GABAA receptor agent 4 

GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an K_i of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential^[1].

K_i: 0.18 µM (γ-GABAAR)^[1]

GABAA receptor agent 4 (compound 1e) shows antagonist activity with IC₅₀s of 4.95, 0.195, 0.250, 1.95, 2.18, 7.56, 0.56, 0.54 µM for α1β2δ, α4β1δ, α4β2δ, α6β2δ, α1β2γ2, α2β2γ2, α3β2γ2, α5β2γ2 subtypes, respectively^[1].
GABAA receptor agent 4 (50 µM; 96 h) rescues inhibition of proliferation induced by alprazolam in both human PBMC and mouse splenocytes populations with minimal cell toxicity^[1].

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

272.39

C₁₇H₂₄N₂O

2035203-91-7

O=C(N1CCC2(CC1)CCNCC2)C3=CC=CC(C)=C3

Room temperature in continental US; may vary elsewhere.

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

• [1]. Bavo F,et al. Structure-Activity Studies of 3,9-Diazaspiro[5.5]undecane-Based γ-Aminobutyric Acid Type A Receptor Antagonists with Immunomodulatory Effect. J Med Chem. 2021 Dec 23;64(24):17795-17812.  [Content Brief]