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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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