γ-Acetylenic GABA hydrochloride is a GABA transaminase inhibitor.

BL-1020 Mesylate (CYP-1020 Mesylate) is an orally available GABA A receptor agonist and D2 antagonist that decreases dopamine activity and enhances GABAA activity.BL-1020 Mesylate has been used in the study of schizophrenia, Alzheimer's disease, and bi-directional cognitive impairment.

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 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. Moreover, this compound exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg/adult) and low toxicity to zebrafish (LC50: 42.4 mg/L) [1].

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

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].

Ruthenium-bipyridine-triphenylphosphine caged GABA

Gamibetal (4-Amino-3-hydroxybutyric Acid) is used as a chiral reagent in the synthesis of antiepileptic and hypotensive drug GABOB and analogues. Also used in the preparation of HIV-1 inhibitors derived from Betulinic Acid (B330250).

GABA-AT-IN-1 (Compound 6) is an inhibitor of γ-aminobutyric acid transaminase (GABA-AT) that crosses the blood-brain barrier.

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.

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.

GABAB receptor agonist

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

Methyl 4-aminobutyrate HCl (GABA methyl ester) is a methyl ester compound derived from the condensation of aminobutyric acid and methanol.

Pikamilone (Picamilon) is an intelligent medicine.

(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.

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM. GABAB receptor antagonist 1 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.

Atagabalin, also known as PD 0200390, is a gabamimetic agent under development for the treatment for insomnia. Atagabalin is related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2). It was discontinued following unsatisfactory t

Pikamilone Sodium is a prodrug of GABA used for therapy of neurogenic bladder in spinal and benign prostatic hyperplasia.

γ-Aminobutyric acid (4-Aminobutyric acid) is the most common inhibitory neurotransmitter in the central nervous system.

4-Acetamidobutanoic acid (4-ACETAMIDOBUTYRIC ACID) can be found in blood, feces, and urine, as well as in human prostate tissue. 4-Acetamidobutanoic acid exists in all eukaryotes, ranging from yeast to humans. 4-Acetamidobutanoic acid is a GABA derivative, a product of the urea cycle and the metabolism of amino groups, and the product of NAD-linked aldehyde dehydrogenase (EC 1.2.1.3) (KEGG).

Gabapentin (Neurontin) is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.

(+)-BORNEOL (d-Borneol) is a natural bicyclic monoterpene used for analgesia and anesthesia in traditional Chinese medicine; enhances GABA receptor activity with an EC50 of 248 μM.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

6-Methoxyflavanone (6-MeOF) is A positive allosteric modulator of the GABA response of human recombinant GABA A receptor, with antianxiety and anti-inflammatory activity, and can be used to reduce cisplatin induced neuropathic pain.

Cholesterol Myristate (Cholesteryl Myristate) is a natural steroid found in traditional Chinese medicine that interacts with various ion channels, including the GABAA receptor, nicotinic acetylcholine receptor, and the inward-rectifier potassium ion channel.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.

DL-Menthol ((±)-Menthol) is a racemic mixture of the monoterpene alcohols (–)-menthol and (+)-menthod, which have been found in Cannabis. (–)-Menthol is more common than (+)-menthol in nature and exhibits analgesic, antibacterial, and anticancer properties, as well as inhibits cholinesterase.2 (+)-Menthol inhibits the growth of F. verticillioides (MIC: 1.5 mM) but, unlike (–)-menthol, does not exhibit analgesic, antibacterial, anticancer, or cholinesterase inhibitory activities.

Nerisopam is an agonist of gamma-aminobutyric acid (GABA) receptor.

NS-2710 is a non-selective GABA(A) receptor partial agonist for the study of anxiety disorders.

2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors.It offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response. 2'MeO6MF has anxiolytic and sedative effects.

SCS is a GABAA receptor antagonist.

Suriclone (RP 31264) is a selective cyclic pyrrolidone analog with sedative and anxiolytic activity, but not significant sedative effects.Suriclone shows its effects by modulating GABA-A receptors.

UK-124114 (Selamectin) is a macrocyclic lactone derivative of ivermectin, an anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. In an H. contortus larval development assay, selamectin (0.1 μg/ml) shows the effect of growth inhibition.

Fengabine (SL-79229) is a GABA receptor agonist with antidepressant activity and is used to treat depression.

Golexanolone (Golexanolona) is a novel GABA-A receptor-modulating steroid antagonist that reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in rats with chronic hyperammonemia, and may be used to study hepatic encephalopathy.

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.

RWJ-51204 is a selective adenosine A2A receptor antagonist and a partial agonist of GABA(A) receptor (IC50: 0.2-2 nM). It has neuroprotective and movement-improving effects and can be used in research related to Parkinson's disease.

NO-711ME (N-O711 Methyl ester) is a prodrug of NO-711. It also is a potent and selective GABA uptake inhibitor.

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

Divaplon is a GABA receptor agonist (IC50: 0.056 µM) that displays non-sedating anxiolytic behavioral characteristics in a rat model of anxiety.

Losigamone (AO-33) is an agonist of GABA receptor and can be used in studies about the treatment of partial seizures.

Positive allosteric modulator of GABAA receptors

Neurotensin TFA (39379-15-2 free base) is an endogenous 13 amino acid neuropeptide with profound opioid-independent analgesic effects. It behaves as a neurotransmitter in the brain, as a hormone in the gut, and also as a neuromodulator. It is implicated in the pathophysiology of several CNS disorders (including schizophrenia, Parkinson's disease, drug abuse, pain, cancer, inflammation, eating disorders, and central control of blood pressure) due to its association with a wide variety of neurotransmitter systems such as dopaminergic, sertonergic, glutamatergic, GABAergic, and cholinergic systems. It has a role as a human metabolite, a mitogen, a neurotransmitter and a vulnerary.

Homocarnosine acetate is a dipeptide unique to brain consisting of γ-aminobutyric acid (GABA) and histidine. Homocarnosine acetate has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation

Imidazenil is an modulator of GABA-A that blocks the sedative effects without lowering the convulsion threshold.