This week in therapeutics

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Neurology

Pain

m-Opioid receptor (OPRM1; MOR)

SAR studies identified synthetic peptide analogs of endomorphin-1 that could be useful for treating pain. In vitro SAR studies identified a series of unnatural amino acid-bearing endomorphin-1 derivatives that agonized OPRM1 at subpicomolar concentrations. In an in vitro assay, the lead compound in the series had about a 35-fold longer half-life than natural endomorphin-1. In a mouse pain assay, the lead compound showed more potent analgesic effects than morphine. Next steps include further optimizing the compounds and conducting preclinical safety studies.

SciBX 6(14); doi:10.1038/scibx.2013.343
Published online April 11, 2013

Patent pending; unavailable for licensing

Liu, X. et al. J. Med. Chem.; published online March 11, 2013;
doi:10.1021/jm400195y
Contact: Rui Wang, Lanzhou University, Lanzhou, China
e-mail:
wangrui@lzu.edu.cn