GABAA receptor agent 4

Names

[ CAS No. ]:
2035203-91-7

[ Name ]:
GABAA receptor agent 4

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

Ki: 0.18 µM (γ-GABAAR)[1]


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C17H24N2O

[ Molecular Weight ]:
272.39

Related Compounds