γ-Aminobutyric acid-13C4 (4-Aminobutyric acid-13C4) is the 13C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors).

FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the

Basmisanil is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome.

Arbaclofen placarbil is a novel transported prodrug of the active R-isomer of baclofen. Baclofen is a racemic GABAB receptor agonist

Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the treatment of a variety of central nervous system (CNS) disorders.

LAU159 is a novelα6β3γ2 GABAA receptor inhibitor.

TPMPA is a GABAA-ρ1 (ρ1 GABAC) receptor antagonist that is 8-fold selective for GABAA-ρ1 over GABAA-ρ2 (ρ2 GABAC) receptors expressed in X.

Homocarnosine is a dipeptide of γ-aminobutyric acid (GABA) and histidine unique to brain. Homocarnosine is an inhibitory neuromodulator synthesized in the neuron from GABA and exhibiting anticonvulsant effects.Homocarnosine has antioxidant and anti-inflammatory actions, prevention of DNA damage, and inhibition of advanced glycation end-product formation.

Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM.

γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain.

Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect.

Etifoxine Hydrochloride is a psychotropic agent with anxiolytic and anticonvulsant activity. Etifoxine Hydrochloride is an activator of GABAA R β2 and GABAA R β3.

Vigabatrin(γ-Vinyl-GABA; Sabril) is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase. IC50 value: Target: GABA transaminase Clinical studies have sh

CGP 35348 is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM. CGP 35348 shows affinity for the GABAB receptor only. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage.

3-Aminopropylphosphinic acid (3-APPA), a phosphonic analog of GABA, is a GABAB receptor agonist.

Pregabalin arenacarbil is a prodrug of Pregabalin.Pregabalin is an analog of gamma-aminobutyric acid (GABA) for the research of post herpetic neuralgia, peripheral diabetic neuropathy,fibromyalgia and epilepsy.

Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1).

Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties.

Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM.

TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons.

LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively.

Lesogaberan (hydrochloride) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively.

17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid.

Acamprosate D3 calcium is the deuterium labeled Acamprosate calcium. Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems.

Fengabine is a GABAergic antidepressant drug. Fengabine can be used for the research of depression.

CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC50 of 6 nM. CGP55845 hydrochloride can be used for neurological research.

Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact.

Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively.

GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3).

Etomidate (Amidate, R 16659) hydrochloride is a general anesthetic that produces its effects by enhancing GABA(A) receptor activity.