GABA Receptor Agonist

Picamilon is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.

4-Acetamidobutanoic acid-d3 is the deuterated analog of 4-Acetamidobutanoic acid (HY-101411). 4-Acetamidobutanoic acid (N-acetyl GABA), the main metabolite of GABA, exhibits antioxidant and antibacterial activities.

ZK 93423 is a potent benzodiazepine GABAA receptor agonist with a certain cooling effect on rodents.

α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential.

(R)-4-Amino-3-hydroxybutyric acid ((R)-GABOB) is a 4-aminobutyric acids (GABAB) agonist. (R)-4-Amino-3-hydroxybutyric acid is promising for research of nervous disorders.

Gidazepam is an agonist of GABA receptor channels (GABA RCs).

1-Anthramine (1-aminoanthracene) is a fluorescent general anesthetic. potentiates GABAergic transmission with K_d = 0.1 mM, for binding to the general anesthetic site in horse spleen apoferritin (HSAF). 1-Anthramine fluorescence is enhanced when bound to HSAF. 1-Anthramine potentiates chloride currents elicited by GABA. 1-Anthramine can reversibly inhibit the movement of Xenopus laevis, with an EC₅₀ value of 16 μM.

Loreclezole, an antiepileptic compound, is a selective GABA_A receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.

Tetrahydrodeoxycorticosterone-d₃ is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties.

Piperazine (1,4-Diazacyclohexane) citrate is a gamma-aminobutyric acid (GABA) agonist. Piperazine citrate is a vital building block and is an essential core in numerous marketed agents with diverse pharmacological activities.

CP-409092 hydrochloride is a partial agonist of GABA_A receptor, with anti-anxiety activity.

DAA1106 is a peripheral benzodiazepine receptor (PBR) agonist that is permeable to the blood-brain barrier, but has no affinity for GABAA receptors.

TP003 is a non-selective benzodiazepine site agonist with EC₅₀s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABA_A receptors.

Alphadolone acetate (Alfadolone acetate) is a steroid agent that can suppress or relieve pain, with antinociception.

PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects.

Dihydrohonokiol B (Dihydrohonokiol) is an anxiolytic agent. Dihydrohonokiol B can reduce the neurotoxicity induced by amyloid β protein by stimulating the GABA_C receptor. Dihydrohonokiol B can be used in the research of neurodegenerative diseases such as Alzheimer's disease.

SSD114 hydrochloride is a novel GABA_B receptor positive allosteric modulator.

CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC₅₀ of 1.3 nM. CGS 20625 enhances GABA in Xenopus laevis oocytes . CGS 20625 can be used for the research of pentylenetetrazol-induced seizures and anxiety.

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

SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface.