Comparative analysis of isoxazoline activity on human and canine GABA receptors expressed in Xenopus oocytes.

ABSTRACT:

Background

Isoxazolines, including sarolaner, lotilaner, afoxolaner and fluralaner, are a class of ectoparasiticides that target gamma-aminobutyric acid receptors (GABARs) in insects and acari. However, their potential action on mammalian GABARs has not been extensively compared.

Methods

This study investigated the inhibitory effects of these isoxazolines on human and canine GABARs expressed in Xenopus oocytes. Eleven functional GABAR subunit combinations from human and canine isoforms were successfully cloned and expressed. Two-electrode voltage-clamp measurements were performed to determine the inhibitory effects of the isoxazolines.

Results

Sarolaner, afoxolaner and fluralaner exhibited partial to high inhibition of human and canine GABARs, with fluralaner showing

SUBMITTER: Sager H 

PROVIDER: S-EPMC12144822 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature