NS11394 possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.

Lorediplon is a new GABAA modulator Drug for treatment of insomnia.

Indiplon is a novel sedative-hypnotic recently approved for the treatment of insomnia.

Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.

CGP 52432 is a potent, selective GABAB receptor antagonist (IC50 = 85 nM).

Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.

ONO-8590580 is a Novel GABAAα5 Negative Allosteric Modulator Enhances Long-Term Potentiation and Improves Cognitive Deficits in Preclinical Models.

Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM.

CL 218872 is a selective and orally active benzodiazepine of α1 subunit-containing GABAAreceptor with a Ki of 130 nM. CL 218872 exerts anxiolytic and anticonvulsant in vivo.

17-PA is a selective antagonist of neurosteroid potentiation and direct gating of GABAA receptors.

U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.

DCBS152A is a potent, functionally selectiver negative modulator of GABAA receptor at the modulatory PQ site in some receptor isoforms.

epi-Aszonalenin A is a benzodiazepine fungal metabolite originally isolated from Aspergillus novofumigatus. epi-Aszonalenin A can be used as a psychoactive agent.

TB-21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptor with a Ki of 1.6 nM. TB-21007 enhanced spatial memory in rats.

3α,21-Dihydroxy-5α-pregnan-20-one-d3 (THDOC-d3) is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.

ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity.

Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor.

Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.

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

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.