β-CCM is a benzodiazepine receptor inverse agonist with anxiogenic and proconvulsant effects. β-CCM enhances emotional reactivity and reduces vulnerability to interference in spatial working memory tasks. β-CCM can be used for research on anxiety-related disorders.

TET-13 is a positive allosteric modulator of GABAA receptor with an EC50 of 5.65 μM, lower than that of Etomidate (EC50: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED50: 0.48 mg/kg and 0.69 mg/kg, respectively).

SKF 10810 is a GABAA receptor antagonist with an EC50 of 4.3 μM. By blocking GABAergic inhibition of the brain's reward pathways, SKF 10810 may exert antidepressant effects. SKF 10810 can be used for research in neurological disorders.

Rilmazolam, a triazolobenzodiazepine, is an active metabolite of Rilmazafone. NSC687852 (b-AP1

Refisolone is an antagonist of the GABAA receptor.

Moxetomidate is a GABAA receptor agonist with hypnotic effect.

MIDD0301 (GL-II-93) is an orally available, active γ-aminobutyric acid type A receptor (GABAAR) inhibitor and anti-asthmatic agent. MIDD0301 exhibits biological and immunotoxicological safety in mice and does not affect the number of circulating lymphocytes, monocytes, and granulocytes. MIDD0301 has no significant adverse immune response at repeated doses, which is better than Prednisone. MIDD0301 relaxes histamine-contracted guinea pig and human airway smooth muscle and is used in the study of bronchoconstrictive diseases.

Inidascamine is the modulator for cholinergic, glutamatergic, and GABAB receptor, and can be used for researchs of schizophrenia.

ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models.

Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.

CMPPE is a GABAB receptor positive allosteric modulator (PAM) that inhibits alcohol self-administration and reinstatement behavior in rats.

Cinazepam is a partial GABAA receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders.

Ciclotizolam (WE-973) is a thienotriazolodiazepine with anticonvulsant and anti-aggressive activities. Ciclotizolam binds to benzodiazepine receptors in the central nervous system. Ciclotizolam decreases total sleep time in cats.

3-Hydroxy desalkylflurazepam is a benzodiazepine with potential sedative and anxiolytic effects.

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.

Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).

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.

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.

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

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.

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.

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

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.

Tetramethylglycerol (Tetramethylglycoluril) is a small molecule that acts on GABA Receptor, with anti-anxiety activity.

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

Cipepofol (HSK3486), a sedative-hypnotic agent, is a gamma-aminobutyric acid (GABA) receptor potentiator.

Tiagabine(NO328) is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.

Saclofen is a selective GABAB antagonist.

Rac BHFF is a potent and selective GABAB receptor positive allosteric modulator that increases the efficacy and potency of GABA ( > 149% and > 15-fold respectively). Orally active and exhibits anxiolytic activity in vivo.

Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.