Function of brain α 2B -adrenergic receptor characterized with subtype-selective α 2B antagonist and KO mice.

•A novel selective α2B antagonist was identified through high-throughput screen (AGN-209419).•Used radiolabeled AGN-209419 in localization and inhibition assays to demonstrate the role of α2B receptors in CNS function.•Utilized behavioral analyses in α-receptor KO mice to demonstrate role of α2B receptors in CNS function.•Results indicate the α2B receptor may be therapeutically relevant for disorders such as schizophrenia, ADHD, and OCD.