Abstract
Background: The design, medicinal chemistry, pharmacokinetics and development of the highly selective α2-adrenoceptor antagonist fluparoxan are reviewed.
Method: The drug's activity and selectivity in vitro, its efficacy in animals and its excellent oral pharmacokinetics and central α2-adrenoceptor antagonist activity in man, are evaluated as well as its ability to increase extracellular levels of noradrenaline, dopamine and acetylcholine in vivo. Conclusion: Furthermore, its potential for the treatment of central neurodegenerative diseases is highlighted, in particular its improvement of cognitive dysfunction in schizophrenia and in models of Alzheimer's diseaseKeywords: Alzheimer's, depression, fluparoxan, schizophrenia, α2-adrenoceptor antagonist.
Mini-Reviews in Medicinal Chemistry
Title:Fluparoxan: A Comprehensive Review of its Discovery, Adrenergic and CNS Activity and Treatment of Cognitive Dysfunction in Central Neurodegenerative Diseases
Volume: 17 Issue: 7
Author(s): Alan D. Borthwick*
Affiliation:
- DrugMolDesign, 15 Temple Grove, London NW11 7UA,United Kingdom
Keywords: Alzheimer's, depression, fluparoxan, schizophrenia, α2-adrenoceptor antagonist.
Abstract: Background: The design, medicinal chemistry, pharmacokinetics and development of the highly selective α2-adrenoceptor antagonist fluparoxan are reviewed.
Method: The drug's activity and selectivity in vitro, its efficacy in animals and its excellent oral pharmacokinetics and central α2-adrenoceptor antagonist activity in man, are evaluated as well as its ability to increase extracellular levels of noradrenaline, dopamine and acetylcholine in vivo. Conclusion: Furthermore, its potential for the treatment of central neurodegenerative diseases is highlighted, in particular its improvement of cognitive dysfunction in schizophrenia and in models of Alzheimer's diseaseExport Options
About this article
Cite this article as:
Borthwick D. Alan*, Fluparoxan: A Comprehensive Review of its Discovery, Adrenergic and CNS Activity and Treatment of Cognitive Dysfunction in Central Neurodegenerative Diseases, Mini-Reviews in Medicinal Chemistry 2017; 17 (7) . https://dx.doi.org/10.2174/1389557516666160321115041
DOI https://dx.doi.org/10.2174/1389557516666160321115041 |
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
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
Related Articles
-
Prevention and Management of Ovarian Hyperstimulation Syndrome
Current Women`s Health Reviews Comparison of Intra and Post-operative Sedation Efficacy of Dexmedetomidinemidazolam and Dexmedetomidine-propofol for Major Abdominal Surgery
Current Drug Metabolism Significance of 1,3,4-Oxadiazole Containing Compounds in New Drug Development
Current Drug Research Reviews Different Concepts of Drug Delivery in Disease Entities
Mini-Reviews in Medicinal Chemistry Emerging Synergisms Between Drugs and Physiologically-Patterned Weak Magnetic Fields: Implications for Neuropharmacology and the Human Population in the Twenty-First Century
Current Neuropharmacology Application of Dual-Source CT Coronary Angiography in Type 2 Diabetic Patients with Symptomatic Coronary Heart Disease
Current Vascular Pharmacology Renal Endothelial Dysfunction in Acute Kidney Ischemia Reperfusion Injury
Cardiovascular & Hematological Disorders-Drug Targets Current Treatment Concepts of Philadelphia-Negative MPN
Current Cancer Drug Targets Novel Targets for Cardiac Antiarrhythmic Drug Development
Current Pharmaceutical Design Applications of Barton-McCombie Reaction in Total Syntheses
Current Organic Synthesis Neurological Aspects of Medical Use of Cannabidiol
CNS & Neurological Disorders - Drug Targets Polymorphism in Endothelin-1 Gene: An Overview
Current Clinical Pharmacology Targeting Soluble Epoxide Hydrolase for Inflammation and Pain - An Overview of Pharmacology and the Inhibitors
Inflammation & Allergy - Drug Targets (Discontinued) β-Carboline Alkaloids: Biochemical and Pharmacological Functions
Current Medicinal Chemistry Inhalation Gases or Gaseous Mediators As Neuroprotectants for Cerebral Ischaemia
Current Drug Targets Measurement of Hemodynamic Parameters and Antidepressant Activity in Hypertensive Rats Following Two Weeks Consumption of <i>Acacia Tortilis</i> Leaves Extract
The Natural Products Journal TNF alpha Inhibition as Treatment Modality for Certain Rheumatologic and Gastrointestinal Diseases
Endocrine, Metabolic & Immune Disorders - Drug Targets Hypertension in Children with Autosomal Dominant Polycystic Kidney Disease (ADPKD)
Current Hypertension Reviews The Role of Nitric Oxide on Endothelial Function
Current Vascular Pharmacology In-hospital Falls in Older Patients: The Risk Factors and The Role of Hyponatraemia
Current Aging Science