GABA and Glycine Receptor Modulators

Gamma-Amino Butyric acid (GABA) and Glycine are neurotransmitters in the central nervous system that inhibit nerve transmission in the brain and retina respectively. There are several Sigma Bioactive Small Molecules you can choose from that target GABA and Glycine receptors, including agonists, antagonists, channel inhibitors/blockers, and anticonvulsants.

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A3750 21-Acetoxypregnenolone  
SML0897 ALX 5407 hydrochloride ≥98% (HPLC) ALX-5407 hydrochloride (NFPS hydrochloride) is a selective irreversible inhibitor of the glycine transporter GlyT1 with IC50 values of 3 nM for GlyT1 compared to 100 μM for GlyT2. ALX-5407 hydrochloride showed no activity at the inhibitory glycine receptor or glycine site of the NMDA receptor (IC50 > 100 mM).
T1694 (E)-4-Amino-2-butenoic acid  
A2129 γ-Aminobutyric acid ≥99% GABA (γ-Aminobutyric acid) is an amino acid that functions as an inhibitory neurotransmitter in the central nervous system and also functions as a neuromodulator in some peripheral tissues. It binds to GABAA receptor and inhibits the activity of signal-receiving neurons. The GABAA receptors are found to form a channel in the cell membranes of neurons. Upon binding of GABA, the receptor is activated to allow the passage of negatively charged molecules, such as chloride ions, into the cell. This results in lowering of excitability of the cell.
GABAergic neurons are involved in myorelaxation, anxiolytic treatment, sedation, and anaesthetics. GABA can also influence heart rate and blood pressure.
Major inhibitory neurotransmitter in brain; GABAA and GABAB receptor agonist; increases Cl conductance.
B104 tert-Butyl bicyclo[2.2.2]phosphorothionate solid GABAA receptor antagonist; chloride channel blocker; extremely potent convulsant.
C4024 Carbamazepine powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site. Sodium channel inhibitor.
Carbamazepine is considered as a safe antiepileptic drug. It decreases the multiple drug therapy and maintains a better control of epilepsy.
C8981 Carbamazepine meets USP testing specifications Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site. Sodium channel inhibitor.
C1240 Chlormethiazole hydrochloride ≥98% (HPLC), powder Chlormethiazole serves as an anticonvulsant. It is useful in treating alcohol addiction and eclampsia. Chlormethiazole is also useful in treating convulsive status epilepticus. Long term administration of chlormethiazole leads to addiction to the drug.
GABAA agonist; glycine receptor modulator.
D0447 D12-116 trifluoroacetate salt ≥98% (HPLC), powder D12-116 is a specific allosteric modulator of the glycine receptor (GlyR). The peptide D12-116 produces a marked enhancement of GlyR function while not affecting a1b2g2S GABAA receptors.
D5297 Dehydroisoandrosterone 3-sulfate sodium salt dihydrate ≥93% (TLC), powder Dehydroisoandrosterone 3-sulfate sodium salt dihydrate is a negative allosteric modulator of GABAA receptors.
D4875 16-Dehydropregnenolone acetate ≥95% 16-Dehydropregnenolone acetate (DPA) is synthesized from steroids sapogenin, diosgenin and solasodine. 16-Dehydropregnenolone acetate (DPA) is a crucial intermediate for the synthesis of steroid hormones-based drugs. It is an antagonist for farnesoid X receptor (FXR) and modulates cholesterol metabolism. It is considered as a potential antihyperlipidemic agent. Chemically synthesized steroid derivatives from DPA have cytotoxic features and could serve as potential anticancer agents.
P2016 3α,21-Dihydroxy-5α-pregnan-20-one ≥95% Positive allosteric modulator of GABAA receptors.
P5902 3α,12α-Dihydroxy-5β-pregnan-20-one 3,12-diacetate  
E4625 16,17-Epoxy-21-acetoxypregnenolone ≥98%  
E4875 16α,17α-Epoxypregnenolone  
E5000 16α,17α-Epoxypregnenolone acetate ~95%  
E6530 Etomidate >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
G154 Gabapentin 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.
Gabapentin serves as a ligand for the α2δ subunit of L-type calcium channels.
T101 Gaboxadol hydrochloride solid, ≥98% (HPLC) GABAA receptor agonist.
G7795 Ganaxolone 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.
G7126 Glycine ReagentPlus®, ≥99% (HPLC) Glycine is an inhibitory neurotransmitter in the central nervous system and works as an allosteric regulator of NMDA (N-methyl-D-aspartate) receptors. It is involved in processing of motor and sensory data, thereby regulating movement, vision and audition.
Inhibitory neurotransmitter in spinal cord, allosteric regulator of NMDA receptors.
G2879 Glycine hydrochloride ≥99% (HPLC) Glycine acts on receptors which bring out an enhanced chloride conductance. It shows highest concentrations in the spinal cord as compared to elsewhere in the brain. However, it interacts with and allostericaly activates the excitatory receptor N-methyl-D-aspartate (NMDA), thus, resulting in excitatory transmission in brain.
Glycine comprises a single carbon molecule, that is attached to the amino and a carboxyl group. Glycine hydrochloride (Gly·HCl) is capable of liquifying native chitosan and also helps in the preparation of regenerated chitosan membrane. It can serve as an osmoprotectant. Glycine can act as a flexible link in proteins and can also allow the formation of helices. Free glycine may have a protecting role in tissues against ischemia, hypoxia and reperfusion.
Inhibitory neurotransmitter in spinal cord, allosteric regulator of NMDA receptors.
G6761 Glycine sodium salt hydrate ≥99% (HPLC) Glycine is essential for the regulation immune function, metabolism, growth and development. It modulates intracellular Ca2+ levels and cytokines production. A reduction in glycine levels is observed in obesity, type 2 diabetes (T2DM), and non-alcoholic fatty liver disease (NAFLDs). Glycine is degraded to serine by glycine serine hydroxymethyltransferase 1 in cytoplasm.
G007 Guvacine hydrochloride ≥97% (NMR), solid GABA uptake inhibitor.
H5002 17α-Hydroxypregnenolone  
H5127 17α-Hydroxypregnenolone 3-acetate ≥98%  
H1384 Hypotaurine ≥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.
Hypotaurine, a cystamine analog, is the precursor for taurine synthesis. It can act as an antioxidant and singlet oxygen scavenger, thereby protecting cells from oxidative damage. Hypotaurine is reported to play an important role in the maintenance and stimulation of sperm motility and also in vitro fertilization and embryo development.
G002 Isoguvacine hydrochloride solid GABAA receptor agonist.
M1523 Muscimol powder GABAA receptor agonist.
G019 Muscimol hydrobromide ≥98% (HPLC), solid Muscimol hydrobromide is a GABAA receptor agonist.
211672 Nipecotic acid 98%  
N142 NO-711 hydrochloride ≥98% (HPLC) NO-711 is a potent and selective GABA uptake inhibitor that crosses the blood-brain barrier.
SML0647 Phenazepam ≥97% (HPLC) Phenazepam is the benzodiazepine that exhibit anticonvulsive, anxiolytic, sedative and hypnotic effects in humans and experimental animals. Phenazepam is an agonist of the γ-Aminobutyric acid A (GABAA)-benzodiazepine receptor chloride channel complex.
P1675 Picrotoxin powder GABAA receptor antagonist; binds to the GABA receptor-linked Cl channel.
Picrotoxin is a competitive inhibitor of glycine receptors (GlyRs). It is a non-competitive antagonist, which binds to ligand bounded γ-aminobutyric acid (GABAA) receptor.
P8390 Picrotoxinin GABAA receptor antagonist; binds to the GABA receptor-linked Cl channel.
P9159 Piperidine-4-sulfonic acid GABAA receptor agonist.
P5052 5α-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.
P8887 5α-Pregnan-3α-ol-20-one solid 5α-Pregnan-3α-ol-20-one is a positive allosteric modulator of γ-aminobutyric acid (GABA) A receptor (GABAA). It is also called pregnan and during pregnancy it modulates the atrial volume receptors transducer properties. During estrus cycle, 5α-Pregnan-3α-ol-20-one or allopregnanolone levels changes in hypothalamus. It is present in high levels post adrenalectomy and gonadectomy.
P8004 5α-Pregnan-3β-ol-20-one 3β-acetate ≥98%  
P162 Pregnenolone sulfate sodium salt Pregnenolone sulfate is a neurosteroid and a neuromodulator. It is involved in the stimulation of N-methyl-D-aspartate receptor (NMDA), γ-Aminobutyric acid type A (GABAA ) and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA-kainate). It activates transient receptor potential melastatin (TRPM3) which is a calcium-permeable ion channel. It improves schizophrenia and behavioral anomalies by modulating NMDA mediated Ser/Thr kinase - glycogen synthase kinase 3 β (AKT/GSK3β) signaling pathway.
P5489 Propybicyphat 95% (NMR), solid GABA-gated chloride channel blocker, non-competitive GABA antagonist in mammals.
SML0775 PZ-II-029 ≥98% (HPLC) PZ-II-029 is the first compound to be identified as a specific postitive modulator of GABAA channels composed of α6β3γ2 subunits.
S7936 SB 205384 solid GABAA receptor modulator selective for the α3β2γ2 subunit combination.
SB 205384 is a selective and positive allosteric modulator of non-benzodiazepine site of the GABAA receptor.3 It affects the extrasynaptic GABAA receptors in rat cortical neurons4 and enhances the GABAergic transmission onto pro-opiomelanocortin neurons in mice.5
S4250 D-Serine ≥98% (TLC) D-serine is essential for the normal development of dendrites, neuroblast migration and may have therapeutic potential for treating schizophrenia and depression states. The levels of D-serine is elevated in traumatic brain injury (TBI).
S4500 L-Serine ReagentPlus®, ≥99% (HPLC) L-Serine is a non-essential amino acid that acts as a precursor for nucleotide synthesis. It has roles in the development and function of the central nervous system. L-Serine also has a role in cellular proliferation.
Precursor of glycine by serine hydroxymethyltransferase.
S9066 SKF-89976A >98% (HPLC), solid GABA transporter type 1 (GAT-1) inhibitor that crosses the blood brain barrier.
SKF-89976A contains a cyclic amino acid with lipophilic moiety that enables the compound to cross the blood-brain barrier.1,2 It decreases the excitotoxic swelling of chick retina cells by blocking the glutamate-induced GABA release.3
S1069 (S)-SNAP-5114 ≥98% (HPLC), solid GABA transport inhibitor, showing selectivity for GAT-3 and GAT-2.
SML0774 SR 3677 ≥98% (HPLC) SR-3677 is a very potent, selective ROCK inhibitor, with higher potency against ROCK II (IC50 = 3 nM) than ROCK I (IC50 = 56 nM). In a kinase screening panel, SR-3677 was shown to only have activity against three other kinases (PKA, MRCK and Akt1) all with IC50 values over 1 μM. The compound has nM potency in cell based assays, and is efficacious in an ex-vivo model for increasing aqueous humor outflow in porcine eyes.
SR3677 decreases amyloid precursor protein (sAPPβ) and amyloid-β (Aβ) in a dose-dependent manner. In 5XFAD mouse brain, SR3677 represses the enzymatic activity of β-site APP cleaving enzyme 1 (BACE1). SR3677 has the ability to change the endocytic supply of BACE1 and induce APP traffic to lysosomes.
S106 SR-95531 ≥98% (HPLC), powder SR-95531 is a specific GABAA receptor antagonist that does not affect GABA-transaminase or glutamate-decarboxylase activities.
S0532 Strychnine At low doses, strychnine is used for circulatory problems, gastrointestinal disorders and eye diseases.
Convulsant; glycine receptor antagonist not associated with the NMDA receptor.
Strychnine is used as a rodenticide and a glycine receptor antagonist, which inhibits Renshaw cell-motor neuron synapse. It binds to the α subunit N-terminal region of the glycine receptor. The effect of strychnine is neutralized in the presence of glycine receptor agonist ivermectin. Strychnine also inhibits leukocyte motility.
S8753 Strychnine hydrochloride Convulsant; glycine receptor antagonist not associated with the NMDA receptor.
Strychnine is a potent convulsant, which is extracted from Strychnos nux vomica seeds. At high doses, the compound causes convulsions and ultimately death due to respiratory paralysis. Strychnine acts as a respiratory, circulatory and digestive stimulant.
T0625 Taurine ≥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.
Taurine modulates the concentration of intracellular calcium, protects against ischemia-reperfusion injury and possesses blood pressure-lowering properties. It also has a role in bile formation and fat digestion. Deficiency of taurine is associated with anxiety, hyperactivity, epilepsy and depression.
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.
SML1476 Thiocolchicoside ≥98% (HPLC) Thiocolchicoside acts as a muscle relaxant. In experimental animals, thiocolchicoside results in malfunctions (teratogenic) and impairs chromosomes. It is advised to be used as an analgesic for patients with muscle pain, starting with paracetamol. Thiocolchicoside can be used in irrigation solution at the time of endoscopic treatment of ureteral calculus to reduce the movement of stones.
Thiocolchicoside is a potent competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist with muscle relaxant, anti-inflammatory, and analgesic activity. Thiocolchicoside has also been found to suppress nuclear factor kappa B ligand (RANKL) activation of NF-KB resulting in suppression of osteoclastogenesis.
89231 (−)-α-Thujone ≥96.0% (GC) GABAA receptor antagonist.
SML0035 Tiagabine hydrochloride ≥98% (HPLC) Tiagabine hydrochloride is an anticonvulsant and selective GABA reuptake inhibitor through inhibition of the synaptic GABA transporter GAT1.
Tiagabine increases the synaptic GABA and enhances the neuronal inhibition. It is effective as adjunctive treatment of epilepsy and anxiety disorders.
T8200 Tofisopam ≥98% (HPLC), solid Ligand for the GABAA receptor benzodiazepine modulatory site.
Studies have reported that tofisopam functions by blocking PDE4 (phosphodiesterase 4). Furthermore, the S-enantiomer of tofisopam is considered ten times more active than R-enantiomer.