GABAA receptor agent 6

Names

[ CAS No. ]:
1808463-81-1

[ Name ]:
GABAA receptor agent 6

Biological Activity

[Description]:

GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an Ki of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability[1].

[Related Catalog]:

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

[Target]

Ki: 0.56 µM (γ-GABAAR)[1]


[In Vitro]

GABAA receptor agent 6 (compound 2027) shows antagonist activity with IC50s of 6.68, 1.03, 0.36, 4.13, 4.96, 2.96, 0.29, 0.59 µM for α1β2δ, α4β1δ, α4β2δ, α6β2δ, α1β2γ2, α2β2γ2, α3β2γ2, α5β2γ2 subtypes, respectively[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 ]:
C18H25N3O2

[ Molecular Weight ]:
315.41

Related Compounds