GABAA receptor agent 5

Names

[ CAS No. ]:
1808389-92-5

[ Name ]:
GABAA receptor agent 5

Biological Activity

[Description]:

GABAA receptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an Ki of 0.020 µM. GABAA receptor agent 5 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

[In Vitro]

GABAA receptor agent 5 (compound 018) shows antagonist activity with IC50s of 0.24, 0.088, 0.068, 0.33, 0.79, 0.32, 0.079, 0.051 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 ]:
C21H25N3O2S

[ Molecular Weight ]:
383.51

Related Compounds

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