(S)-Padsevonil is the S-enantiomer of Padsevonil).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.

RO-488684 is a benzodiazepine receptor agonist. RO-488684 can be used for research on sleep and conscious sedation.

CGS-17867A (hydrochloride) is a benzodiazepine receptor ligand. CGS-17867A (hydrochloride) has a weak sedative effect and can increase palatable food intake.

Ro 17-1812 is a benzodiazepine receptor partial agonist with anticonvulsant effect.

RP-60503 is an orally active anxiolytic cyclopyrrolone derivative with low sedative potential. RP-60503 binds to the gamma-aminobutyric acidA (GABA)/benzodiazepine receptor with a Ki value of 1.16 nM. RP-60503 can be used for the research of neurological disease.

HDZI 2,4OH exerts significant anti anxiety activity through GABA receptors. HDZI 2,4OH can penetrate the blood-brain barrier. HDZI 2,4OH exhibits low toxicity in zebrafish. HDZI 2,4OH can be used for research on neurological disorders such as anxiety disorders.

AHN 070 is an irreversible peripheral benzodiazepine receptor (PBR) ligand. AHN 070 can bind to PBR with nanomolar affinity and is pH-dependent. AHN 070 can be used for studying the structure and function of PBR.

Aminochalcone 4AAF is a neuroprotective agent that exerts anxiolytic effects through GABAA and 5-HT receptors. Aminochalcone 4AAF has high selectivity for 5-HT3A and 5-HT2C receptors, and stimulates allosteric behavior toward the 5-HT2A receptor. Aminochalcone 4AAF shows hypoglycemic effects and reduces the level of ROS in the liver. Aminochalcone 4AAF delays the clonic stage of the epileptic seizures . Aminochalcone 4AAF can be used in the study of anxiety, hyperglycemia, and seizures.

Lorotomidate (Example 16) is a GABAA receptor agonist. Lorotomidate has anaesthetic effects (ED50: i.v., 2 mg/kg in KM mice; LD50: 46.5 mg/kg in KM mice). Lorotomidate has no inhibitory effect on the secretion of corticosteroids in animals, and thus has good safety.

4''-Oxoavermectin B1a is a potentiator targeting GABA (γ-aminobutyric acid) and glutamate-gated chloride channels with insecticidal and acaricidal activities. 4''-Oxoavermectin B1a is promising for research of agricultural pests.

Cholesteryl γ-aminobutyrate is a γ-aminobutyric acid (GABA)-mimetic prodrug. Cholesteryl γ-aminobutyrate inhibits the orthodromically-evoked discharge of pyramidal cells in the CA1 region of the hippocampus. Cholesteryl γ-aminobutyrate suppresses the open-field activity of mice and rats in a dose-dependent manner and inhibits Bicuculline-induced seizures in mice. Cholesteryl γ-aminobutyrate can be used for the study of CNS diseases related to impaired GABAergic neuronal function.

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.