High-affinity and selectivity of neosurugatoxin for the inhibition of22Na influx via nicotinic receptor-ion channel in cultured bovine adrenal medullary cells: Comparative study with histrionicotoxin
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説明
In cultured bovine adrenal medullary cells, neosurugatoxin and histrionicotoxin inhibited carbachol-induced influx of 22Na, 45Ca and secretion of catecholamines with IC50 of 27 nM and 3 microM, respectively. The inhibitory effects of neosurugatoxin were reversed by the increased concentrations of carbachol, whereas those of histrionicotoxin were not. Histrionicotoxin at concentrations higher than 10 microM also reduced veratridine-induced influx of 22Na, 45Ca and secretion of catecholamines, while neosurugatoxin had no effects. High K-induced 45Ca influx and catecholamine secretion were not altered by either neosurugatoxin or histrionicotoxin. The present findings suggest (1) neosurugatoxin competitively inhibits nicotinic receptor-ion channel complex at nanomolar concentrations, but has no effects on voltage-dependent Na channel and voltage-dependent Ca channel; (2) histrionicotoxin at micromolar concentrations non-competitively suppresses nicotinic receptor-ion channel complex. Higher concentrations of histrionicotoxin also interferes with voltage-dependent Na channel, but has no effect on voltage-dependent Ca channel; (3) neosurugatoxin, due to its high-affinity and selectivity, may be a useful probe for studying nicotinic receptors in nervous tissues.
収録刊行物
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- Neuroscience
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Neuroscience 33 333-339, 1989-01-01
Elsevier BV
