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Screening an In-House Isoquinoline Alkaloids Library for New Blockers of Voltage-Gated Na⁺ Channels Using Voltage Sensor Fluorescent Probes: Hits and Biases.

ABSTRACT: Voltage-gated Na⁺ (Na_V) channels are significant therapeutic targets for the treatment of cardiac and neurological disorders, thus promoting the search for novel Na_V channel ligands. With the objective of discovering new blockers of Na_V channel ligands, we screened an In-House vegetal alkaloid library using fluorescence cell-based assays. We screened 62 isoquinoline alkaloids (IA) for their ability to decrease the FRET signal of voltage sensor probes (VSP), which were induced by the activation of Na_V channels with batrachotoxin (BTX) in GH3b6 cells. This led to the selection of five IA: liriodenine, oxostephanine, thalmiculine, protopine, and bebeerine, inhibiting the BTX-induced VSP signal with micromolar IC₅₀. These five a

SUBMITTER: Coquerel Q

PROVIDER: S-EPMC9268414 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature

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Dataset Information

Screening an In-House Isoquinoline Alkaloids Library for New Blockers of Voltage-Gated Na⁺ Channels Using Voltage Sensor Fluorescent Probes: Hits and Biases.

OmicsDI is part of the ELIXIR infrastructure

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Dataset Information

Screening an In-House Isoquinoline Alkaloids Library for New Blockers of Voltage-Gated Na+ Channels Using Voltage Sensor Fluorescent Probes: Hits and Biases.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Screening an In-House Isoquinoline Alkaloids Library for New Blockers of Voltage-Gated Na⁺ Channels Using Voltage Sensor Fluorescent Probes: Hits and Biases.