Differential binding of tetrodotoxin and its derivatives to voltage-sensitive sodium channel subtypes (Na_v 1.1 to Na_v 1.7).

ABSTRACT:

Background and purpose

The development of subtype-selective ligands to inhibit voltage-sensitive sodium channels (VSSCs) has been attempted with the aim of developing therapeutic compounds. Tetrodotoxin (TTX) is a toxin from pufferfish that strongly inhibits VSSCs. Many TTX analogues have been identified from marine and terrestrial sources, although their specificity for particular VSSC subtypes has not been investigated. Herein, we describe the binding of 11 TTX analogues to human VSSC subtypes Na_v 1.1-Na_v 1.7.

Experimental approach

Each VSSC subtype was transiently expressed in HEK293T cells. The inhibitory effects of TTX analogues on each subtype were assessed using whole-cell patch-clamp recordings.

Key results

The inhibitory effects of TTX o

SUBMITTER: Tsukamoto T 

PROVIDER: S-EPMC5647187 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature