GABAA receptor agent 2 TFA 

GABAA receptor agent 2 TFA is a potent and high-affinity GABA_A receptor antagonist with an IC₅₀ of 24 nM (human α1β2γ2 GABA_A-expressing tsA201 cells) and a K_i of 28 nM (rat GABA_A receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3)^[1].

IC50: 24 nM (Human α1β2γ2 GABA_A-expressing tsA201 cells)^[1]
Ki: 28 nM (Rat GABA_A receptors)^[1]

With the protonated piperidine nitrogen consistently placed to interact with β2 E155, only a simultaneous interaction with α1 R66 provided enough space above and below the ligand heteroaromatic ring to be compatible with the high affinity (0.022 μM) of the disubstituted GABAA receptor agent 2 (compound 19)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

433.42

C₂₂H₂₂F₃N₃O₃

1781880-44-1

ON1N=CC(C2CCNCC2)=C1C3=CC(C4=CC=CC=C4)=CC=C3.OC(C(F)(F)F)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Henriette A Møller, et al. Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships. J Med Chem. 2010 Apr 22;53(8):3417-21.  [Content Brief]

  [2]. Tommy Sander, et al. New insights into the GABA(A) receptor structure and orthosteric ligand binding: receptor modeling guided by experimental data. Proteins. 2011 May;79(5):1458-77.  [Content Brief]