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Histamine, antihistamines, and the central nervous system

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Histamine is a central nervous system (CNS) neurotransmitter. It acts in the brain via three receptors, H1, H2, and H3. It is a mediator of “wakefulness” and its activity is necessary to maintain wakefulness, alertness, and reaction time. These activities can be impaired by H1-antagonists (reverse agonists) capable of penetrating the blood‐brain barrier. By blocking the homeostatic effects of histamine in the CNS, drowsiness and functional impairment with or without drowsiness can occur. Several tests have been designed to assess the effects of antihistamines on the CNS. These include subjective measurements of drowsiness and more objective measurements of impairment. Second-generation antihistamines have been designed to minimize blood‐brain barrier penetration by reducing lipophilicity and increasing the affinity for P-aminnoglycoprotein.

Keywords: Antihistamines; P-aminoglycoprotein; central nervous system; central nervous system impairment; drowsiness; lipophilicity; reverse agonists

Document Type: Research Article


Affiliations: Departments of Medicine and Pediatrics, University of Tennessee, Memphis, Tennessee, USA.

Publication date: 2009-09-01

More about this publication?
  • Allergy and Asthma Proceedings is a peer reviewed publication dedicated to distributing timely scientific research regarding advancements in the knowledge and practice of allergy, asthma and immunology. Its primary readership consists of allergists and pulmonologists.

    The goal of the Proceedings is to publish articles with a predominantly clinical focus which directly impact quality of care for patients with allergic disease and asthma.

    Featured topics include asthma, rhinitis, sinusitis, food allergies, allergic skin diseases, diagnostic techniques, allergens, and treatment modalities. Published material includes peer-reviewed original research, clinical trials and review articles.

    Articles marked "F" offer free full text for personal noncommercial use only.

    The journal is indexed in Thomson Reuters Web of Science and Science Citation Index Expanded, plus the National Library of Medicine's PubMed service.
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