Abstract
The H3 histamine receptor is expressed in many brain regions, including those involved in sleep/wake regulation and cognitive functions. Inhibition of the H3 receptor leads to increased release of multiple neurotransmitters in these regions, making this receptor an ideal target for the potential enhancement of arousal and/or cognitive processes. The high interest level by several pharmaceutical companies in H3 receptors as potential drug targets has produced rapid advancement in novel compound series with different properties, providing a variety of preclinical tools as well as advancing several candidates into clinical trials. Multiple chemotypes have demonstrated efficacy in preclinical models covering a range of cognitive deficits, suggesting the potential value of H3 antagonists as cognition enhancers in a variety of disease states. These studies have revealed the actions of this class of compounds at the cellular, neuronal systems and behavioral levels. Recently, compounds with improved selectivity, pharmacokinetics and preclinical safety profiles have advanced into clinical trials for a number of potential indications. The results of these clinical trials are eagerly awaited and will increase our understanding of the properties of H3 receptor antagonists that will provide therapeutic value.
Current Topics in Medicinal Chemistry
Title: Histamine H3 Antagonists for Treatment of Cognitive Deficits in CNS Diseases
Volume: 10 Issue: 2
Author(s): Rita Raddatz, Ming Tao and Robert L. Hudkins
Affiliation:
Abstract: The H3 histamine receptor is expressed in many brain regions, including those involved in sleep/wake regulation and cognitive functions. Inhibition of the H3 receptor leads to increased release of multiple neurotransmitters in these regions, making this receptor an ideal target for the potential enhancement of arousal and/or cognitive processes. The high interest level by several pharmaceutical companies in H3 receptors as potential drug targets has produced rapid advancement in novel compound series with different properties, providing a variety of preclinical tools as well as advancing several candidates into clinical trials. Multiple chemotypes have demonstrated efficacy in preclinical models covering a range of cognitive deficits, suggesting the potential value of H3 antagonists as cognition enhancers in a variety of disease states. These studies have revealed the actions of this class of compounds at the cellular, neuronal systems and behavioral levels. Recently, compounds with improved selectivity, pharmacokinetics and preclinical safety profiles have advanced into clinical trials for a number of potential indications. The results of these clinical trials are eagerly awaited and will increase our understanding of the properties of H3 receptor antagonists that will provide therapeutic value.
Export Options
About this article
Cite this article as:
Raddatz Rita, Tao Ming and Hudkins L. Robert, Histamine H3 Antagonists for Treatment of Cognitive Deficits in CNS Diseases, Current Topics in Medicinal Chemistry 2010; 10 (2) . https://dx.doi.org/10.2174/156802610790411027
DOI https://dx.doi.org/10.2174/156802610790411027 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- 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
- Announcements
Related Articles
-
Neurotransmitters and Chemokines Regulate Tumor Cell Migration: Potential for a New Pharmacological Approach to Inhibit Invasion and Metastasis Development
Current Pharmaceutical Design Drug-Loaded Nanocarriers in Tumor Targeted Drug Delivery
Current Biotechnology Psychopharmacological Treatment of Obsessive-Compulsive Disorder (OCD)
Current Neuropharmacology The Benefit of Prescribing Vitamin D as Add on Therapy on the Electrocardiographic Changes in Epileptic Patients
Current Clinical Pharmacology Genetic and Molecular Factors in Drug-Induced Liver Injury: A Review
Current Drug Safety Design, Synthesis and Anticonvulsant Activity Evaluation of 7-Substituted –[1,2,4]-Triazolo[4,3-f]Pyrimidine Derivatives
Medicinal Chemistry CCL2-CCR2 Signaling in Disease Pathogenesis
Endocrine, Metabolic & Immune Disorders - Drug Targets Sustained Delivery of Interferons by Micro- and Nanosystems
Recent Patents on Materials Science Chronic Stress Impacts on Olfactory System
CNS & Neurological Disorders - Drug Targets An Emerging Strategy for Cancer Treatment Targeting Aberrant Glycogen Synthase Kinase 3β
Anti-Cancer Agents in Medicinal Chemistry Transforming Growth Factor-β Signaling in Motor Neuron Diseases
Current Molecular Medicine A Convenient, Solvent Free and High Yielding Synthesis of Bicyclo- Heterocyclic Compounds
Letters in Organic Chemistry The Impact of Antiepileptic Drugs on Vitamin Levels in Epileptic Patients
Current Pharmaceutical Biotechnology Beyond Acetylcholinesterase Inhibitors for Treating Alzheimer's Disease: α7-nAChR Agonists in Human Clinical Trials
Current Pharmaceutical Design Bone Marrow-Derived Mesenchymal Stem Cells Contribute to the Reduction of Amyloid-β Deposits and the Improvement of Synaptic Transmission in a Mouse Model of Pre-Dementia Alzheimer’s Disease
Current Alzheimer Research Apoptosis Induction by Thalidomide: Critical for Limb Teratogenicity but Therapeutic Potential in Idiopathic Pulmonary Fibrosis?
Current Molecular Pharmacology Pharmacological Treatment of Diabetic Peripheral Neuropathy: An Update
CNS & Neurological Disorders - Drug Targets Blockers of Voltage-Gated Sodium Channels for the Treatment of Central Nervous System Diseases
Recent Patents on CNS Drug Discovery (Discontinued) Potassium Channels and CNS Diseases
CNS & Neurological Disorders - Drug Targets 2D Pharmacophoric Design and Synthesis of Novel Pyrimidine Derivatives as Anticonvulsants
Current Bioactive Compounds