Allosteric modulation of muscarinic acetylcholine receptors
| Autor: | Jan Proška, Stanislav Tuček |
|---|---|
| Rok vydání: | 1995 |
| Předmět: |
Pharmacology
0303 health sciences Chemistry Allosteric regulation Muscarinic acetylcholine receptor M3 Muscarinic acetylcholine receptor M2 Muscarinic acetylcholine receptor M1 Ligands Toxicology Receptors Muscarinic 3. Good health 03 medical and health sciences 0302 clinical medicine Allosteric Regulation Muscarinic acetylcholine receptor M5 Muscarinic acetylcholine receptor Muscarinic acetylcholine receptor M4 Biophysics Animals Humans 030217 neurology & neurosurgery 030304 developmental biology Acetylcholine receptor |
| Zdroj: | Trends in Pharmacological Sciences. 16:205-212 |
| ISSN: | 0165-6147 |
| Popis: | Five subtypes of muscarinic acetylcholine receptors have been identified in mammalian tissues, but the selectivity of ligandsthat are active at these receptors is low. It is possible, however, that selective compounds may be developed by targeting their allosteric site(s). Important new insights into the mechanism of allosteric control of muscarinic receptors have been obtained recently in investigations of the allosteric effects of neuromuscular blockers, and competition between ligands for the allosteric binding site has now been demonstrated. It is now apparent that the binding site for most allosteric ligands is close to the binding site for acetylcholine but that it is located at a more extracellular position. Stanislav Tucek and Jan Proska discuss the pharmacological implications of ligand interaction at these two sites and the therapeutic possibilities. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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