gabaa receptor agent-1

GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.

3-Methyl-GABA, an anticonvulsant agent [1] [2], acts as a potent activator of GABA aminotransferase, fits the binding pocket of the GABA A receptor (GABAaR), and activates L-glutamic acid decarboxylase (GAD).

Anxiolytic nonsedative agent-1 (TCS 1205) is a potent and selective GABAA agonist. Anxiolytic nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.

GABAA receptor agent 4 (compound 1e) is a potent antagonist of γ-GABAAR, exhibiting a Ki of 0.18 µM, and demonstrates immunomodulatory potential by effectively rescuing the inhibition of T cell proliferation [1].

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

GABAA receptor agent 8 (compound 5e) is a potent positive modulator of the GABAA receptor, exhibiting anticonvulsant activity in both in vitro and in vivo studies, with low neurotoxicity, indicating its potential in epilepsy research [1].

GABAA receptor agent 7 (compound 5c) is a potent positive modulator of the GABAA receptor with anticonvulsant activity in vitro and in vivo, and low neurotoxicity, making it suitable for epilepsy research [1].

GABAA Receptor Agent 5 (compound 018) serves as a potent γ-GABAAR antagonist, possessing a Ki of 0.020 μM. This compound exhibits γ-GABAAR antagonist properties, yet it demonstrates low cellular membrane permeability [1].

GABAA receptor agent 2 TFA is a potent, high-affinity GABAA receptor antagonist with an IC50 of 24 nM [human α1β2γ2GABAA-expressing tsA201 cells] and a Ki of 28 nM [rat GABAA receptor]. GABAA receptor agent 2 TFA has no effect on four human GABA transport proteins [hGAT-1, hBGT-1, hGAT-2, and hGAT-3].