GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties.


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(-)-Bicuculline methobromide

(-)-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].

  • CAS Number: 73604-30-5
  • MF: C21H20BrNO6
  • MW: 462.29100
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-METHYLGLUTACONIC ACID

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].

  • CAS Number: 5746-90-7
  • MF: C6H8O4
  • MW: 144.13
  • Catalog: GABA Receptor
  • Density: 1.307g/cm3
  • Boiling Point: 399.4ºC at 760mmHg
  • Melting Point: 101 - 105°C (lit.)
  • Flash Point: 209.5ºC

gaboxadol

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].

  • CAS Number: 64603-91-4
  • MF: C6H9ClN2O2
  • MW: 140.140
  • Catalog: GABA Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 340.5±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 159.7±27.9 °C

Cipepofol

Cipepofol (HSK3486), a sedative-hypnotic agent, is a gamma-aminobutyric acid (GABA) receptor potentiator[1].

  • CAS Number: 1637741-58-2
  • MF: C14H20O
  • MW: 204.31
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TPA 023

TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.

  • CAS Number: 252977-51-8
  • MF: C20H22FN7O
  • MW: 395.43300
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Oxopyrrolidine-2-carboxylic acid

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].

  • CAS Number: 149-87-1
  • MF: C5H7NO3
  • MW: 129.114
  • Catalog: Influenza Virus
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 453.1±38.0 °C at 760 mmHg
  • Melting Point: 180-185ºC
  • Flash Point: 227.8±26.8 °C

CGP 52432

CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.

  • CAS Number: 139667-74-6
  • MF: C15H24Cl2NO4P
  • MW: 384.23500
  • Catalog: GABA Receptor
  • Density: 1.258g/cm3
  • Boiling Point: 544.4ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 283.1ºC

GABAA receptor agent 8

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].

  • CAS Number: 2376841-54-0
  • MF: C19H16N4O
  • MW: 316.36
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-Ethyl-2,6,7-trioxa-1-phosphabicyclo[2.2.2]octane 1-oxide

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].

  • CAS Number: 1005-93-2
  • MF: C6H11O4P
  • MW: 178.123
  • Catalog: GABA Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 213.1±7.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 96.9±38.5 °C

Anisatin

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].

  • CAS Number: 5230-87-5
  • MF: C15H20O8
  • MW: 328.31500
  • Catalog: GABA Receptor
  • Density: 1.149g/cm3
  • Boiling Point: 251.2ºC at 760 mmHg
  • Melting Point: 227-228ºC
  • Flash Point: 106.7ºC

Etomidate

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.

  • CAS Number: 33125-97-2
  • MF: C14H16N2O2
  • MW: 244.289
  • Catalog: GABA Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 391.5±17.0 °C at 760 mmHg
  • Melting Point: 72-74ºC
  • Flash Point: 190.6±20.9 °C

DS2

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].

  • CAS Number: 374084-31-8
  • MF: C18H12ClN3OS
  • MW: 353.82500
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(-)-BICUCULLINE METHBROMIDE

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].

  • CAS Number: 66016-70-4
  • MF: C21H20BrNO6
  • MW: 462.29100
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dimdazenil

Dimdazenil (EVT-201) is a GABAA receptor partial positive allosteric modulator (PAM). Dimdazenil can be used in the research of insomnia[1].

  • CAS Number: 308239-86-3
  • MF: C17H17ClN6O2
  • MW: 372.81
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lorediplon

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]

  • CAS Number: 917393-39-6
  • MF: C20H15FN4O2S
  • MW: 394.42200
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5alpha-Pregnan-3alpha-ol-20-one

Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor.

  • CAS Number: 516-54-1
  • MF: C21H34O2
  • MW: 318.493
  • Catalog: GABA Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 431.2±18.0 °C at 760 mmHg
  • Melting Point: 176-178°
  • Flash Point: 183.9±13.8 °C

D-(2H3)Methionine

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.

  • CAS Number: 284665-18-5
  • MF: C5H8D3NO2S
  • MW: 152.23
  • Catalog: GABA Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 306.9±37.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 139.4±26.5 °C

Pipequaline hydrochloride

Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity[1][2].

  • CAS Number: 80221-58-5
  • MF: C22H25ClN2
  • MW: 352.90
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: 489.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 249.7ºC

CGP 64213

CGP 64213 is a GABAb receptor agonist.

  • CAS Number: 200402-50-2
  • MF: C26H36IN2O7P
  • MW: 646.45
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Picrotoxinin

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].

  • CAS Number: 17617-45-7
  • MF: C15H16O6
  • MW: 292.28400
  • Catalog: Chloride Channel
  • Density: 1.52g/cm3
  • Boiling Point: 551.6ºC at 760mmHg
  • Melting Point: 203-205ºC
  • Flash Point: 214ºC

MIDD0301

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.

  • CAS Number: 2187489-08-1
  • MF: C19H13BrFN3O2
  • MW: 414.234
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Arachidonoyl-γ-aminobutyric acid

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].

  • CAS Number: 128201-89-8
  • MF: C24H39NO3
  • MW: 389.571
  • Catalog: GABA Receptor
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 580.8±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 305.1±30.1 °C

SAGE-217

SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.

  • CAS Number: 1632051-40-1
  • MF: C25H35N3O2
  • MW: 409.56
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GABAA receptor agent 4

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].

  • CAS Number: 2035203-91-7
  • MF: C17H24N2O
  • MW: 272.39
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Isonipecotic acid-d9

Isonipecotic acid-d9 is the deuterium labeled Isonipecotic acid[1]. Isonipecotic acid is a GABAA receptor partial agonist[2].

  • CAS Number: 1219798-43-2
  • MF: C6H2D9NO2
  • MW: 138.21
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

mGAT-IN-1

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].

  • CAS Number: 2556833-08-8
  • MF: C28H34ClN3O2S2
  • MW: 544.17
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-hydroxysaclofen

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].

  • CAS Number: 117354-64-0
  • MF: C9H12ClNO4S
  • MW: 265.71400
  • Catalog: GABA Receptor
  • Density: 1.551 g/cm3
  • Boiling Point: N/A
  • Melting Point: 267-269ºC
  • Flash Point: N/A

Temgicoluril

Tetramethylglycerol (Tetramethylglycoluril) is a small molecule that acts on GABA Receptor, with anti-anxiety activity[1].

  • CAS Number: 10095-06-4
  • MF: C8H14N4O2
  • MW: 198.22
  • Catalog: GABA Receptor
  • Density: 1.237g/cm3
  • Boiling Point: 362.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 171.9ºC

CGP 36216

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].

  • CAS Number: 123691-29-2
  • MF: C5H14NO2P
  • MW: 151.14
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Phenylpyrrolidone

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].

  • CAS Number: 4641-57-0
  • MF: C10H11NO
  • MW: 161.20
  • Catalog: GABA Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 355.5±11.0 °C at 760 mmHg
  • Melting Point: 67-69 °C(lit.)
  • Flash Point: 174.7±10.5 °C