α subunit-containing gabaa receptors (gabaaα5)

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

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 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 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 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].

Survivin (baculoviral inhibitor of apoptosis IAP repeat-containing protein-5) is a member of the IAP gene family, which has been implicated in both inhibitions of apoptosis and mitosis regulation1. Survivin is one of the most uniformly up-regulated genes

GABAA receptor agonist 1 (compound 3e) is a potent agonist that binds to the GABA binding site of the GABAA receptor, producing GABAergic effects and exhibiting anti-depression activities in classical mouse models of FST and TST, indicating its potential in depression research [1].

GABAA receptor agonist 2 (compound 4c) is a highly potent compound that exhibits anti-depressive properties in classical mouse models of depression, such as the FST and TST. By binding to the GABA binding site on the GABAA receptor, it produces GABAergic effects. Notably, compound 4c holds promise for depression research [1].

GABAA receptor modulator-2 (Compound 20) is a selective, orally active α5-GABAAR negative conformation modulator (Ki: 4.1 nM) that exhibits high metabolic stability and a good central nervous system safety profile.

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 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].

Basmisanil (RG1662) is a negative allosteric modulator/inverse agonist of GABAAα5 receptors.Formulations containing basmisanil are in clinical trials for the treatment of cognitive impairments associated with Down syndrome.