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The third histamine receptor. Highly potent and selective ligands
J M Arrang1, M Garbarg, J C Lancelot
1Unité 109 de Neurobiologie et Pharmacologie, Centre Paul-Broca, INSERM, Paris, France.
International Archives of Allergy and Applied Immunology
|January 1, 1989
Summary
The H3 receptor, found in the brain and lung mast cells, may offer new treatments for allergic diseases. A potent agonist, (R)-alpha-methylhistamine, shows promise for therapeutic applications.
Area of Science:
- Neuroscience
- Immunology
- Pharmacology
Background:
- The third histamine receptor (H3R) was initially identified in the central nervous system.
- H3R expression has also been observed in peripheral cells, including lung mast cells.
Purpose of the Study:
- To explore the potential therapeutic applications of H3 receptor modulation in allergic diseases.
- To investigate the role of the H3 receptor in cells relevant to allergic responses.
Main Methods:
- Identification of the third histamine receptor in brain neurons and lung mast cells.
- Evaluation of the H3 receptor agonist (R)-alpha-methylhistamine for its potency.
Main Results:
- The H3 receptor is present not only in brain neurons but also in lung mast cells.
- (R)-alpha-methylhistamine is a novel and potent agonist of the H3 receptor.
Conclusions:
- The presence of H3 receptors in lung mast cells suggests a role in allergic reactions.
- The potent H3 receptor agonist (R)-alpha-methylhistamine may hold therapeutic potential for managing allergic diseases.