—gaba

γ-Acetylenic GABA hydrochloride is a GABA transaminase inhibitor.

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].

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.

GABA/BSA is an antigen-adjuvant conjugate of GABA (γ1-aminobutyric acid) with bovine serum albumin (BSA). Conjugating the antigen with a protein adjuvant enhances the production of antigen-specific antibodies in a vaccine model. This conjugate does not affect protein folding or damage major epitopes, and it can improve cross-presentation and the generation of antigen-specific T cells.

GABA/KLH is an antigen-adjuvant conjugate composed of GABA (γ1-aminobutyric acid) and keyhole limpet hemocyanin (KLH). This conjugation of antigen with a protein adjuvant enhances the production of antigen-specific antibodies in vaccine models. The conjugate preserves protein folding and maintains primary epitopes while promoting cross-presentation and the generation of antigen-specific T cells.

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.