Conotoxin GIIIA: selective inhibition of 22Na influx via voltage-dependent Na channels in adrenal medullary cells
| Autor: | Yasuhito Uezono, Masahide Arita, Yuchio Yanagawa, Mei Satake, Futoshi Izumi, Akihiko Wada |
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| Rok vydání: | 1990 |
| Předmět: |
medicine.medical_specialty
Biology Receptors Nicotinic complex mixtures Peptides Cyclic Sodium Channels chemistry.chemical_compound Catecholamines Internal medicine medicine Animals Conotoxin Cells Cultured Pharmacology Saxitoxin Veratridine Conus geographus Sodium Radioisotopes Sodium channel Calcium Radioisotopes Giant axon General Medicine biology.organism_classification Endocrinology medicine.anatomical_structure chemistry Adrenal Medulla Biophysics Cattle Neuron Adrenal medulla Conotoxins |
| Zdroj: | Naunyn-Schmiedeberg's archives of pharmacology. 342(3) |
| ISSN: | 0028-1298 |
| Popis: | Conotoxin GIIIA and GIIIB from the marine snail Conus geographus have been reported to inhibit voltage-dependent Na channels in skeletal muscle and postganglionic sympathetic neuron, but have no effect on Na channels in brain, giant axon and heart. In eel electroplax, conotoxins were also shown to share the common binding sites with saxitoxin (see review Gray et al. 1988). In bovine adrenal medullary cells, conotoxin GIIIA inhibited veratridine-induced influx of 22Na, 45Ca and secretion of catecholamines with an IC50 of 6 mumols/l while saxitoxin suppressed veratridine-induced responses with an IC50 of 6.3 nmol/l. [3H]Saxitoxin binding to the cells was inhibited by unlabeled saxitoxin with an IC50 of 5.1 nmol/l, but was slightly reduced by 10 mumols/l conotoxin GIIIA. Conotoxin GIIIA, at 10 mumols/l, did not alter carbachol-induced influx of 22Na, 45CA and secretion of catecholamines as well as high K-induced 45Ca influx and catecholamine secretion. These results indicate that conotoxin GIIIA, at concentrations 950 fold higher than saxitoxin, inhibits Na influx via voltage-dependent Na channels, but has no effect on the nicotinic receptor-ion channel complex or the voltage-dependent Ca channels. Conotoxin GIIIA seems to bind at the sites which are distinct from saxitoxin, but are functionally linked to the voltage-dependent Na channels. Conotoxins may be useful for the classification of Na channels in excitable cell membranes. |
| Databáze: | OpenAIRE |
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