Biomaterial Database

Histamine H(3) receptor (H(3)R) antagonists and inverse agonists in the treatment of sleep disorders. 2011

Meredith Broderick, and Tony Masri

Sound Sleep Health, Seattle, WA 98125, USA. mbroderick@soundsleephealth.com

After the discovery and characterization of the H(3)R and H(4)R receptors, they have become widely anticipated as potential therapeutic agents in the treatment of sleep disorders. In preliminary studies, histamine H(3) receptor (H(3)R) antagonists and inverse agonists have demonstrated promise in the treatment of sleep disorders associated with excessive daytime sleepiness. This review article summarizes the current research in this area and characteristics of H(3)R and H(3)R antagonists and inverse agonists in development.

UI	MeSH Term	Description	Entries
D006970	Disorders of Excessive Somnolence	Disorders characterized by hypersomnolence during normal waking hours that may impair cognitive functioning. Subtypes include primary hypersomnia disorders (e.g., IDIOPATHIC HYPERSOMNOLENCE; NARCOLEPSY; and KLEINE-LEVIN SYNDROME) and secondary hypersomnia disorders where excessive somnolence can be attributed to a known cause (e.g., drug affect, MENTAL DISORDERS, and SLEEP APNEA SYNDROME). (From J Neurol Sci 1998 Jan 8;153(2):192-202; Thorpy, Principles and Practice of Sleep Medicine, 2nd ed, p320)	Daytime Sleepiness,Daytime Somnolence,Excessive Daytime Sleepiness,Hypersomnia,Hypersomnolence,Primary Hypersomnia Disorders,Secondary Hypersomnia Disorders,DOES (Disorders of Excessive Somnolence),Excessive Somnolence Disorders,Hypersomnia, Recurrent,Hypersomnolence Disorders,Hypersomnolence Disorders, Primary,Hypersomnolence Disorders, Secondary,Primary Hypersomnolence Disorders,Secondary Hypersomnolence Disorders,DOESs (Disorders of Excessive Somnolence),Daytime Sleepiness, Excessive,Daytime Sleepinesses,Daytime Somnolences,Excessive Daytime Sleepinesses,Excessive Somnolence Disorder,Hypersomnia Disorder, Primary,Hypersomnia Disorder, Secondary,Hypersomnias,Hypersomnolence Disorder,Hypersomnolence Disorder, Primary,Hypersomnolence Disorder, Secondary,Primary Hypersomnia Disorder,Primary Hypersomnolence Disorder,Recurrent Hypersomnia,Recurrent Hypersomnias,Secondary Hypersomnia Disorder,Secondary Hypersomnolence Disorder,Sleepiness, Daytime,Sleepiness, Excessive Daytime,Somnolence Disorder, Excessive,Somnolence, Daytime
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D012893	Sleep Wake Disorders	Abnormal sleep-wake schedule or pattern associated with the CIRCADIAN RHYTHM which affect the length, timing, and/or rigidity of the sleep-wake cycle relative to the day-night cycle.	Sleep Disorders,Long Sleeper Syndrome,Short Sleep Phenotype,Short Sleeper Syndrome,Sleep-Related Neurogenic Tachypnea,Subwakefullness Syndrome,Disorder, Sleep,Disorder, Sleep Wake,Disorders, Sleep,Disorders, Sleep Wake,Long Sleeper Syndromes,Neurogenic Tachypnea, Sleep-Related,Neurogenic Tachypneas, Sleep-Related,Phenotype, Short Sleep,Phenotypes, Short Sleep,Short Sleep Phenotypes,Short Sleeper Syndromes,Sleep Disorder,Sleep Phenotypes, Short,Sleep Related Neurogenic Tachypnea,Sleep Wake Disorder,Sleep-Related Neurogenic Tachypneas,Sleeper Syndrome, Long,Sleeper Syndrome, Short,Sleeper Syndromes, Long,Sleeper Syndromes, Short,Subwakefullness Syndromes,Syndrome, Long Sleeper,Syndrome, Short Sleeper,Syndrome, Subwakefullness,Syndromes, Long Sleeper,Syndromes, Short Sleeper,Syndromes, Subwakefullness,Tachypnea, Sleep-Related Neurogenic,Tachypneas, Sleep-Related Neurogenic,Wake Disorder, Sleep,Wake Disorders, Sleep
D015195	Drug Design	The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis.	Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D017442	Histamine Agonists	Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.	Histamine H1 Agonists,Histamine H2 Agonists,Histamine H3 Agonists,H1 Agonist,H1 Agonists,H2 Agonist,H2 Agonists,H3 Agonist,H3 Agonists,Histamine Agonist,Histamine H1 Agonist,Histamine H1 Receptor Agonist,Histamine H1 Receptor Agonists,Histamine H2 Agonist,Histamine H2 Receptor Agonist,Histamine H2 Receptor Agonists,Histamine H3 Agonist,Histamine H3 Receptor Agonists,Histaminergic Agonist,Histaminergic Agonists,Agonist, H1,Agonist, H2,Agonist, H3,Agonist, Histamine,Agonist, Histamine H1,Agonist, Histamine H2,Agonist, Histamine H3,Agonist, Histaminergic,Agonists, H1,Agonists, H2,Agonists, H3,Agonists, Histamine,Agonists, Histamine H1,Agonists, Histamine H2,Agonists, Histamine H3,Agonists, Histaminergic,H1 Agonist, Histamine,H1 Agonists, Histamine,H2 Agonist, Histamine,H2 Agonists, Histamine,H3 Agonist, Histamine,H3 Agonists, Histamine
D054314	Drug Inverse Agonism	Phenomena and pharmaceutics of compounds that bind to the same receptor binding-site as an agonist (DRUG AGONISM) for that receptor but exerts the opposite pharmacological effect.	Inverse Agonism,Inverse Agonist,Inverse Agonists,Agonism, Drug Inverse,Agonism, Inverse,Agonisms, Inverse,Agonist, Inverse,Agonists, Inverse,Inverse Agonism, Drug,Inverse Agonisms
D054828	Histamine H3 Antagonists	Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.	Antihistaminics, H3,Histamine H3 Receptor Antagonists,Histamine H3 Blockers,Antagonists, Histamine H3,Blockers, Histamine H3,H3 Antagonists, Histamine,H3 Antihistaminics,H3 Blockers, Histamine
D018100	Receptors, Histamine H3	A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)	H3 Receptor,Histamine H3 Receptors,H3 Receptors,Histamine H3 Receptor,H3 Receptor, Histamine,H3 Receptors, Histamine,Receptor, H3,Receptor, Histamine H3,Receptors, H3