Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Neurology

Insomnia

Orexin 2 receptor (HCRTR2; OX2R)

In vitro and mouse studies identified an OX2R-selective antagonist that may help treat insomnia. In vitro, the antagonist bound OX2R with a Ki of about 14 nM and about 30-fold selectivity over OX1R (HCRTR1). In mouse locomotor activity studies, the antagonist increased inactivity compared with vehicle. In electrical brain recording studies in mice, the antagonist increased non-rapid eye movement (NREM) sleep time compared with vehicle and had no effect on REM sleep time. Next steps could include testing the antagonist in the clinic for primary insomnia.

SciBX 6(38); doi:10.1038/scibx.2013.1069
Published online Oct. 3, 2013

Patented by Novartis AG; licensing status undisclosed

Bestschart, C. et al. J. Med. Chem.; published online Aug. 21, 2013;
doi:10.1021/jm4007627
Contact: Claudia Betschart, Novartis Institutes for BioMedical Research, Basel, Switzerland
e-mail:
claudia.betschart@novartis.com

Contact: Samuel Hintermann, same affiliation as above
e-mail:
samuel.hintermann@novartis.com