GABAA receptor agent 4_product_DataBase

Bioactivity	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].
Target	Ki: 0.18 µM (γ-GABAAR)
Invitro	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].
Name	GABAA receptor agent 4
CAS	2035203-91-7
Formula	C17H24N2O
Molar Mass	272.39
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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