tpa-023

TPA-023 (MK-0777) is a nonbenzodiazepine anxiolytic drug with a novel chemical structure. It acts as a mixed, subtype-selective ligand at the benzodiazepine site of GABA~A~ receptors containing α1, α2, α3, and α5 subunits. Specifically, it is a partial agonist at the benzodiazepine sites of the α2 and α3-containing subtypes and acts as a silent antagonist at the α1 and α5-containing subtypes. This profile results in primarily anxiolytic and anticonvulsant effects without sedation or significant cognitive impairment in animal models and human trials[1][3][9]. In clinical studies on healthy volunteers, TPA-023 was comparable to lorazepam for anxiety but lacked negative effects on cognition or coordination seen with traditional benzodiazepines. The drug was investigated for schizophrenia and generalized anxiety disorder but development was discontinued due to preclinical toxicity (cataract formation) observed in long-term dosing studies[1][9].

Other names

TPA023TPA-023TPA 023