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Adenosine receptor ligands: differences with acute versus chronic treatment
K A Jacobson1, D K von Lubitz, J W Daly
1Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.
Trends in Pharmacological Sciences
|March 1, 1996
Summary
Selective adenosine receptor ligands show promise but have complex effects. Acute drug administration can yield opposite results compared to chronic use, a phenomenon known as
Area of Science:
- Pharmacology
- Neuroscience
- Medicinal Chemistry
Background:
- Adenosine receptors are key targets for drug development in various therapeutic areas.
- Selective agonists and antagonists for adenosine receptor subtypes have been developed over three decades.
- Caffeine and theophylline are known adenosine receptor antagonists.
Purpose of the Study:
- To discuss the phenomenon of 'effect inversion' with adenosine receptor ligands.
- To highlight the challenges in therapeutic applications of these ligands.
Main Methods:
- Review of existing research on adenosine receptor ligands.
- Analysis of studies demonstrating acute versus chronic effects of ligands.
- Discussion of observed 'effect inversion' in different physiological processes.
Main Results:
- Adenosine receptor ligands exhibit 'effect inversion', where acute and chronic administration produce opposing outcomes.
- This inversion has been observed in cognitive processes, seizure activity, and ischemic damage.
- The complexity arises from the dynamic changes in receptor function or downstream signaling.
Conclusions:
- The therapeutic utility of adenosine receptor ligands is complicated by effect inversion.
- Understanding this phenomenon is crucial for designing effective and safe treatments.
- Further research is needed to elucidate the mechanisms underlying effect inversion for optimized drug development.