| Identification | Back Directory | [Name]
TPA-023B | [CAS]
425377-76-0 | [Synonyms]
TPA-023B
BAY-2873384
TPA 023B,TPA023B
[1,1'-Biphenyl]-2-carbonitrile, 2',6-difluoro-5'-[3-(1-hydroxy-1-methylethyl)imidazo[1,2-b][1,2,4]triazin-7-yl]- | [Molecular Formula]
C21H15F2N5O | [MDL Number]
MFCD30532602 | [MOL File]
425377-76-0.mol | [Molecular Weight]
391.37 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
TPA-023B gives dose- and time-dependent occupancy of rat brain GABAA receptors as measured using an in vivo [3H]flumazenil binding assay, with 50% occupancy corresponding to a respective dose and plasma drug concentration of 0.09 mg/kg and 19 ng/mL[1].
TPA-023B is anxiolytic in rodent and primate (squirrel monkey) models of anxiety (elevated plus maze, fear-potentiated startle, conditioned suppression of drinking, conditioned emotional response) yet has no significant effects in rodent or primate assays of ataxia and/or myorelaxation (rotarod, chain-pulling, lever pressing), up to doses (10 mg/kg) corresponding to occupancy of greater than 99%[1]. | [storage]
Store at -20°C | [References]
[1] Atack JR, et al. Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist. J Psychopharmacol. 2011 Mar;25(3):329-44. DOI:10.1177/0269881109354928 |
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