GABAA receptor agent 2 (TFA)

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

Product Specifications

CAS Number

[1781880-44-1]

UNSPSC

12352005

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gabaa-receptor-agent-2-tfa.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C22H22F3N3O3

Molecular Weight

433.42

References & Citations

[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.|[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.