(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca2+-activated K+ channels in various types of neurons[1].
3-Methylglutaconic acid is the major metabolites accumulating in 3-Methylglutaconic aciduria (MGTA). 3-Methylglutaconic acid can induce lipid oxidative damage and protein oxidative. 3-Methylglutaconic acid decreases the non-enzymatic antioxidant defenses in cerebral cortex supernatants to elicit oxidative stress in the cerebral cortex. 3-Methylglutaconic acid can be used for brain damage disease research[1].
THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs[1].
Cipepofol (HSK3486), a sedative-hypnotic agent, is a gamma-aminobutyric acid (GABA) receptor potentiator[1].
TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.
DL-Pyroglutamic acid (CAE) as an inactivator of hepatitis B surface, inactivates vaccinia virus, herpes simplex virus, and influenza virus except poliovirus. DL-Pyroglutamic acid is also a possible inhibitor of GABA transaminase, increases GABA amount with antiepileptic action[1][2].
CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy[1].
Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1].
Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM[1].
Etomidate(R-16659) is a GABAA receptors agonist, which is a short acting intravenous anaesthetic agent used for the induction of general anaesthesia.Target: GABA ReceptorEtomidate is a potent inhibitor of the adrenal response to surgery. The absence of clinical consequences associated with the blunted response suggests that a major increase in adrenal hormone production may not be necessary during surgery [1]. Etomidate is an intravenous induction agent that is associated with hemodynamic stability during intubation. The agent is therefore attractive for use in critically ill patients who have a high risk of hemodynamic instability during this procedure [2]. Etomidate use was not associated with all cause 28-day mortality or hospital mortality but was associated with significantly higher ICU mortality (91% vs. 64% for etomidate and controls groups, respectively; p = 0.02). Etomidate patients who received subsequent doses of hydrocortisone required lower doses of vasopressors and had more vasopressor-free days but no improvement in mortality [3].Clinical indications: FDA Approved Date: 1983Toxicity: Undesirable side effects of etomidate that may limit its use include pain on injection, myoclonus and adrenocortical suppression lasting 4-6 hours following an induction dose.
DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research[1].
Bicuculline methobromide is a selective GABAA receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders[1][2].
Dimdazenil (EVT-201) is a GABAA receptor partial positive allosteric modulator (PAM). Dimdazenil can be used in the research of insomnia[1].
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.Target: GABALorediplon is a drug for the treatment of insomnia, has been successfully completed with a best-in-class efficacy profile in terms of maintaining sleep and sleep quality, Lorediplon targets GABAA. [1] Lorediplon demonstrates a minimum of 10-fold and 6-fold increase in potency (respectively) in the spontaneous motor activation studies. At concentrations of 1.2mg/kg, Lorediplon demonstrates a 57%increased effect on Slow Wave Sleep (SWS), when compared with a placebo.[2]
Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor.
Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity[1][2].
CGP 64213 is a GABAb receptor agonist.
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors[1].
MIDD0301 is a potent, positive allosteric, α5β3γ2 selective, GABAA receptor (GABAAR) ligand with EC50 of 17 nM, shows no significant binding at the peripheral GABAAR at 10 uM; causes amplification of GABA induced current mediated by α1-3,5β3γ2 GABAARs in the presence of MIDD0301 in automated patch clamp test; relaxes airway smooth muscle at single micromolar concentrations as demonstrated with ex vivo guinea pig tracheal rings, also attenuates airway hyperresponsiveness (AHR) in an ovalbumin murine model of asthma by oral administration, with low brain distribution; reduces lung cytokine expression of IL-17A, IL-4, and TNF-α, as wells as the number of CD4+ T cells.
N-Arachidonoyl-GABA is one member of a new class of lipoamino acids related to anandamide identified in bovine brain. N-Arachidonoyl-GABA displays analgesic activity[1].
SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an Ki of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential[1].
Isonipecotic acid-d9 is the deuterium labeled Isonipecotic acid[1]. Isonipecotic acid is a GABAA receptor partial agonist[2].
mGAT-IN-1 (compound 28) is a potent and non-selective GAT inhibitor. mGAT-IN-1 has a high inhibitory potency toward mGAT3, with an IC50 of 2.5 μM and pIC50 of 5.61[1].
2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats[1][2][3].
Tetramethylglycerol (Tetramethylglycoluril) is a small molecule that acts on GABA Receptor, with anti-anxiety activity[1].
CGP36216 (Compound 9) is a GABAB receptor antagonist. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 can be used for research of anxiety and trauma-related disorders[1][2].
1-Phenyl-2-pyrrolidinone (1-Phenylpyrrolidin-2-one) is a phenyl analogue of GABA with sedative effect, decreasing the exploratory behavior of rats at 50-100 mg/kg (i.v.). 1-Phenyl-2-pyrrolidinone also has been proved to inhibit emotional reactions in dogs and cats. 1-Phenyl-2-pyrrolidinone induces decreases in the pressor reaction to emotional stress without accompanied by normalization of the function of baroreceptor reflexes[1][2].