Discovery and development of orexin receptor antagonists as therapeutics for insomnia

• Published in: British journal of pharmacology Vol. 171; no. 2; pp. 283 - 293
• Main Authors: Winrow, C J, Renger, J J
• Format: Journal Article
• Language: English
• Published: England Blackwell Publishing Ltd 01.01.2014; The British Pharmacological Society
• Subjects: Acetamides - adverse effects; Acetamides - pharmacokinetics; Acetamides - pharmacology; Acetamides - therapeutic use; Animals; Biological Availability; Digestive system; Drug Design; Drug therapy; GABA; High-Throughput Screening Assays; Humans; Hypnotics and Sedatives - adverse effects; Hypnotics and Sedatives - pharmacokinetics; Hypnotics and Sedatives - pharmacology; Hypnotics and Sedatives - therapeutic use; Insomnia; Intracellular Signaling Peptides and Proteins - physiology; Isoquinolines - adverse effects; Isoquinolines - pharmacokinetics; Isoquinolines - pharmacology; Isoquinolines - therapeutic use; Neuropeptides - physiology; orexin receptor antagonist; Orexin Receptor Antagonists; Orexins; Signal Transduction - drug effects; Sleep; Sleep Initiation and Maintenance Disorders - drug therapy; Themed Section: Orexin Receptors; sleep; GABA; orexin receptor antagonist; insomnia

Insomnia persistently affects the quality and quantity of sleep. Currently approved treatments for insomnia primarily target γ‐aminobutyric acid‐A (GABA‐A) receptor signalling and include benzodiazepines and GABA‐A receptor modulators. These drugs are used to address this sleep disorder, but have th...