Abstract
Histamine, a low molecular weight amine has been extensively studied for its various pharmacological profiles. Until recently histamine was thought to act on three receptors - H1, H2 and H3. Merely a decade back, sequencing of human genome has revealed a new histamine receptor - H4 receptor. This 390 amino acid sequenced receptor has around 38% homology with histamine H3 receptor besides; the pharmacological profile of the protein is quite different from other histamine receptors. H4 receptor is mainly expressed in mast cells and leukocytes and involves various physiological functions related to inflammation and allergy. Potent selective H4 receptor agonists and antagonists have been synthesized and in vivo studies have indicated their action on H4 receptor. In this review, structure, expression, homology sequence of H4 receptor among the different species have been documented. Further, structure activity relationship (SAR) of H4 and ligands on the basis of their nucleus has been discussed in depth. In addition, anti-inflammatory effects of H4 receptor antagonists, with special emphasis to JNJ7777120, a selective H4 receptor antagonist have been focused exhaustively.
Keywords: Agonist, antagonist, G protein-coupled receptor (GPCR), JNJ7777120, histamine H4 receptor, inflammation, Structure activity relationship (SAR), peptic ulcers, gastroesophageal reflux disease, sleep-wake disorder, epilepsy, obesity, depression, dementia, schizophrenia, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), neuropathic pain, Antihistamines
Mini-Reviews in Medicinal Chemistry
Title: Histamine H4 Receptor: A Novel Target for Inflammation Therapy
Volume: 11 Issue: 2
Author(s): C. Saravanan, S. K. Bharti, S. Jaggi and S. K. Singh
Affiliation:
Keywords: Agonist, antagonist, G protein-coupled receptor (GPCR), JNJ7777120, histamine H4 receptor, inflammation, Structure activity relationship (SAR), peptic ulcers, gastroesophageal reflux disease, sleep-wake disorder, epilepsy, obesity, depression, dementia, schizophrenia, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), neuropathic pain, Antihistamines
Abstract: Histamine, a low molecular weight amine has been extensively studied for its various pharmacological profiles. Until recently histamine was thought to act on three receptors - H1, H2 and H3. Merely a decade back, sequencing of human genome has revealed a new histamine receptor - H4 receptor. This 390 amino acid sequenced receptor has around 38% homology with histamine H3 receptor besides; the pharmacological profile of the protein is quite different from other histamine receptors. H4 receptor is mainly expressed in mast cells and leukocytes and involves various physiological functions related to inflammation and allergy. Potent selective H4 receptor agonists and antagonists have been synthesized and in vivo studies have indicated their action on H4 receptor. In this review, structure, expression, homology sequence of H4 receptor among the different species have been documented. Further, structure activity relationship (SAR) of H4 and ligands on the basis of their nucleus has been discussed in depth. In addition, anti-inflammatory effects of H4 receptor antagonists, with special emphasis to JNJ7777120, a selective H4 receptor antagonist have been focused exhaustively.
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Cite this article as:
Saravanan C., K. Bharti S., Jaggi S. and K. Singh S., Histamine H4 Receptor: A Novel Target for Inflammation Therapy, Mini-Reviews in Medicinal Chemistry 2011; 11 (2) . https://dx.doi.org/10.2174/138955711794519519
DOI https://dx.doi.org/10.2174/138955711794519519 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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