gaba

γ-Acetylenic GABA hydrochloride is a GABA transaminase inhibitor.

Vigabatrin (Sabril), an analogue of gamma-aminobutyric acid, is an irreversible inhibitor of 4-aminobutyrate Transaminase responsible for the catabolism of γ-aminobutyric acid.

Vigabatrin Hydrochloride (γ-Vinyl-GABA hydrochloride) is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA), which irreversibly inhibits the catabolism of GABA by GABA transaminase.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

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.

Piperazine citrate, an organic compound, consists of a six-membered ring, containing two nitrogen atoms at opposite positions in the ring. It used as an Anthelmintic.

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.

Fluralaner (A1443) is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes (IC50: 455 pM).

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

Baclofen hydrochloride (4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride) is a GAMMA-AMINOBUTYRIC ACID derivative that is a specific GABA-B RECEPTORS agonist. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

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.

GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism.

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.

NEO 376 (SPI-376) is a selective 5-HT1 receptor, GABA receptor and dopamine receptor modulator, showing anti-psychotic actively.

SCH 50911 hydrochloride is a selective, orally-active and competitive antagonist of γ-Aminobutyric acid B GABA(B) receptor(IC50 : 1.1 μM).

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.

Lotilaner is a parasiticide. It is used as a potent non-competitive antagonist of insects GABACl receptors (IC50 of 23.84 nM for Drosophila melanogaster GABA receptor). It also has no effect on a dog GABAA receptor.