Publication Date

1-18-2024

Journal

Nature Communications

DOI

10.1038/s41467-024-44853-8

PMID

38238329

PMCID

PMC10796428

PubMedCentral® Posted Date

1-18-2024

PubMedCentral® Full Text Version

Post-print

Published Open-Access

yes

Keywords

Mice, Male, Humans, Animals, Receptors, Cholinergic, alpha7 Nicotinic Acetylcholine Receptor, Receptors, Nicotinic, Nicotinic Agonists, Acetylcholine, Seizures, Epilepsy

Abstract

Epilepsy is a prevalent disorder involving neuronal network hyperexcitability, yet existing therapeutic strategies often fail to provide optimal patient outcomes. Chemogenetic approaches, where exogenous receptors are expressed in defined brain areas and specifically activated by selective agonists, are appealing methods to constrain overactive neuronal activity. We developed BARNI (Bradanicline- and Acetylcholine-activated Receptor for Neuronal Inhibition), an engineered channel comprised of the α7 nicotinic acetylcholine receptor ligand-binding domain coupled to an α1 glycine receptor anion pore domain. Here we demonstrate that BARNI activation by the clinical stage α7 nicotinic acetylcholine receptor-selective agonist bradanicline effectively suppressed targeted neuronal activity, and controlled both acute and chronic seizures in male mice. Our results provide evidence for the use of an inhibitory acetylcholine-based engineered channel activatable by both exogenous and endogenous agonists as a potential therapeutic approach to treating epilepsy.

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