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Histamine pharmacology and new CNS drug targets.
- Source :
-
CNS neuroscience & therapeutics [CNS Neurosci Ther] 2011 Dec; Vol. 17 (6), pp. 620-8. Date of Electronic Publication: 2010 Nov 22. - Publication Year :
- 2011
-
Abstract
- During the last decade, the identification of a number of novel drug targets led to the development of promising new compounds which are currently under evaluation for their therapeutic prospective in CNS related disorders. Besides the established pleiotropic regulatory functions in the periphery, the interest in the potential homeostatic role of histamine in the brain was revived following the identification of H(3) and H(4) receptors some years ago. Complementing classical CNS pharmacology, the development of selective histamine receptor agonists, antagonists, and inverse agonists provides the lead for the potential exploitation of the histaminergic system in the treatment of brain pathologies. Although no CNS disease entity has been associated directly to brain histamine dysfunction until now, the H(3) receptor is recognized as a drug target for neuropathic pain, sleep-wake disorders, including narcolepsy, and cognitive impairment associated with attention deficit hyperactivity disorder, schizophrenia, Alzheimer's, or Parkinson's disease, while the first H(3) receptor ligands have already entered phase I-III clinical trials. Interestingly, the localization of the immunomodulatory H(4) receptor in the nervous system exposes attractive perspectives for the therapeutic exploitation of this new drug target in neuroimmunopharmacology. This review focuses on a concise presentation of the current "translational research" approach that exploits the latest advances in histamine pharmacology for the development of beneficial drug targets for the treatment of neuronal disorders, such as neuropathic pain, cognitive, and sleep-wake pathologies. Furthermore, the role of the brain histaminergic system(s) in neuroprotection and neuroimmunology/inflammation remains a challenging research area that is currently under consideration.<br /> (© 2010 Blackwell Publishing Ltd.)
- Subjects :
- Animals
Brain physiology
Brain Chemistry physiology
Cognition Disorders drug therapy
Humans
Multiple Sclerosis drug therapy
Neuralgia drug therapy
Neuroprotective Agents pharmacology
Receptors, G-Protein-Coupled drug effects
Receptors, G-Protein-Coupled physiology
Receptors, Histamine physiology
Receptors, Histamine H3 drug effects
Receptors, Histamine H3 physiology
Receptors, Histamine H4
Sleep Wake Disorders drug therapy
Central Nervous System Agents pharmacology
Central Nervous System Agents therapeutic use
Histamine physiology
Histamine Agents pharmacology
Histamine Agents therapeutic use
Receptors, Histamine drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1755-5949
- Volume :
- 17
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- CNS neuroscience & therapeutics
- Publication Type :
- Academic Journal
- Accession number :
- 22070192
- Full Text :
- https://doi.org/10.1111/j.1755-5949.2010.00212.x