1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. TPA-023B

TPA-023B 

Cat. No.: HY-19505
Handling Instructions

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.

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TPA-023B Chemical Structure

TPA-023B Chemical Structure

CAS No. : 425377-76-0

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Description

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 Vitro

TPA-023B also has high affinity for α5 subtype (Ki of 1.1 nM) of human recombinant GABAA receptor, but over 1500-fold lower for the α4- and α6 containing subtypes (Ki > 1000 nM). TPA-023B also has a 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)[1].
TPA-023B antagonizes the ability of chlordiazepoxide to potentiate the GABA EC20-induced current in cells expressing the α1 subtype. More specifically, 3 μM chlordiazepoxide potentiates the GABA EC20 current by 105% and this effect could be reduced to 8% in the presence of 100 nM TPA-023B[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].

Molecular Weight

391.37

Formula

C₂₁H₁₅F₂N₅O

CAS No.

425377-76-0

SMILES

N#CC1=CC=CC(F)=C1C2=CC(C3=CN=C4N3N=CC(C(C)(O)C)=N4)=CC=C2F

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Keywords:

TPA-023BGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorHigh-affinityα2α3α1MRK-409non-sedatinganxiolyticcurrentInhibitorinhibitorinhibit

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TPA-023B
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HY-19505
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