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LAU159 is a potent, functionally selective positive modulator of α6β3γ2 GABAA receptor.

Other Indication

Phase 3 Clinical




Alprazolam (D-65MT;U 31889) is a triazolobenzodiazepine agent with anxiolytic, sedative-hypnotic and anticonvulsant activities; binds to a specific site distinct from the inhibitory neurotransmitter GABA binding site on the benzodiazepine-GABA-A-chloride ionophore receptor complex located in the limbic, thalamic and hypothalamic regions of the central nervous system (CNS).


Phase 2 Clinical



612527-56-7 HZ-166 (HZ166) is a GABAA receptor subtype-selective benzodiazepine site ligand with preferential activity at α2- and α3-GABA(A) receptors; displays a statistically significant higher affinity for receptors not containing the α1 subunit with a rank order of α5 (Ki=140nM) > α2 (Ki=269 nM) > α1 (Ki=382 nM); The Ki value of HZ166 for the α3β3γ2 combination (185± 47 nM) was statistically significantly lower than the Ki value observed for α1β3γ2 but not different from those of α2β3γ2 and α5β3γ2; HZ-166 is antihyperalgesic in mouse models of inflammatory and neuropathic pain.


2014348-91-3 KRM-II-81 is a potent, selective α1/α2/α3 GABAA receptors positive allosteric modulator with EC50 of 937 nM for α1β3γ2, negligible efficacy at α4/α5/α6 GABAA receptors; shows α2 and α3-subtypes being 17- and 28-fold more potent than α1 subtypes in HEK-293T cells expressing GABAA receptors with different α subunits.


2089238-18-4 GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC; inhibits α1β2γ2L receptor 29 ± 5% of THDOC enhancement of the GABA response, does not antagonize the effect of GABA at the GABAA receptor; during the specific conditions used for the different receptors, IC50=250 nM for the α1β2γ2L GABAA receptor and 350 nM for the α5β3γ2L GABAA receptor; restores spatial learning and motor coordination in rats with chronic hyperammonemia and hepatic encephalopathy.

Sleep Disorder

Phase 2 Clinical



1802661-73-9 ONO-8590580 is a novel potent, selective GABAA α5 negative allosteric modulator, binds to the benzodiazepine binding sites on recombinant human α5-containing GABAA receptors with Ki of 7.9 nM; shows functionally selective GABAA α5 NAM activity for GABA-induced Cl- channel activity with a maximum 44.4% inhibition and an EC50 of 1.1 nM; significantly augments tetanus-induced long-term potentiation of CA1 synapse response in rat hippocampal slices at 300 nM; significantly prevents MK-801-induced memory deficit in vivo (3-20 mg/kg, p.o.).


2187489-08-1 MIDD0301 is a potent, positive allosteric, α5β3γ2 selective, GABAA receptor (GABAAR) ligand with EC50 of 17 nM, shows no significant binding at the peripheral GABAAR at 10 uM; causes amplification of GABA induced current mediated by α1-3,5β3γ2 GABAARs in the presence of MIDD0301 in automated patch clamp test; relaxes airway smooth muscle at single micromolar concentrations as demonstrated with ex vivo guinea pig tracheal rings, also attenuates airway hyperresponsiveness (AHR) in an ovalbumin murine model of asthma by oral administration, with low brain distribution; reduces lung cytokine expression of IL-17A, IL-4, and TNF-α, as wells as the number of CD4+ T cells.

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