[11C] Ro15-4513

[11C] Ro15-4513 is a carbon-11 radiolabeled version of Ro15-4513, a high-affinity ligand for benzodiazepine sites on GABAA receptors, developed for use as a PET imaging radiotracer. Ro15-4513 acts primarily as a partial inverse agonist at diazepam-sensitive benzodiazepine binding sites (notably α1, α2, α3, α5 subunits) and as a partial agonist at diazepam-insensitive subtypes (notably α4, α6 with β and γ2 or δ subunits)[1][2][3][5][6][7]. The compound is notable for its relatively high affinity for the α5 subunit-containing GABAA receptor, enabling its use for in vivo imaging of these receptor populations in brain[3][5][7]. Ro15-4513 has been described as an "alcohol antagonist" due to its ability to competitively antagonize ethanol at overlapping sites, and it displays proconvulsant and anxiogenic effects[1][2][6]. For PET studies, the carbon-11 isotope is used; this formulation is not intended as a therapeutic drug but as an investigational imaging agent for neuroscience and psychiatric research.

Brand names

[11C] Ro15-4513

Other names

ethyl 8-azido-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl esterethanol antagonist