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Orexin 1 receptor (HCRTR1; OX1R)

In vitro and rat studies identified selective, tetrahydroisoquinoline-based OX1R antagonists that could help treat addiction. In in vitro assays, the tetrahydroisoquinoline-based antagonists showed higher specificities and potencies for OX1R than OX2R (HCRTR2). In a rat model of addiction, one of the most potent and selective antagonists decreased cocaine-induced addiction behaviors compared with vehicle. Next steps could include further optimization of the compounds to improve their potency and selectivity.
Merck & Co. Inc.'s dual OX1R and OX2R antagonist suvorexant is under review to treat insomnia.
At least two other companies have OX1R antagonists in Phase II or earlier testing for neurological indications.

SciBX 6(36); doi:10.1038/scibx.2013.1000
Published online Sept. 19, 2013

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Perrey, D.A. et al. J. Med. Chem.; published online Aug. 13, 2013;
Contact: Yanan Zhang, RTI International,
Research Triangle Park, N.C.