Journal article
Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors
GE Callander, M Olorunda, D Monna, E Schuepbach, D Langenegger, C Betschart, S Hintermann, D Behnke, S Cotesta, M Fendt, G Laue, S Ofner, E Briard, CE Gee, LH Jacobson, D Hoyer
Frontiers in Neuroscience | Published : 2013
Abstract
Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. Both efficacy and safety are crucial in clinical settings and thorough investigations of pharmacokinetics and pharmacodynamics can predict contributing factors such as duration of action and undesirable effects. To this end, we studied the interactions between various "dual" orexin receptor antagonists and the orexin receptors, OX1R and OX2R, over time using saturation and competition radioligand binding with [3H]-BBAC ((S)-N-([1,1'-biphenyl]-2-yl)-1-(2-((1-methyl-1H-benzo[d]imidazol-2-yl)thio)acetyl)pyrrolidine-2-carboxamide). In addition, the kinetics of these compounds were..
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Funding Acknowledgements
With the exception of Gabrielle E. Callander, the authors are either past or present Novartis employees, or have been supported by Novartis.