TPA 023

SKU: orb1307656

Description

TPA 023 is a potent and selective agonist for GABAA receptors containing α2 and/or α3 subunits, exhibiting binding affinities in the sub-nanomolar range (Ki = 0.19 - 0.41 nM). This compound is a valuable research tool for investigating the roles of specific GABAA receptor subtypes in anxiety, sedation, and cognitive functions in both in vitro and in vivo studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 252977-51-8
• MW: 395.43
• Purity: 99.75%
• Formula: C₂₀H₂₂FN₇O
• SMILES: CCn1ncnc1COc1nn2c(nnc2cc1C(C)(C)C)-c1ccccc1F
• Target: GABA Receptor
• Solubility: DMSO:50 mg/mL (126.44 mM)

Bioactivity

• Target IC50:
  GABAA:（ki）0.19-0.41 nM
• In Vivo:
  TPA023 (0.7, 2.0, and 5 mg/kg, p.o.) blocks ketamine's cognitive-impairing ability but does not influence the behavioral symptoms of rhesus monkeys. In rats, TPA023 (0.42 mg/kg; oral) displays good receptor occupancy and results in 50% occupancy of rat brain GABAA receptors, with the corresponding plasma concentration being 25 ng/mL. TPA023 (3 mg/kg p.o. in 0.5% methylcellulose) shows anxiolytic-like effect on rats. TPA023(10 mg/kg i.p.) is efficacious in the mouse pentylenetetrazole-induced seizure model, providing full seizure protection(84% occupancy), with the ED50 of 0.19-0.41 nM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GABA Receptor, GABAA, GABAReceptor, Gamma-aminobutyric acid Receptor, Inhibitor, inhibit, TPA 023, TPA023, TPA-023, γ-Aminobutyric acid Receptor

Compound Identifiers

PubChem CID

9908684