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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15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
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bifenazate

Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm[1]. Bifenazate is a positive allosteric modulator of GABA receptor[2].

  • CAS Number: 149877-41-8
  • MF: C17H20N2O3
  • MW: 300.35
  • Catalog: GABA Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 122℃
  • Flash Point: N/A

Imepitoin

AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.IC50 Value: Target: GABA receptorin vitro: AWD 131-138 dose-dependently stimulated GABA currents(Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted in average to about 12-21% of the maximal stimulation achieved using diazepam. The threshold of stimulation was about 0.3-1.0 microM [1]. in vivo: AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml). When AWD 131-138 (10-100 microg/kg/injection) was studied by substitution, responding declined to vehicle substitution levels within three sessions. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels [2]. Prolonged oral administration with twice-daily dosing of ELB 138 with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ dog model [3].

  • CAS Number: 188116-07-6
  • MF: C13H14ClN3O2
  • MW: 279.722
  • Catalog: GABA Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 421.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 208.9±31.5 °C

Etifoxine-d5

Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].

  • CAS Number: 1346598-10-4
  • MF: C17H12D5ClN2O
  • MW: 305.81
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ocinaplon

Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit[1].

  • CAS Number: 96604-21-6
  • MF: C17H11N5O
  • MW: 301.30200
  • Catalog: GABA Receptor
  • Density: 1.37 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

17β-Estradiol sulfate-d4 sodium

17β-Estradiol sulfate-d4 (sodium) is the deuterium labeled 17β-Estradiol sulfate 17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid[1][2].

  • CAS Number: 352431-50-6
  • MF: C18H19D4NaO5S
  • MW: 378.45
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

broflanilide

Broflanilide is a potential insecticide and metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.

  • CAS Number: 1207727-04-5
  • MF: C25H14BrF11N2O2
  • MW: 663.277
  • Catalog: GABA Receptor
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 467.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 236.8±28.7 °C

NNC 711

NNC-711 (hydrochloride) is a potent and selective inhibitor of GAT-1 ( GABA transporter 1) with an IC50 of 40 nM for hGAT-1. NNC-711 has anticonvulsant and analgesic effect in vivo and exhibits cognition-enhancing activity[1][2][3].

  • CAS Number: 145645-62-1
  • MF: C21H23ClN2O3
  • MW: 386.87200
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: 541.2ºC at 760 mmHg
  • Melting Point: 204 - 206 °C
  • Flash Point: 281.1ºC

NS-11394

NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.IC50 value:Target: GABA A receptor modulatorin vitro: NS11394 is unique in having superior efficacy at GABA(A)-alpha(3) receptors while maintaining low efficacy at GABA(A)-alpha(1) receptors. NS11394 has an excellent pharmacokinetic profile, which correlates with pharmacodynamic endpoints (CNS receptor occupancy), yielding a high level of confidence in deriving in vivo conclusions anchored to an in vitro selectivity profile and allowing for translation to higher species [2]. in vivo: Oral administration of NS11394 (1-30 mg/kg) to rats attenuated spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin, effects that were blocked by the benzodiazepine site antagonist flumazenil [1]. NS11394 impairs memory in both rats and mice, which is possibly attributable to its efficacy at GABA(A)-alpha(5) receptors, albeit activity at this receptor might be relevant to its antinociceptive effects [2].

  • CAS Number: 951650-22-9
  • MF: C23H19N3O
  • MW: 353.417
  • Catalog: GABA Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 623.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 331.0±34.3 °C

L-655,708

L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki = 0.45 nM).IC50: 0.45 nM (Ki)Target: GABAin vitro: L-655708 is a potent, selective inverse agonist for the benzodiazepine site of GABAA receptors containing the α5 subunit (Ki = 0.45 nM). Displays 50-100-fold selectivity over GABAA receptors containing α1, α2, α3 orα6 subunits in combination with β3 and γ2. Enhances LTP in a mouse hippocampal slice model and increases spatial learning, without displaying proconvulsant activity.in vivo: L-655708 at 0.7 mg/kg, administered intraperitoneally, would result in 60-70% occupancy of α5 GABAA receptors with limited binding to α1, α2, and α3 subunit-containing GABAA receptors and no significant off-target behavioral effects, such as sedation and motor impairment.[1]

  • CAS Number: 130477-52-0
  • MF: C18H19N3O4
  • MW: 341.36100
  • Catalog: GABA Receptor
  • Density: 1.42g/cm3
  • Boiling Point: 584.4ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 307.2ºC

Aminooxyacetic acid hemihydrochloride

Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.

  • CAS Number: 2921-14-4
  • MF: NH2OCH2COOH·0.5HCl
  • MW: 109.30
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: 326.7ºC at 760 mmHg
  • Melting Point: 156 °C (dec.)(lit.)
  • Flash Point: 151.4ºC

Etifoxine

Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. IC50 value:Target: GABAA receptorEtifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration.

  • CAS Number: 21715-46-8
  • MF: C17H17ClN2O
  • MW: 300.783
  • Catalog: GABA Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 421.2±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 208.5±31.5 °C

CGP 7930

CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons[1].

  • CAS Number: 57717-80-3
  • MF: C19H32O2
  • MW: 292.45600
  • Catalog: GABA Receptor
  • Density: 0.971g/cm3
  • Boiling Point: 364.7ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 152.6ºC

U-89843A

U-89843A is an allosteric modulator of GABAA receptor. U-89843A enhances GABA-induced Cl- currents[1].

  • CAS Number: 157013-85-9
  • MF: C16H24ClN5
  • MW: 321.85
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tiagabine hydrochloride hydrate

Tiagabine hydrochloride hydrate is a potent and selective GABA uptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively[1].

  • CAS Number: 145821-57-4
  • MF: C20H28ClNO3S2
  • MW: 430.02
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ginkgolide A

Ginkgolide A is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist.Target: GABA ReceptorGinkgolide A is a highly active PAF antagonist cage molecule that is isolated from the leaves of the Ginkgo biloba tree. Shows potential in a wide variety of inflammatory and immunological disorders. Ginkgolide A significantly shortened the sleeping time induced by anesthetics in mice [1]. Ginkgolide A failed to affect apoptotic damage neither in serum-deprived nor in staurosporine-treated neurons [2].

  • CAS Number: 15291-75-5
  • MF: C20H24O9
  • MW: 408.399
  • Catalog: GABA Receptor
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 710.1±60.0 °C at 760 mmHg
  • Melting Point: 280°C (dec.)
  • Flash Point: 256.5±26.4 °C

Flumazenil

Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

  • CAS Number: 78755-81-4
  • MF: C15H14FN3O3
  • MW: 303.288
  • Catalog: GABA Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 528.0±50.0 °C at 760 mmHg
  • Melting Point: 201-203°C
  • Flash Point: 273.1±30.1 °C

DPNI-caged-GABA

DPNI-GABA is a nitroindoline cage compound that inhibits GABA(A) receptors and reduces GABA-evoked peak responses with an IC50 value of 0.5 mM[1].

  • CAS Number: 927866-58-8
  • MF: C15H23N3O12P2
  • MW: 499.30
  • Catalog: GABA Receptor
  • Density: 1.676±0.06 g/cm3 (20 °C, 760 mmHg)
  • Boiling Point: 900.8±75.0 °C (760 mmHg)
  • Melting Point: N/A
  • Flash Point: N/A

Tigolaner

Tigolaner is a GABA antagonist that regulates chloride channel. Tigolaner is an antiparasitic agent[1].

  • CAS Number: 1621436-41-6
  • MF: C21H13ClF8N6O
  • MW: 552.81
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HZ-166

HZ-166 (HZ166) is a GABAA receptor subtype-selective benzodiazepine site ligand with preferential activity at α2- and α3-GABA(A) receptors; displays a statistically significant higher affinity for receptors not containing the α1 subunit with a rank order of α5 (Ki=140nM) > α2 (Ki=269 nM) > α1 (Ki=382 nM); The Ki value of HZ166 for the α3β3γ2 combination (185± 47 nM) was statistically significantly lower than the Ki value observed for α1β3γ2 but not different from those of α2β3γ2 and α5β3γ2; HZ-166 is antihyperalgesic in mouse models of inflammatory and neuropathic pain.

  • CAS Number: 612527-56-7
  • MF: C21H16N4O2
  • MW: 356.385
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tiagabine hydrochloride

Tiagabine hydrochloride(NO328 hydrochloride) is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.Target: GABA reuptake inhibitorTiagabine had an early onset of effect, as shown by significant reduction from baseline in mean HAM-A total score compared with placebo at week 1 (observed cases, p < .05). Tiagabine was generally well tolerated and not associated with changes in sexual functioning or depressive status. Symptoms of a discontinuation syndrome during taper were not observed. Tiagabine may be a useful treatment option for adult patients diagnosed with GAD [1]. Tiagabine was generally well tolerated; the most common adverse events were nausea, dizziness and headaches [2]. Tiagabine (0.1 microM), an antiepileptic drug that specifically inhibits the GAT-1 GABA transporter inhibited GABA uptake 50% in temporal cortex and 60-68% in white structures [3].

  • CAS Number: 145821-59-6
  • MF: C20H26ClNO2S2
  • MW: 412.009
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: 568ºC at 760 mmHg
  • Melting Point: >192oC dec.
  • Flash Point: 297.3ºC

Afoxolaner

Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod[1][2].

  • CAS Number: 1093861-60-9
  • MF: C26H17ClF9N3O3
  • MW: 625.87000
  • Catalog: Chloride Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

mGAT3/4-IN-1

mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice[1].

  • CAS Number: 2556833-57-7
  • MF: C26H31ClN2O2S2
  • MW: 503.12
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Procaine hydrochloride

Procaine Hydrochloride is a local anesthetic drug of the amino ester group.Target: OthersProcaine is a local anesthetic of the ester type that has a slow onset and a short duration of action.Procaine (0.01-100 microM) inhibited the 5-HT3 receptor-mediated inward current in the whole-cell patch clamp recording. Procaine appears to produce a competitive inhibition on 5-HT3 receptors with a KD of 1.7 microM [1]. Procaine is a DNA-demethylating agent that produces a 40% reduction in 5-methylcytosine DNA content as determined by high-performance capillary electrophoresis or total DNA enzyme digestion. Procaine can also demethylate densely hypermethylated CpG islands. Procaine also has growth-inhibitory effects in these cancer cells, causing mitotic arrest [2]. Procaine functions as an excitant of limbic system cells, and that procaine alters synaptic transmission in some, but not all, output pathways from the amygdale [3].

  • CAS Number: 51-05-8
  • MF: C13H21ClN2O2
  • MW: 272.771
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: 195-196°C 17mm
  • Melting Point: 155-156 °C(lit.)
  • Flash Point: 195-196°C/17mm

Valnoctamide

Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors[1].

  • CAS Number: 4171-13-5
  • MF: C8H17NO
  • MW: 143.22700
  • Catalog: GABA Receptor
  • Density: 0.883g/cm3
  • Boiling Point: 274.4ºC at 760mmHg
  • Melting Point: 113.5-114ºC
  • Flash Point: 119.8ºC

γ-Acetylenic GABA hydrochloride

γ-Acetylenic GABA hydrochloride is a GABA transaminase inhibitor.

  • CAS Number: 103451-26-9
  • MF: C6H10ClNO2
  • MW: 163.6
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bgt1-in-9

BGT1-IN-9 is an M1 muscarinic agonist.

  • CAS Number: 185444-92-2
  • MF: C5H10ClN3O2
  • MW: 179.605
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PF-06372865

PF-06372865 is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator; exhibits functional selectivity for receptors containing α2/3/5 subunits, with significant positive allosteric modulation (90-140%) but negligible activity (<20%) at GABAA receptors containing α1 subunits; demonstrates a robust increase in saccadic peak velocity, increases in beta frequency qEEG and a slight saturating increase in body sway in clinical trials. Epilepsy Phase 1 Clinical

  • CAS Number: 1614245-70-3
  • MF: C22H21FN4O3S
  • MW: 440.493
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Oxiracetam

Oxiracetam is a cyclic derivative of γ-aminobutyric acid (GABA) which has been commonly used as nootropic drug to treat cognitive impairments.

  • CAS Number: 62613-82-5
  • MF: C6H10N2O3
  • MW: 158.155
  • Catalog: GABA Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 494.6±40.0 °C at 760 mmHg
  • Melting Point: 165-168ºC
  • Flash Point: 252.9±27.3 °C

Rilmazafone

Rilmazafone is a benzodiazepine (omega) ligand with sedative and hypnotic effects[1].

  • CAS Number: 99593-25-6
  • MF: C21H20Cl2N6O3
  • MW: 475.33
  • Catalog: GABA Receptor
  • Density: 1.45g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S)-Cipepofol

(S)-Cipepofol is the inactive isomer of Cipepofol (HY-116152).Cipepofol (HSK3486) is a sleep-promoting active molecule and a gamma-aminobutyric acid (GABA) receptor enhancer[1].

  • CAS Number: 1637741-59-3
  • MF: C14H20O
  • MW: 204.31
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A