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

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.

Zuranolone(SAGE-217, CS-2797) is an orally active and potent neuroactive steroid and positive allosteric modulator of the GABAA receptor, with EC50s of 296 nM for α1β2γ2 receptor.

ASP8062 is a potent, selective GABA B receptor positive allosteric modulator (PAM), positive allosteric modulating activity for human and rat GABAB receptors, exerts analgesic effects in rat model of fibromyalgia.

DS-II-73 is a selective α2/3/5-containing GABAA receptor (GABAAR) potentiator with IC50 of 320 nM, 381 nM and 435 nM for α2β3γ2 α3β3γ2 α5β3γ2.

CGP 36742 (SGS-742) is a BBB-penetrant GABAB receptor antagonist, discretely up-regulates GABAB receptor binding sites.

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

Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.