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Cat. No. Product Name CAS No. Information
PC-36106

SAGE-217

1632051-40-1

SAGE-217 (Zuranolone, SAGE217) is a potent, orally active GABAA receptor positive allosteric modulator with EC50 of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA r eceptors, respectively; effectively reduces pentylenetretazol (PTZ)-induced seizures in mice, abolishes both behavioral and electrographic seizure activity.

Depression

Phase 3 Clinical

PC-62098

LAU159

2055050-87-6

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

Other Indication

Phase 3 Clinical

PC-61895

Alprazolam

28981-97-7

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).

Epilepsy

Phase 2 Clinical

PC-35484

HZ-166

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.
PC-35483

KRM-II-81

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.
PC-35454

GR3027

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

PC-63442

ONO-8590580

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.).

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