Reserpine: interactions with batrachotoxin and brevetoxin sites on voltage-dependent sodium channels.

作者: Andrew Flowers , Kenolisa Onwueme , Cyrus R. Creveling , John W. Daly

DOI: 10.1023/A:1015301610349

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摘要: Reserpine inhibited batrachotoxin-elicited sodium influx in guinea pig brain synaptoneurosomes with an IC50 of about 1 μM. In the presence brevetoxin increased to 80 binding batrachotoxinin-A [3H]benzoate ([3H]BTX-B) a complex manner causing partial inhibition from 0.001 0.08 μM, then rebound stimulation 0.1 0.8 followed by complete The was prevented brevetoxin; reserpine smoothly at μM slightly reduced off-rate [3H]BTX-B measured veratridine, while concentration 50 it enhanced off-rate, presumably allosteric mechanism. 0.3–10 elicited [3H]brevetoxin-3. local anesthetic dibucaine had effects similar reserpine: It partially [3H]brevetoxin. potency as inhibitor 2 results suggest that binds both site cause batrachotoxin-binding and action, but also another causing, like brevetoxin, enhancement action. Local anesthetics may bind site.

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