PHP 501 trifluoroacetate

Names

[ Name ]:
PHP 501 trifluoroacetate

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

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

[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₂F₃N₃O₃

[ Molecular Weight ]:
433.42

PHP 501 trifluoroacetate

Names

Biological Activity

Chemical & Physical Properties

Related Compounds