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.
Export Options
About this article
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 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Drugs and mitochondria
Mitochondria play a central role in the life and death of cells. They are not merely the center for energy metabolism but are also the headquarters for different catabolic and anabolic processes, calcium fluxes, and various signaling pathways. Mitochondria maintain homeostasis in the cell by interacting with reactive oxygen-nitrogen species ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
![](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Anticancer Mammalian Target of Rapamycin (mTOR) Signaling Pathway Inhibitors: Current Status, Challenges and Future Prospects in Management of Epilepsy
CNS & Neurological Disorders - Drug Targets N-Methylation of Nitrogen-Containing Organic Substrates: A Comprehensive Overview
Current Organic Chemistry Understanding the Potential Role and Delivery Approaches of Nitric Oxide in Chronic Wound Healing Management
Current Pharmaceutical Design CAR, The Continuously Advancing Receptor, in Drug Metabolism and Disease
Current Drug Metabolism In Search of Novel and Therapeutically Significant Melatoninergic Ligands
Recent Patents on CNS Drug Discovery (Discontinued) Perspectives on Phytochemicals as Antibacterial Agents: An Outstanding Contribution to Modern Therapeutics
Mini-Reviews in Medicinal Chemistry Therapeutic Drugs that Slow the Heart Rate of Early Rat Embryos. Is there a Risk for the Human?
Current Pharmaceutical Design Editorial [Hot topic: Chemical Agents Positively and Negatively Affecting the Central Nervous System (Guest Editors: Abel Santamaria & Mauricio Diaz-Munoz)]
Central Nervous System Agents in Medicinal Chemistry Genetics of Serotonin Receptors and Depression: State of the Art
Current Drug Targets Adeno-Associated Virus (AAV) Vectors in the CNS
Current Gene Therapy Neurochemical Imbalance in Epilepsy from Animal Model to Human
Current Psychopharmacology The Pharmacological Significance of <i>Convolvulus Prostratus</i>: Modern Perspectives of An Ancient Herb
Current Indian Science Computational Methods Dedicated to Neurological Disorder Detection through Epistasis Analysis: A Review
Current Chinese Engineering Science Molecular Therapeutics of HBV
Current Gene Therapy Alzheimer’s Disease and Autistic Spectrum Disorder: Is there any Association?
CNS & Neurological Disorders - Drug Targets Modulation of Potassium Channels as a Therapeutic Approach
Current Pharmaceutical Design Anticonvulsant Activity of A Novel Series of 2,5-Disubstituted 1,3,4-Oxadiazoles: Semicarbazones Based Pharmacophoric Model Studies
Letters in Drug Design & Discovery Promising Polymeric Drug Carriers for Local Delivery: The Case of <i>in situ</i> Gels
Current Drug Delivery Alkaloids as Important Scaffolds in Therapeutic Drugs for the Treatments of Cancer, Tuberculosis, and Smoking Cessation
Current Topics in Medicinal Chemistry Editorial [Hot Topic: New Mechanisms of Neuronal Injury and Neuroprotection (Guest Editor: Weihai Ying)]
Current Drug Targets