GiGA1

GiGA1 (G protein-independent GIRK Activator 1) is a selective, small-molecule agonist of G protein-gated inwardly rectifying potassium (GIRK) channels, specifically targeting GIRK1/GIRK2 heterotetramers. Discovered through a structure-based virtual screening of the alcohol-binding pocket in GIRK channels, GiGA1 acts in a G-protein-independent manner to activate GIRK1-containing channels with rapid activation and deactivation kinetics. By enhancing potassium conductance, GiGA1 hyperpolarizes neurons and reduces excitability in the brain. It has demonstrated preclinical efficacy as an anticonvulsant in animal models of acute chemoconvulsant-induced seizures and tumor-associated epilepsy (TAE), and is also being investigated for its potential to reduce alcohol-mediated behaviors in models of alcohol use disorder (AUD).

Other names

1-(thiophen-2-yl)-3-(o-tolyl)ureaG protein-independent GIRK activator 1G-protein-independent GIRK activator 1