—gaba

γ-Acetylenic GABA hydrochloride is a GABA transaminase inhibitor.

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.

GABA receptor antagonist 2 (Compound IId) is a GABA receptor blocker with an LC50 of 0.0735 μg/mL against Plutella xylostella (P. xylostella). This compound exhibits significant insecticidal activity against P. xylostella and its resistant strains, as well as against Spodoptera frugiperda and Chilo suppressalis. GABA receptor antagonist 2 can bind to the GABA receptor at the Drosophila RdlG335 site and is useful for managing resistant pest populations.

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].

MC-Gly-Gly-Phe-Gly-GABA-Exatecan, functioning both as an ADC linker agent and a topoisomerase inhibitor (Exatecan), displays cytotoxic and antitumor properties in vitro and in vivo [1] [2]. It specifically targets various antibodies and boasts an IC 50 of 22 μM.

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.