1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. GABAA receptor agent 2 TFA

GABAA receptor agent 2 TFA 

Cat. No.: HY-135482
Handling Instructions

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).

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GABAA receptor agent 2 TFA Chemical Structure

GABAA receptor agent 2 TFA Chemical Structure

CAS No. : 1781880-44-1

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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].

IC50 & 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].

Molecular Weight

433.42

Formula

C₂₂H₂₂F₃N₃O₃

CAS No.

1781880-44-1

SMILES

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

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Storage

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

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Keywords:

GABAA receptor agent 2GABAA receptor agent2GABAA receptor agent-2GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorGABAAhigh-affinityα1β2γ2Inhibitorinhibitorinhibit

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GABAA receptor agent 2 TFA
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HY-135482
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