Orexin (Hypocretin) Receptor Agonists and Antagonists for Treatment of Sleep Disorders

Orexin Receptor Antagonism, a New Sleep-Enabling Paradigm: A Proof-of-Concept Clinical Trial

(2012) P Hoever et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Differential Effects of a Dual Orexin Receptor Antagonist (SB-649868) and Zolpidem on Sleep Initiation and Consolidation, SWS, REM Sleep and EEG Power Spectra in a Model of Situational Insomnia

(2012) Paolo Bettica et al.   NEUROPSYCHOPHARMACOLOGY

Dual Hypocretin Receptor Antagonism Is More Effective for Sleep Promotion than Antagonism of Either Receptor Alone

(2012) Stephen R. Morairty et al.   PLoS One

Mechanism for Hypocretin-mediated sleep-to-wake transitions

(2012) M. E. Carter et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Orexin Receptors: Pharmacology and Therapeutic Opportunities

(2011) Thomas E. Scammell et al.   Annual Review of Pharmacology and Toxicology

Differential Roles of Orexin Receptor-1 and -2 in the Regulation of Non-REM and REM Sleep

(2011) M. Mieda et al.   JOURNAL OF NEUROSCIENCE

Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia

(2011) Christopher J. Winrow et al.   NEUROPHARMACOLOGY

Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in narcoleptic mice

(2011) T. Mochizuki et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Connectomics of orexin-producing neurons: interface of systems of emotion, energy homeostasis and arousal

(2011) Takeshi Sakurai et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Sleep Neurobiology from a Clinical Perspective

(2011)   SLEEP

Orexin Receptor Antagonism, a New Sleep-Promoting Paradigm: An Ascending Single-Dose Study With Almorexant

(2010) P Hoever et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Disposition and Metabolism of [14C]SB-649868, an Orexin 1 and 2 Receptor Antagonist, in Humans

(2010) C. Renzulli et al.   DRUG METABOLISM AND DISPOSITION

Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia

(2010) Christopher D. Cox et al.   JOURNAL OF MEDICINAL CHEMISTRY

Orexin Directly Excites Orexin Neurons through Orexin 2 Receptor

(2010) A. Yamanaka et al.   JOURNAL OF NEUROSCIENCE

Hypocretin/orexin and narcolepsy: new basic and clinical insights

(2009) S. Nishino et al.   Acta Physiologica

Sleep Homeostasis Modulates Hypocretin-Mediated Sleep-to-Wake Transitions

(2009) M. E. Carter et al.   JOURNAL OF NEUROSCIENCE

Blockade of Orexin-1 Receptors Attenuates Orexin-2 Receptor Antagonism-Induced Sleep Promotion in the Rat

(2009) C. Dugovic et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Neuronal activity of orexin and non-orexin waking-active neurons during wake–sleep states in the mouse

(2008) K. Takahashi et al.   NEUROSCIENCE