gaba

γ-Acetylenic GABA hydrochloride is a GABA transaminase inhibitor.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.

Broflanilide is metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin GABA receptor and inhibits S. litura RDL GABAR (IC50: 1.3 nM).

Riluzole (RP-54274) is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.

γ-Aminobutyric acid (4-Aminobutyric acid) is the predominant inhibitory neurotransmitter in the central nervous system.

L-Cycloserine ((-)-Cycloserine) irreversibly inhibits GABA pyridoxal 5′-phosphate-dependent aminotransferase in E. coli, as well in the brains of various animals, results in increased levels of gamma-aminobutyric acid (GABA), which is an inhibitory neurotransmitter in vivo.

Tramiprosate (Alzhemed) is an orally active, blood-brain-barrier-crossing, naturally occurring amino acid found in a variety of red seaweeds that binds soluble Aβ and maintains it in a non-protofibrillar form.It is a GABA analog with neuroprotective, anticonvulsant, and antihypertensive activity.

Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.

Fipronil (Fluocyanobenpyrazole) is a broad-use insecticide that belongs to the phenylpyrazole chemical family. Fipronil is a broad-spectrum insecticide that disrupts the insect central nervous system by blocking GABA-gated chloride channels and glutamate-gated chloride (GluCl) channels, resulting in central nervous system toxicity. This causes hyperexcitation of contaminated insects' nerves and muscles. Specificity of fipronil on insects may come from a better efficacy on GABA receptor, but also because GluCl channels do not exist in mammals.

L-Allylglycine is an amino acid derivative that reduces glutamate decarboxylase (GAD) activity by 60% when administered at a dose of 39.8 μmol/g per hour ex vivo in mouse brain preparations. L-Allylglycine (1.2 mmol/kg, i.p.) induces convulsions and decreases GABA concentration throughout the cerebellum, pons, medulla, striatum, cortex, and hippocampus in mice. Chronic administration (3.2 μg/0.5 μl per hour for 13 days) of L-allylglycine in rats increases locomotor activity in an open field test and impairs attention in the 5-choice serial reaction time task (5CSRTT). In vitro, L-allylglycine inhibits GAD only when used at high concentrations (1-80 mM). The more potent in vivo activity can be attributed to metabolic conversion of L-allylglycine to 2-keto-4-pentanoic acid, a more potent convulsant and GAD inhibitor.

(-)-borneol (L-Borneol) has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.

Aminooxyacetic acid hemihydrochloride (Carboxymethoxylamine Hemihydrochloride) is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.

Etifoxine hydrochloride (HOE 36-801 hydrochloride) is an anxiolytic and anticonvulsant drug. Unlike benzodiazepines, Etifoxine hydrochloride appears to produce its anxiolytic effects by binding to β2 and β3 subunits of the GABAA receptor complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines.

Isoguvacine hydrochloride (1,2,3,6-tetrahydro-4-pyridinecarboxylic acid hydrochloride) is a GABA receptor agonist. Isoguvacine hydrochloride binds to rat synaptic cortical membranes and activates α1β2γ2S, α2β2γ2S, α3β2γ2S, α5β2γ2S, and ρ1 subunit GABAA receptors.

Afoxolaner is an isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

L-838417 is a GABAA receptor subtype-selective benzodiazepine site-selective ligand and GABAA receptor-positive modulator.L-838417 is a selective partial agonist of the α2, α3, and α5 subtypes and an antagonist of the α1 subtype and is used in the study of anxiety disorders.

Tiagabine (NO050328) is an Anti-epileptic Agent. The physiologic effect of tiagabine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Homocarnosine acetate is a dipeptide unique to brain consisting of γ-aminobutyric acid (GABA) and histidine. Homocarnosine acetate has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation

Phellopterin is a partial agonist of the central benzodiazepine receptors in vitro. Phellopterin shows a cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM. Phellopterin reduce TNF-alpha-induced VCAM-1 expression through regulation o

rac-BHFF ((R,S)-BHFF) is potent and selective GABA B receptor positive allosteric modulator that increases the potency and efficacy of GABA ( > 15-fold and > 149% respectively). It exhibits anxiolytic activity in vivo and is orally active.

Guvacine hydrochloride is an inhibits of GABA uptake (IC50 : 10 μM)

L-DABA (L-2,4-Diaminobutyric acid) is an inhibitor of GABA transaminase with an IC50 greater than 500 μM.

AZD7325 (AZD-7325) is a GABA-Aα2,3 -selective receptor modulator.

Guvacine ethyl ester (Arecoline) is an alkaloid found in betel nut that is used in the synthesis of GABA uptake inhibitors.