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Histamine H₄ receptor: a novel target for inflammation therapy
C Saravanan1, S K Bharti, S Jaggi
1Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi- 221005, India.
Mini Reviews in Medicinal Chemistry
|January 13, 2011
Summary
The newly discovered histamine H₄ receptor plays a key role in inflammation and allergies. Research explores its structure, function, and the development of targeted H₄ receptor antagonists for therapeutic potential.
Area of Science:
- Pharmacology
- Immunology
- Genomics
Background:
- Histamine receptors H₁, H₂, and H₃ were previously known.
- The human genome sequencing revealed the histamine H₄ receptor.
- The H₄ receptor shares homology with H₃ but has distinct pharmacological properties.
Purpose of the Study:
- To review the structure, expression, and sequence homology of the H₄ receptor.
- To discuss the structure-activity relationship (SAR) of H₄ receptor ligands.
- To focus on the anti-inflammatory effects of H₄ receptor antagonists.
Main Methods:
- Bioinformatic analysis of H₄ receptor sequence and homology.
- Review of published literature on H₄ receptor ligands and their SAR.
- Analysis of in vivo studies on H₄ receptor antagonists, including JNJ7777120.
Main Results:
- The H₄ receptor is primarily expressed in immune cells like mast cells and leukocytes.
- Selective H₄ receptor agonists and antagonists have been developed.
- H₄ receptor antagonists, such as JNJ7777120, demonstrate anti-inflammatory effects.
Conclusions:
- The H₄ receptor is a significant target for modulating inflammatory and allergic responses.
- Understanding H₄ receptor SAR is crucial for designing effective therapeutics.
- H₄ receptor antagonists show promise for treating inflammatory conditions.
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