(+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.

(R)-Baclofen(STX209) is a selective GABAB receptor agonist.

Afloqualone is a agonist of GABA receptor .

Afoxolaner is an isoxazoline that inhibits insect and acarine ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid (GABA), blocking pre and post synaptic transfer of chloride ions across cell membranes.

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

An allosteric GABAA receptor modulator that strongly suppresses GABA-induced chloride currents...

Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant.

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.

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

Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.

CNS 7056 is a new short-acting sedative/anaesthetic that acts on GABAA receptors in the brain.

Emamectin Benzoate works as a chloride channel activator by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods.

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

Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 and 1,600 nM for cockroach and rat receptors, respectively).

Flumazenil(Ro 15-1788) is a benzodiazepine antagonist, non-selective for α1, α2, α3 or α5-containing GABAA receptors.

Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.

Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog.

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.

GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC.

HZ-166 (HZ166) is a GABAA receptor subtype-selective benzodiazepine site ligand with preferential activity at α2- and α3-GABA(A) receptors.

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

LAU159 is a novelα6β3γ2 GABAA receptor inhibitor.