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The histamine H3 receptor as a therapeutic drug target for CNS disorders. 2009

Mark J Gemkow, and Adam J Davenport, and Silke Harich, and Bart A Ellenbroek, and Andrea Cesura, and David Hallett
Evotec AG, Schnackenburgallee 114, 22525 Hamburg, Germany. mark.gemkow@evotec.com

The histamine H3 receptor plays a regulatory role in the pre-synaptic release of histamine and other neurotransmitters, making it an attractive target for CNS indications including cognitive disorders, narcolepsy, ADHD and pain. As more and more H3 antagonists/H3 inverse agonists progress through the clinic, knowledge is gained to define the profile of the 'ideal' compound in terms of specificity, pharmacokinetic parameters and both duration and magnitude of receptor occupancy. Whether a single compound profile for the treatment of different disorders can be defined remains to be seen.

UI MeSH Term Description Entries
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D002493 Central Nervous System Diseases Diseases of any component of the brain (including the cerebral hemispheres, diencephalon, brain stem, and cerebellum) or the spinal cord. CNS Disease,Central Nervous System Disease,Central Nervous System Disorder,CNS Diseases,Central Nervous System Disorders
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D005544 Forecasting The prediction or projection of the nature of future problems or existing conditions based upon the extrapolation or interpretation of existing scientific data or by the application of scientific methodology. Futurology,Projections and Predictions,Future,Predictions and Projections
D006633 Histamine Antagonists Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only. Antihistamine,Antihistamines,Histamine Antagonist,Antagonist, Histamine,Antagonists, Histamine
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
D016503 Drug Delivery Systems Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity. Drug Targeting,Delivery System, Drug,Delivery Systems, Drug,Drug Delivery System,Drug Targetings,System, Drug Delivery,Systems, Drug Delivery,Targeting, Drug,Targetings, Drug
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

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