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The Discovery of Suvorexant, the First Orexin Receptor Drug for Insomnia

Annual review of pharmacology and toxicology, 2017-01, Vol.57 (1), p.509-533

2017

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Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

Nature structural & molecular biology, 2016-04, Vol.23 (4), p.293-299

2016

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International Union of Basic and Clinical Pharmacology. LXXXVI. Orexin receptor function, nomenclature and pharmacology

Pharmacological reviews, 2012-07, Vol.64 (3), p.389-420

2012

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Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress

Neuroscience, 2017-04, Vol.348, p.313-323

2017

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Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man

Scientific reports, 2016-06, Vol.6 (1), p.27147, Article 27147

2016

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Orexin receptors as therapeutic drug targets

Progress in Brain Research, 2012, Vol.198, p.163-188

2012

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

Neuropharmacology, 2012-02, Vol.62 (2), p.978-987

2012

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Mammalian TIMELESS and Tipin are Evolutionarily Conserved Replication Fork-associated Factors

Journal of molecular biology, 2007-02, Vol.366 (1), p.36-52

2007

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Inhibition of Orexin Signaling Promotes Sleep Yet Preserves Salient Arousability in Monkeys

Sleep (New York, N.Y.), 2016-03, Vol.39 (3), p.603-612

2016

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Promotion of Sleep by Suvorexant-A Novel Dual Orexin Receptor Antagonist

Journal of neurogenetics, 2011-03, Vol.25 (1-2), p.52-61

2011

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The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold

BMC neuroscience, 2013-08, Vol.14 (1), p.90-90, Article 90

2013

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The dual orexin receptor antagonist, DORA‐22, lowers histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine

Journal of neurochemistry, 2017-07, Vol.142 (2), p.204-214

2017

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Timeless links replication termination to mitotic kinase activation

PloS one, 2011-05, Vol.6 (5), p.e19596-e19596

2011

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Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology

Bioorganic & medicinal chemistry letters, 2016-12, Vol.26 (23), p.5809-5814

2016

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Illuminating the Circadian Clock in Monarch Butterfly Migration

Science (American Association for the Advancement of Science), 2003-05, Vol.300 (5623), p.1303-1305

2003

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Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists

Bioorganic & medicinal chemistry letters, 2017-03, Vol.27 (6), p.1364-1370

2017

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Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure

Neuropharmacology, 2010, Vol.58 (1), p.185-194

2010

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Orexin receptor antagonist-induced sleep does not impair the ability to wake in response to emotionally salient acoustic stimuli in dogs

Frontiers in behavioral neuroscience, 2014-05, Vol.8, p.182-182

2014

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Discovery of a Pharmacologically Active Antagonist of the Two-Pore-Domain Potassium Channel K2P9.1 (TASK-3)

ChemMedChem, 2012-01, Vol.7 (1), p.123-133

2012

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A palindrome-driven complex rearrangement of 22q11.2 and 8q24.1 elucidated using novel technologies

Genome Research, 2007-04, Vol.17 (4), p.470-481

2007

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Orexin signaling during social defeat stress influences subsequent social interaction behaviour and recognition memory

Behavioural brain research, 2019-01, Vol.356, p.444-452

2019

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A palindrome-mediated mechanism distinguishes translocations involving LCR-B of chromosome 22q11.2

Human molecular genetics, 2004-01, Vol.13 (1), p.103-115

2004

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Dual orexin receptor antagonists show distinct effects on locomotor performance, ethanol interaction and sleep architecture relative to gamma-aminobutyric acid-A receptor modulators

Frontiers in neuroscience, 2013-01, Vol.7, p.254-254

2013

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The Discovery of Suvorexant, the First Orexin Receptor Drug for Insomnia

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

International Union of Basic and Clinical Pharmacology. LXXXVI. Orexin receptor function, nomenclature and pharmacology

Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress

Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man

Orexin receptors as therapeutic drug targets

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

Mammalian TIMELESS and Tipin are Evolutionarily Conserved Replication Fork-associated Factors

Inhibition of Orexin Signaling Promotes Sleep Yet Preserves Salient Arousability in Monkeys

Promotion of Sleep by Suvorexant-A Novel Dual Orexin Receptor Antagonist

The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold

The dual orexin receptor antagonist, DORA‐22, lowers histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine

Timeless links replication termination to mitotic kinase activation

Discovery of 5′′-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2′:5′,3′′-terpyridine-3′-carboxamide (MK-1064): A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia

Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology

Illuminating the Circadian Clock in Monarch Butterfly Migration

Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists

Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure

Orexin receptor antagonist-induced sleep does not impair the ability to wake in response to emotionally salient acoustic stimuli in dogs

Discovery of a Pharmacologically Active Antagonist of the Two-Pore-Domain Potassium Channel K2P9.1 (TASK-3)

A palindrome-driven complex rearrangement of 22q11.2 and 8q24.1 elucidated using novel technologies

Orexin signaling during social defeat stress influences subsequent social interaction behaviour and recognition memory

A palindrome-mediated mechanism distinguishes translocations involving LCR-B of chromosome 22q11.2

Dual orexin receptor antagonists show distinct effects on locomotor performance, ethanol interaction and sleep architecture relative to gamma-aminobutyric acid-A receptor modulators

Safety, tolerability, and pharmacokinetics of antisense oligonucleotide BIIB078 in adults with C9orf72-associated amyotrophic lateral sclerosis: a phase 1, randomised, double blinded, placebo-controlled, multiple ascending dose study

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