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Exploring Adenosine Receptor Ligands: Potential Role in the Treatment of Cardiovascular Diseases
Werner J Geldenhuys1, Ahmad Hanif2, June Yun3
1Department of Pharmaceutical Sciences, West Virginia University, School of Pharmacy, Morgantown, WV 26506, USA. werner.geldenhuys@hsc.wvu.edu.
Insights
Adenosine receptors are key targets for treating cardiovascular diseases. This review explores ligands that modulate these receptors, focusing on structural impacts on drug efficacy for vascular conditions.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Cardiovascular Science
Background:
- Cardiovascular diseases are a leading cause of death globally.
- Adenosine receptors, a class of G-protein coupled receptors, are implicated in various physiological and pathological cardiovascular processes.
- These receptors are recognized as promising therapeutic targets for a range of conditions.
Purpose of the Study:
- To review identified adenosine receptor ligands.
- To evaluate their effects on the vascular system.
- To analyze structure-activity relationships for ligand potency and efficacy.
Main Methods:
- Literature review of adenosine receptor ligands.
- Analysis of clinical and medicinal chemistry data.
- Evaluation of structure-activity relationships impacting potency and efficacy.
Main Results:
- Numerous adenosine receptor ligands have been identified.
- These ligands demonstrate significant effects on vascular system physiology and pathology.
- Specific structural modifications correlate with altered ligand potency and efficacy.
Conclusions:
- Adenosine receptors are a viable therapeutic target for cardiovascular diseases.
- Medicinal chemistry approaches focusing on structural modifications can optimize ligand development.
- Further research into adenosine receptor modulation may yield novel treatments for vascular diseases and obesity.
Abstract:
Cardiovascular diseases remain the number one diseases affecting patients' morbidity and mortality. The adenosine receptors are G-protein coupled receptors which have been of interest for drugs target for the treatment of multiple diseases ranging from cardiovascular to neurological. Adenosine receptors have been connected to several biological pathways affecting the physiology and pathology of the cardiovascular system. In this review, we will cover the different adenosine receptor ligands that have been identified to interact with adenosine receptors and affect the vascular system. These ligands will be evaluated from clinical as well as medicinal chemistry perspectives with more emphasis on how structural changes in structure translate into ligand potency and efficacy. Adenosine receptors represent a novel therapeutic target for development of treatment options treating a wide variety of diseases, including vascular disease and obesity.
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