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Nicotinic agonists, antagonists, and modulators from natural sources.
1Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, Maryland 20892, USA. jdaly@nih.gov
Cellular and Molecular Neurobiology
|August 3, 2005
Summary
Natural products like nicotine and muscarine have been crucial for defining acetylcholine receptors. These natural compounds and their derivatives inspire the development of synthetic drugs targeting these receptors.
Area of Science:
- Pharmacology
- Neuroscience
- Natural Products Chemistry
Background:
- Acetylcholine receptors are classified as nicotinic or muscarinic, based on their response to nicotine and muscarine.
- Numerous natural products have been identified as agonists, antagonists, or modulators of acetylcholine receptor function.
Purpose of the Study:
- To review the historical and ongoing impact of natural products on acetylcholine receptor research.
- To highlight the role of natural compounds in the discovery of synthetic agents targeting acetylcholine receptors.
Main Methods:
- Literature review of natural products affecting acetylcholine receptors.
- Analysis of natural product structures and their pharmacological activities.
- Examination of synthetic agents derived from natural product leads.
Main Results:
- Natural sources have yielded diverse nicotinic agonists (e.g., cytisine, epibatidine) and antagonists (e.g., tubocurarines, strychnine).
- Positive modulators of nicotinic function, such as galanthamine and codeine, are also derived from natural sources.
- Natural products have served as critical templates for designing synthetic acetylcholine receptor ligands.
Conclusions:
- Research into acetylcholine receptors and their functions is fundamentally linked to natural product discovery.
- Natural products continue to be indispensable for developing novel therapeutic agents targeting the cholinergic system.