Abstract
The histamine H3 receptor is a pre-synaptic auto- and hetero-receptor that controls the release of histamine and a variety of other neurotransmitters in the brain. As such, modulation of the histamine H3 receptor is expected to affect wake via control of the release of histamine and to affect cognition via regulation of several other neurotransmitters including acetylcholine and norepinephrine. Over the last several years numerous pre-clinical studies have shown that histamine H3 antagonists promote wakefulness, improve cognition, and in some cases affect food intake. Based on the interest level generated from these early pharmacology studies, and following the cloning and expression of the human histamine H3 receptor, many pharmaceutical companies began drug discovery programs aimed at the identification of histamine H3 antagonists suitable for human clinical trials. These efforts have led to many new chemotypes, and several promising compounds have recently entered the clinic for a variety of conditions, including ADHD, Narcolepsy, EDS associated with Narcolepsy, Cognitive disorders and Schizophrenia. Recent efforts towards the identification and pharmacological characterization of novel histamine H3 antagonists will be discussed.
Keywords: Histamine, histamine H3, wake, cognition, histamine h3 antagonists/inverse agonists
Current Topics in Medicinal Chemistry
Title: Histamine H3 Antagonists as Wake-Promoting and Pro-Cognitive Agents
Volume: 8 Issue: 11
Author(s): Emily M. Stocking and Michael A. Letavic
Affiliation:
Keywords: Histamine, histamine H3, wake, cognition, histamine h3 antagonists/inverse agonists
Abstract: The histamine H3 receptor is a pre-synaptic auto- and hetero-receptor that controls the release of histamine and a variety of other neurotransmitters in the brain. As such, modulation of the histamine H3 receptor is expected to affect wake via control of the release of histamine and to affect cognition via regulation of several other neurotransmitters including acetylcholine and norepinephrine. Over the last several years numerous pre-clinical studies have shown that histamine H3 antagonists promote wakefulness, improve cognition, and in some cases affect food intake. Based on the interest level generated from these early pharmacology studies, and following the cloning and expression of the human histamine H3 receptor, many pharmaceutical companies began drug discovery programs aimed at the identification of histamine H3 antagonists suitable for human clinical trials. These efforts have led to many new chemotypes, and several promising compounds have recently entered the clinic for a variety of conditions, including ADHD, Narcolepsy, EDS associated with Narcolepsy, Cognitive disorders and Schizophrenia. Recent efforts towards the identification and pharmacological characterization of novel histamine H3 antagonists will be discussed.
Export Options
About this article
Cite this article as:
Stocking M. Emily and Letavic A. Michael, Histamine H3 Antagonists as Wake-Promoting and Pro-Cognitive Agents, Current Topics in Medicinal Chemistry 2008; 8 (11) . https://dx.doi.org/10.2174/156802608784936728
DOI https://dx.doi.org/10.2174/156802608784936728 |
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
-
Current Theories and Clinical Trial Evidence for Limiting Human Abdominal Aortic Aneurysm Growth
Current Drug Targets Homocysteine Serum Levels as Prognostic Marker of Hepatocellular Carcinoma with Portal Vein Thrombosis
Current Molecular Medicine Resveratrol Improves Cardiovascular Function in DOCA-Salt Hypertensive Rats
Current Pharmaceutical Biotechnology Identification and Treatment of Patients with Early COPD
Current Respiratory Medicine Reviews Pancreastatin, A Regulatory Peptide that Modulates Energy Metabolism
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Primary and Secondary Hypertriglyceridaemia
Current Drug Targets Sesame Seed Lignans: Potent Physiological Modulators and Possible Ingredients in Functional Foods & Nutraceuticals
Recent Patents on Food, Nutrition & Agriculture Protrhombotic Effects of Contraceptives
Current Pharmaceutical Design Editorial [Hot topic: Phosphodiesterase-5 Inhibitors and their Use in the Treatment of Urological Conditions (Executive Editor: Perimenis Petros)]
Current Pharmaceutical Design Managing Comorbidity in COPD: A Difficult Task
Current Drug Targets Development of Functional Dark Chocolate by Incorporating Flaxseed (Linum usitatissimum) Oil and Honey with Improved Organoleptic and Textural Attributes
Current Nutrition & Food Science Development and Validation of a Simple LC-UV Method to Assay Doxazosin in Polymeric Nanocapsules and Tablets
Current Pharmaceutical Analysis The Cellular Effects of Carbon Monoxide in the Airway
Current Molecular Medicine Role of Infrared Spectroscopy in Medicinal Plants Research in Pakistan
Current Bioactive Compounds Cardiovascular and Renovascular Implications of COX-2 Inhibition
Current Pharmaceutical Design Targeted Therapies in Solid Tumours: Pinpointing the Tumours Achilles Heel
Current Pharmaceutical Design Radial Approach for Percutaneous Coronary Intervention
Reviews on Recent Clinical Trials Zinc Complexes Developed as Metallopharmaceutics for Treating Diabetes Mellitus based on the Bio-Medicinal Inorganic Chemistry
Current Topics in Medicinal Chemistry The Roles of Vitamin D and Its Analogs in Inflammatory Diseases
Current Topics in Medicinal Chemistry Matrix Metalloproteinases as Valid Clinical Target
Current Pharmaceutical Design