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).

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.

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

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

Boc-GABA-OH serves as a PROTAC linker essential for synthesizing UNC6852, an EED-targeted PROTAC[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-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-AT-IN-1 (Compound 6) inhibits γ-aminobutyric acid transaminase (GABA-AT) and crosses the blood-brain barrier.

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].

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.

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.

GABAB receptor agonist

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].

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).

Ruthenium-bipyridine-triphenylphosphine caged GABA

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.

Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2 PAM, respectively.Darigabat is used in the study of anxiety disorders and epilepsy.

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist that decreases GABA-induced IP3 (inositol trisphosphate) production with an IC50 of 37.9 μM. It is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

Imagabalin is an active compound used in the study of neurological diseases.

(Iso)-Atagabalin HCl(isomer-Atagabalin HCl) is an alpha -2- delta ligand that can be used to treat non-restorative sleep.

Atagabalin HCl is a novel voltage-dependent calcium channel (VDCC) α2δ subunit (1 and 2) ligand that affects slow-wave sleep and can be used to treat insomnia.