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GABA and Glycine Receptor Modulators



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89231(−)-α-Thujone purum, ≥96.0% (GC) pricing
T200(1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid hydrate ≥97% (HPLC), solid TPMPA is a hybrid of isoguvacine and 3-APMPA designed to retain affinity for GABAC receptors but not to interact with GABAA or GABAB receptors. Electrical assays show that TPMPA is a competitive antagonist of cloned human mu 1 GABAC receptors expressed in Xenopus laevis oocytes (Kb approx. 2 μM). TPMPA is >100-fold weaker as an inhibitor of rat brain GABAA receptors expressed in oocytes (Kb approx. 320 μM) and has only weak agonist activity on GABAB receptors assayed in rat hippocampal slices (EC50 approx. 500 μM). TPMPA may be used to investigate GABAC receptor function in the outer retina and in any other areas of the nervous system in which these types of receptor are present.
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H8645(1S,9R)-(+)-β-Hydrastine Potent competitive GABAA receptor antagonist which is more potent than bicuculline; isolated from Corydalis stricta.
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T1694(E)-4-Amino-2-butenoic acid solid Potent GABAc receptor agonist.
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S1069(S)-SNAP-5114 ≥98% (HPLC), solid GABA transport inhibitor, showing selectivity for GAT-3 and GAT-2.
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E462516,17-Epoxy-21-acetoxypregnenolone ≥98% pricing
D487516-Dehydropregnenolone acetate ≥95% pricing
E487516α,17α-Epoxypregnenolone pricing
E500016α,17α-Epoxypregnenolone acetate ~95% pricing
H500217α-Hydroxypregnenolone pricing
H512717α-Hydroxypregnenolone 3-acetate ≥98% pricing
A375021-Acetoxypregnenolone pricing
A41473-Amino-1-propanesulfonic acid sodium salt ≥98% GABAA receptor agonist.
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P59023α,12α-Dihydroxy-5β-pregnan-20-one 3,12-diacetate pricing
P20163α,21-Dihydroxy-5α-pregnan-20-one ≥95% Positive allosteric modulator of GABAA receptors.
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P50525α-Pregnan-3α-ol-11,20-dione powder, ≥98% (TLC) Synthetic steroid compound alphaxalone (AFX) - 5α-Pregnan-3α-ol-11,20-dione- is a neurosteroid that directly activates and potentiates GABAA receptor-activated membrane current (IGABA). It acts as a positive allosteric modulator of the GABAA receptor; anesthetic. The alpha subunit subtype of GABAA determines the efficacy, but not the potency, of AFX neuroactive steroid to potentiate IGABA.
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P88875α-Pregnan-3α-ol-20-one solid Positive allosteric modulator of GABAA chloride channel.
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P80045α-Pregnan-3β-ol-20-one 3β-acetate ≥98% pricing
S4250D-Serine ≥98% (TLC) Glycine mimic active at the strychnine-insensitive glycine binding site associated with the NMDA receptor as well as the inhibitory post-synaptic glycine receptor.
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S4500L-Serine ReagentPlus®, ≥99% (TLC) Precursor of glycine by serine hydroxymethyltransferase.
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A8977ALX 5407 hydrochloride >98% (HPLC), solid Selective, irreversible GlyT-1 glycine transporter inhibitor.
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A5475ALX-1393 >98% (HPLC), powder GlyT-2 glycine transporter inhibitor.
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C8981Carbamazepine meets USP testing specifications Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site.
Sodium channel inhibitor
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C4024Carbamazepine powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site.
Sodium channel inhibitor
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C1240Chlormethiazole hydrochloride ≥98% (HPLC), crystalline GABAA agonist; glycine receptor modulator.
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C1983Cloflubicyne ≥95% (NMR), solid pricing
D1193DEABL ≥98% (LC/MS), solid Positive modulator of GABAA receptor; anticonvulsant
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D5297Dehydroisoandrosterone 3-sulfate sodium salt dihydrate ≥98%, powder Dehydroisoandrosterone 3-sulfate sodium salt dihydrate is a negative allosteric modulator of GABAA receptors.
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E5277Etbicyphat ≥95% (NMR), solid Blocker of neuronal voltage-dependent and GABA-gated chloride channels; non-competitive GABA antagonist; causes epileptiform seizures.
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E5402Etbicythionat ≥98% (NMR), solid A potent non-competitive GABA antagonist in mammals; causes epileptiform seizures.
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E6530Etomidate >98% (HPLC), powder Etomidate is a general anesthetic; potentiates GABAA transmission. The possible neuroprotective effect of etomidate against streptozotocin-induced (STZ-induced) hyperglycaemia were investigated in the rat brain and spinal cord. Etomidate treatment demonstrated neuroprotective effect on the neuronal tissue against the diabetic oxidative damage
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F6551Flucybene ≥95% (NMR), solid A potent non-competitive GABA antagonist in mammals, molluscs and insects; convulsant.
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G5919GS39783 ≥98% (HPLC), powder Positive allosteric modulator of GABAB receptors
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G154Gabapentin solid Anticonvulsant with unknown mechanism of action; crosses the blood brain barrier; increases GABA concentrations in the brain and reduces excitatory amino acid neurotransmission, perhaps through its effects on voltage-gated calcium channels; exhibits antinociceptive, anxiolytic, neuroprotective and anti-epileptic effects.
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T101Gaboxadol hydrochloride solid, ≥98% (HPLC) GABAA receptor agonist.
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G7795Ganaxolone solid Ganaxolone (3alpha-hydroxy-3beta-methyl-5alpha-pregnane-20-one) is a positive allosteric modulator of the GABAA receptor subtype; synthetic analog of the endogenous neurosteroid allopregnanolone; effective against chemically induced seizures in rats and mice. Ganaxolone is an orally active analog of allopregnanolone that is not converted to the hormonally active 3-keto form. The enhanced anticonvulsant potency of ganaxolone after neurosteroid withdrawal supports the use of ganaxolone as a specific treatment for perimenstrual catamenial epilepsy.
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G7126Glycine ReagentPlus®, ≥99% (TLC) Inhibitory neurotransmitter in spinal cord, allosteric regulator of NMDA receptors.
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G2879Glycine hydrochloride ≥99% (TLC) Inhibitory neurotransmitter in spinal cord, allosteric regulator of NMDA receptors.
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G6761Glycine sodium salt ≥99% (TLC) Inhibitory neurotransmitter in spinal cord, allosteric regulator of NMDA receptors.
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G007Guvacine hydrochloride ≥97% (NMR), solid GABA uptake inhibitor.
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H1384Hypotaurine ≥98% (TLC) Antioxidant that binds hydroxyl radicals. Endogenous inhibitory neuromodulator that is blocked by strychnine and picrotoxin. Inhibits the Na2+-dependent transport of GABA and β-alanine. It is a degradation product of cysteine and a precursor of taurine.
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I7013Imidazole-4-acetic acid sodium salt Competitive antagonist at GABAC receptors.
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G002Isoguvacine hydrochloride solid GABAA receptor agonist.
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G019Muscimol hydrobromide ≥98% (HPLC), solid Muscimol hydrobromide is a GABAA receptor agonist.
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M1523Muscimol powder GABAA receptor agonist.
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N142NO-711 hydrochloride solid, ≥98% (HPLC) Potent and selective GABA uptake inhibitor that crosses the blood-brain barrier.
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211672Nipecotic acid 98% pricing
P204Phenylbenzene ω-phosphono-α-amino acid solid Selective strychnine-sensitive glycine receptor antagonist.
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P1675Picrotoxin powder GABAA receptor antagonist; binds to the GABA receptor-linked Cl channel.
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P8390Picrotoxinin GABAA receptor antagonist; binds to the GABA receptor-linked Cl channel.
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P9159Piperidine-4-sulfonic acid GABAA receptor agonist.
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P162Pregnenolone sulfate sodium salt Neurosteroid that antagonizes the GABAA receptor chloride channel.
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P5489Propybicyphat 95% (NMR), solid GABA-gated chloride channel blocker, non-competitive GABA antagonist in mammals.
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S7936SB 205384 solid GABAA receptor modulator selective for the α3β2γ2 subunit combination.
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S9066SKF-89976A >98% (HPLC), solid GABA transporter type 1 (GAT-1) inhibitor that crosses the blood brain barrier.
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A196SKF-97541 hydrochloride solid Selective GABAB receptor agonist; GABAC receptor antagonist.
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S106SR-95531 ≥98% (HPLC), solid SR-95531 ia a specific GABAA receptor antagonist that does not affect GABA-transaminase or glutamate-decarboxylase activities.
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S8194Salicylidene salicylhydrazide ≥98% (HPLC), solid Potent and selective inhibitor of α2β1γ1δ GABAA receptor subtype.
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S0532Strychnine Convulsant; glycine receptor antagonist not associated with the NMDA receptor.
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S8753Strychnine hydrochloride Convulsant; glycine receptor antagonist not associated with the NMDA receptor.
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T0625Taurine ≥99% Non-selective endogenous agonist at glycine receptors. Conditionally essential sulfonated amino acid which modulates apoptosis in some cells; functions in many metabolic activities; a product of methionine and cysteine metabolism.
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T8200Tofisopam ≥98% (HPLC), solid Ligand for the GABAA receptor benzodiazepine modulatory site.
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X4628Xli 093 hydrate ≥98% (HPLC), powder Xli 093 is α5 subtype selective benzodiazepine/GABAA receptor antagonist. Xli 093 shows Ki = 5 nM at the α5 receptor in Ltk- cell membranes expressing human α5β3γ2 receptors; little or no affinity at other BDZ/ GABAA subtypes; does not trigger chloride currents in any subtype of tested subtypes, up to 1 μM in concentration; dose-dependently and completely inhibits diazepam stimulated currents in α5β3γ2 receptors.
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A2129γ-Aminobutyric acid ≥99% Major inhibitory neurotransmitter in brain; GABAA and GABAB receptor agonist; increases Cl conductance.
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H3635γ-Hydroxybutyric acid sodium salt Endogenous GABA analog that induces absence-like seizures. It blocks dopamine release by blocking impulse flow in dopaminergic neurons.
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B104tert-Butyl bicyclo[2.2.2]phosphorothionate solid GABAA receptor antagonist; chloride channel blocker; extremely potent convulsant.
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