Medchemexpress LLC (R)-6-(1-hydroxy-1-methylethyl)-4-(2-fluorophenyl)-1-((E)-3-fluorostyryl)-1H-pyrazolo[3,4-c]pyridin | 425377-76-0 | 98.5% | 391.37 | 5 MG

Supplier:  Medchemexpress LLC HY195055MG

TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.

• High-affinity and orally active
• GABAA receptor α2/α3 subtype partial agonist
• GABAA receptor α1 subtype antagonist
• Non-sedating anxiolytic-like properties
• High affinity for α5 subtype (Ki of 1.1 nM) of human recombinant GABAA receptor
• Over 1500-fold lower affinity for the α4- and α6 containing subtypes (Ki > 1000 nM)
• Comparable affinity for native rat GABAA receptors in different regions of the CNS (Ki of 0.32-0.99 nM in cerebellum, spinal cord and frontal cortex)
• Anxiolytic in rodent and primate models of anxiety
• No significant effects in rodent or primate assays of ataxia and/or myorelaxation, even at high doses (10 mg/kg) with greater than 99% occupancy

Catalog No. 50-004-01834