced hyperalgesia symptoms, paving the way to an original drug development strategy for pain treatment.

BIOSEB Instruments Used:
Rodent pincher - analgesia meter (BIO-RP-M)