Unexpected sensitivity of the human alpha7 neuronal nicotinic acetylcholine receptor to aminoglycosides
| Autor: | Sonia Bertrand, Jean-Charles Hoda, Ryoko Krause, Daniel Bertrand |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
medicine.medical_specialty
Patch-Clamp Techniques Microinjections alpha7 Nicotinic Acetylcholine Receptor medicine.drug_class Antibiotics Pharmacology Receptors Nicotinic Membrane Potentials Radioligand Assay Internal medicine Iodine Isotopes medicine Homomeric Animals Humans Drug Interactions Acetylcholine receptor Dose-Response Relationship Drug Chemistry General Neuroscience Aminoglycoside Neomycin Hydrogen-Ion Concentration Bungarotoxins Acetylcholine Electric Stimulation Blockade Anti-Bacterial Agents Nicotinic acetylcholine receptor Nicotinic agonist Endocrinology Aminoglycosides nervous system Oocytes medicine.drug |
| Zdroj: | Neuroreport. 17(1) |
| ISSN: | 0959-4965 |
| Popis: | The wide use of antibiotics and the development of resistance is a major health concern and, despite their relatively severe side effects, aminoglycoside antibiotics are still used in clinics. Effects of seven aminoglycosides were investigated at the human homomeric alpha7 and heteromeric alpha4beta2 neuronal nicotinic acetylcholine receptors. All aminoglycosides tested inhibited the acetylcholine-evoked responses with more pronounced effects at alpha7 than at alpha4beta2. Neomycin displayed higher blockade with a half inhibition in the nanomolar range at low calcium concentration and in the micromolar range in physiological calcium concentration but still exerted blockade below the concentration used in the clinic. These data suggest that some of their side effects may be attributable to their interactions with neuronal nicotinic acetylcholine receptors. |
| Databáze: | OpenAIRE |
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