Antillatoxin is a sodium channel activator that displays unique efficacy in heterologously expressed rNav1.2, rNav1.4 and rNav1.5 α subunits.

ABSTRACT:

Background

Antillatoxin (ATX) is a structurally unique lipopeptide produced by the marine cyanobacterium Lyngbya majuscula. ATX activates voltage-gated sodium channel α-subunits at an undefined recognition site and stimulates sodium influx in neurons. However, the pharmacological properties and selectivity of ATX on the sodium channel α-subunits were not fully characterized.

Results

In this study, we characterized the pharmacological properties and selectivity of ATX in cells heterologously expressing rNa(v)1.2, rNa(v)1.4 or rNa(v)1.5 α-subunits by using the Na(+) selective fluorescent dye, sodium-binding benzofuran isophthalate. ATX produced sodium influx in cells expressing each sodium channel α-subunit, whereas two other sodium channel activators, veratridine and brevetox

SUBMITTER: Cao Z 

PROVIDER: S-EPMC3009643 | biostudies-literature | 2010 Dec

REPOSITORIES: biostudies-literature