Abstract
The three β-adrenoceptor subtypes (β1, β2, β3) represent important therapeutic targets. The use of β2- adrenoceptor agonists as bronchodilators and β1 or β1/β2 antagonists as antihypertensives is well established; research is ongoing in these areas to refine pharmacodynamic properties. It is also feasible to design molecules combining β-adrenoceptor affinity with other pharmacophores. This is facilitated by the ability to confer β- adrenoceptor antagonist activity via attachment of a phenylethanolamine moiety or to incorporate diverse structural elements in the N-alkyl substituent of a β-adrenoceptor agonist or antagonist. β3-Adrenoceptor agonists have not yet been successfully developed as drugs for any therapeutic indication; nevertheless, during the past few years many highly potent and selective β3-agonists have been reported, some with good oral bioavailability. Selective β3-adrenoceptor antagonists have also been identified; useful pharmacological tools are now available for the evaluation of the functional role of each β-adrenoceptor subtype.
Keywords: Phenylethanolamine, phenoxypropanolamine, D2 receptor, phosphodiesterase, calcium channel
Current Topics in Medicinal Chemistry
Title: Recent Advances in Identification and Characterization of β-Adrenoceptor Agonists and Antagonists
Volume: 7 Issue: 2
Author(s): J. Paul Hieble
Affiliation:
Keywords: Phenylethanolamine, phenoxypropanolamine, D2 receptor, phosphodiesterase, calcium channel
Abstract: The three β-adrenoceptor subtypes (β1, β2, β3) represent important therapeutic targets. The use of β2- adrenoceptor agonists as bronchodilators and β1 or β1/β2 antagonists as antihypertensives is well established; research is ongoing in these areas to refine pharmacodynamic properties. It is also feasible to design molecules combining β-adrenoceptor affinity with other pharmacophores. This is facilitated by the ability to confer β- adrenoceptor antagonist activity via attachment of a phenylethanolamine moiety or to incorporate diverse structural elements in the N-alkyl substituent of a β-adrenoceptor agonist or antagonist. β3-Adrenoceptor agonists have not yet been successfully developed as drugs for any therapeutic indication; nevertheless, during the past few years many highly potent and selective β3-agonists have been reported, some with good oral bioavailability. Selective β3-adrenoceptor antagonists have also been identified; useful pharmacological tools are now available for the evaluation of the functional role of each β-adrenoceptor subtype.
Export Options
About this article
Cite this article as:
Hieble J. Paul, Recent Advances in Identification and Characterization of β-Adrenoceptor Agonists and Antagonists, Current Topics in Medicinal Chemistry 2007; 7 (2) . https://dx.doi.org/10.2174/156802607779318208
DOI https://dx.doi.org/10.2174/156802607779318208 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
-
Beta-blockers in the Perioperative Period: Are there Indications other than Prevention of Cardiac Ischemia?
Current Drug Targets Vitamin D, Sunlight and Cancer Connection
Anti-Cancer Agents in Medicinal Chemistry Functional Foods: Salient Features and Clinical Applications
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Development of Vesicular Acetylcholine Transporter Ligands: Molecular Probes for Alzheimers Disease
Current Bioactive Compounds Risk Scores and Prediction Models in Chronic Heart Failure: A Comprehensive Review
Current Pharmaceutical Design Complex Inheritance for Susceptibility to Sudden Cardiac Death
Current Pharmaceutical Design Iron Chelating Strategies in Systemic Metal Overload, Neurodegeneration and Cancer
Current Medicinal Chemistry Obesity: The Metabolic Disease, Advances on Drug Discovery and Natural Product Research
Current Topics in Medicinal Chemistry Cell Therapy for the Treatment of Chronic Ischemic Heart Disease
Current Pharmaceutical Design Inducers of Heme Oxygenase-1
Current Pharmaceutical Design Molecular Basis of Adrenomedullin 1 Receptor Function and Its Roles in the Cardiovascular System
Current Hypertension Reviews Percutaneous Valve Interventions
Current Cardiology Reviews EGF Receptor as a Drug Target in Arterial Hypertension
Mini-Reviews in Medicinal Chemistry The Role of COX-2 in Heart Pathology
Cardiovascular & Hematological Agents in Medicinal Chemistry Clinical Proteomics in Application to Predictive Diagnostics and Personalized Treatment of Diabetic Patients
Current Proteomics Treatment of Takotsubo Cardiomyopathy
Current Pharmaceutical Design Radiobromine-Labelled Tracers for Positron Emission Tomography: Possibilities and Pitfalls
Current Radiopharmaceuticals Platelet Function in Inflammatory Diseases: Insights from Clinical Studies
Inflammation & Allergy - Drug Targets (Discontinued) Surgical or Interventional Revascularization in Diabetic Patients with Coronary Artery Disease?
Current Diabetes Reviews Editorial: (New Drug (LCZ696) for the Treatment of Heart Failure with Reduced Ejection Fraction After 10 Years. Can One Study Change the Guidelines?)
Current Vascular Pharmacology