[HTML][HTML] Orexins as novel therapeutic targets in inflammatory and neurodegenerative diseases

A Couvineau, T Voisin, P Nicole, V Gratio… - Frontiers in …, 2019 - frontiersin.org
Orexins [orexin-A (OXA) and orexin-B (OXB)] are two isoforms of neuropeptides produced by
the hypothalamus. The main biological actions of orexins, focused on the central nervous …

Orexin receptor antagonists for the treatment of insomnia and potential treatment of other neuropsychiatric indications

WJ Herring, T Roth, AD Krystal… - Journal of sleep …, 2019 - Wiley Online Library
In this review, we outline the role of orexin receptor antagonists in disorders of sleep/wake
and other potential neuropsychiatric conditions, with a focus on suvorexant, which is …

[HTML][HTML] The selective orexin-2 antagonist seltorexant (JNJ-42847922/MIN-202) shows antidepressant and sleep-promoting effects in patients with major depressive …

K Recourt, P de Boer, R Zuiker, R Luthringer… - Translational …, 2019 - nature.com
Excessive arousal has a role in the pathophysiology of major depressive disorder (MDD).
Seltorexant (JNJ-42847922/MIN-202) is a selective antagonist of the human orexin-2 …

The selective orexin-2 receptor antagonist seltorexant improves sleep: an exploratory double-blind, placebo controlled, crossover study in antidepressant-treated …

S Brooks, GE Jacobs, P De Boer… - Journal of …, 2019 - journals.sagepub.com
Background: Insomnia is common in patients with major depressive disorder. Although
antidepressants improve mood, insomnia often persists as a result of physiological …

Preclinical in vivo characterization of lemborexant (E2006), a novel dual orexin receptor antagonist for sleep/wake regulation

CT Beuckmann, T Ueno, M Nakagawa, M Suzuki… - Sleep, 2019 - academic.oup.com
Abstract Study Objectives To present results from in vivo studies underlying the preclinical
development of lemborexant (E2006), a novel dual orexin (hypocretin) receptor antagonist …

Lysophospholipid (S1P) receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

V Blaho, J Chun, D Jonnalagadda… - IUPHAR/BPS Guide …, 2019 - journals.ed.ac.uk
Abstract Sphingosine 1-phosphate (S1P) receptors (nomenclature as agreed by the NC-
IUPHAR Subcommittee on Lysophospholipid receptors [70]) are activated by the …

Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure–Activity Relationships, and Sleep‐Promoting Properties in Rats

C Brotschi, C Roch, J Gatfield, A Treiber… - …, 2019 - Wiley Online Library
The orexin system plays an important role in the regulation of wakefulness. Suvorexant, a
dual orexin receptor antagonist (DORA) is approved for the treatment of primary insomnia …

[PDF][PDF] Targeting Orexin Neurons for Treatment of Obesity is It Feasible in Human Being-A Systematic Review

KK Kaur - Journal of Neurology Research Reviews & Reports …, 2019 - researchgate.net
Obesity is increasing at epidemic proportions both in children and adults posing a big public
health problem among children as well as adults. With parallel increase in comorbidities like …

[PDF][PDF] MOLECULAR EVOLUTION OF G PROTEIN-COUPLED RECEPTORS—INSIGHTS INTO THE OREXIN SYSTEM

O RE - 2019 - helda.helsinki.fi
The diversity of G protein-coupled receptors is a fundamental element in this thesis. GPCRs
are the largest family of membrane proteins, with about 800 in humans. While the human …

[HTML][HTML] Small-molecule ligands as challenge for positron emission tomography of peptide receptors in neurons and microglia of the brain

M Pissarek - World Journal of Neuroscience, 2019 - scirp.org
Neuropeptide and chemokine receptors of the G protein-coupled receptor (GPCR) family
belong to different classes and subgroups providing different docking sites and special …