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.

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.

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

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

β-Amyrin (beta-Amyrin) has antiviral, hepatoprotective, antinociceptive, anti-inflammatory

Bacopasaponin C may have antioxidant activity, it also shows anti-leishmanial property.

Boc-GABA-OH serves as a PROTAC linker essential for synthesizing UNC6852, an EED-targeted PROTAC[1].

GABA-A Receptor Ligand-1 (Compound 4) is a ligand for the GABA-A receptor with a pKi of 7.27. It alleviates mitochondrial dysfunction, promotes neurite outgrowth and neuronal regeneration, and demonstrates neuroprotective effects in a rat ischemic stroke model.

GABA-IN-4 (Compound 17) is a derivative of N-(indol-3-ylglyoxylyl)benzylamine. It exhibits high affinity for the benzodiazepine receptor (BzR), the binding site within the GABAA receptor complex, with a Ki value of 67 nM. Benzodiazepines are widely used as anxiolytic, sedative-hypnotic, and anticonvulsant agents.

GABOB is an anticonvulsant used to treat epilepsy. GABOB is an endogenous active metabolite, it is analogue to the neurotransmitter γ-aminobutyric acid (GABA), therefore may function as a neurotransmitter.

3-Methyl-GABA, an anticonvulsant agent [1] [2], acts as a potent activator of GABA aminotransferase, fits the binding pocket of the GABA A receptor (GABAaR), and activates L-glutamic acid decarboxylase (GAD).

GABAB receptor agonist

Ruthenium-bipyridine-triphenylphosphine caged GABA

γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is a potent, irreversible inhibitor of GABA-transaminase, effectively raising the concentration of γ-Aminobutyric acid (GABA) in the brain of rats.

GABA-AT-IN-1 (Compound 6) inhibits γ-aminobutyric acid transaminase (GABA-AT) and crosses the blood-brain barrier.

GABA-IN-2 (Compound 5), a GABA inhibitor, exhibits both larvicidal and insecticidal properties, achieving an 87% mortality rate at a concentration of 50 mg L [1].

GABA-IN-1 (Compound 6), a GABA inhibitor, exhibits larvicidal and insecticidal properties, achieving a mortality rate of 93% at a concentration of 50 mg L [1].

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg L. This compound also exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg adult) and low toxicity to zebrafish (LC50: 42.4 mg L) [1].