radequinil

AC-3933 (radequinil) is a novel small molecule that acts as a potent and selective partial inverse agonist at the benzodiazepine receptor (BzR), a modulatory site on the GABA-A receptor complex. It was developed as a drug candidate for cognitive disorders such as Alzheimer's disease. Preclinical studies demonstrated that AC-3933 enhances acetylcholine release in the hippocampus and improves memory performance in animal models of amnesia and age-related cognitive decline. Its procognitive effects are distinct from those of acetylcholinesterase inhibitors and other BzR ligands; some effects are not antagonized by flumazenil, suggesting additional mechanisms beyond classic BzR inverse agonism. Despite promising preclinical results, clinical development was discontinued after failure to demonstrate efficacy in human trials[1][3][4][5].

Other names

5-(3-methoxyphenyl)-3-(5-methyl-1,2,4-oxadiazol-3-yl)-1,6-naphthyridin-2(1H)-one