GABA Receptor - file.medchemexpress.com · GABA Receptor Gamma-aminobutyric acid...

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www.MedChemExpress.com 1 GABA Receptor Gamma-aminobutyric acid Receptor;γ-Aminobutyric acid Receptor 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.

Transcript of GABA Receptor - file.medchemexpress.com · GABA Receptor Gamma-aminobutyric acid...

Page 1: GABA Receptor - file.medchemexpress.com · GABA Receptor Gamma-aminobutyric acid Receptor;γ-Aminobutyric acid Receptor GABA receptors are a class of receptors that respond to the

www.MedChemExpress.com 1

GABA ReceptorGamma-aminobutyric acid Receptor;γ-Aminobutyric acid Receptor

GABA receptors are a class of receptors that respond to theneurotransmitter gamma-aminobutyric acid (GABA), the chiefinhibitory neurotransmitter in the vertebrate central nervous system.There are two classes of GABA receptors: GABAA and GABAB. GABAAreceptors are ligand-gated ion channels (also known as ionotropicreceptors), whereas GABAB receptors are G protein-coupled receptors(also known asmetabotropic receptors). It has long been recognizedthat the fast response of neurons to GABA that is blocked bybicuculline and picrotoxin is due to direct activation of an anionchannel. 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 basisof pharmacological properties.

Page 2: GABA Receptor - file.medchemexpress.com · GABA Receptor Gamma-aminobutyric acid Receptor;γ-Aminobutyric acid Receptor GABA receptors are a class of receptors that respond to the

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

200 mg

Purity: 99.22%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

100 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg

Purity: >98%Clinical Data: Phase 3Size: 10 mg, 50 mg

Purity: 98.0%Clinical Data: Phase 3Size: 10mM x 1mL in Water,

10 mg, 50 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

100 mg

Purity: 99.98%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

100 mg

Purity: 99.97%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

50 mg, 100 mg, 250 mg

GABA Receptor Inhibitors & Modulators

Bioactivity: (+)-Bicuculline is a light-sensitive competitive antagonist of.GABA-A receptor

Bioactivity: (+)-Borneol (d-Borneol) is a natural bicyclic monoterpene usedfor analgesia and anesthesia in traditional Chinese medicine;enhances activity with an of 248 μM.GABA receptor EC50

Bioactivity: (+)-Kavain, a main kavalactone extracted from Piper, has anticonvulsive properties, attenuatingmethysticum

vascular smooth muscle contraction through interactions withvoltage-dependent Na and Ca channels . (+)-Kav…+ 2+ [1]

Bioactivity: (-)-Borneol has a highly efficacious positive modulatingaction at receptor with an of 237 μM.GABA EC50

Bioactivity: (-)-Securinine is plant-derived alkaloid and also a GABAA antagonist.receptor

Bioactivity: (R)-Baclofen(STX209) is a selective GABAB receptor agonist.IC50 value: Target: GABAB receptor GABAB receptors aremetabotropic receptors which produce slow inhibitory signals.By manipulating GABAB receptor activity using Baclofen, avariety of functions are studied including synaptic…

Bioactivity: (R)-Baclofen Hcl(STX-209 Hcl) is a derivative ofgamma-aminobutyric acid (GABA) primarily used to treatspasticity and is in the early research stages for use for thetreatment of alcoholism. Target: GABA Baclofen (brand namesKemstro, Lioresal, Liofen, Gablofen, Beklo and Baclosan) is a…

Bioactivity: (S)-SNAP5114 is a selective inhibitor, withGABA transport values of 5 μM and 21 μM for hGAT-3 and rGAT-2,IC50

respectively. (S)-SNAP5114 is an anticonvulsant drug [1]

.[2]

Bioactivity: 3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolatedfrom the roots of WILLD, with anti-stressPolygala tenuifoliaeffect, prolonging the sleeping time in animals .[1] [2]

3,4,5-Trimethoxycinnamic acid increases expression of GAD65and , but shows no effect on the…γ-subunit of GABAA receptor

Bioactivity: 4-Acetamidobutanoic acid (N-acetyl GABA) is a γ-aminobutyricacid ( ) derivative.GABA

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

(+)-Bicuculline (d-Bicuculline) Cat. No.: HY-N0219

(+)-Borneol (d-Borneol) Cat. No.: HY-N1368A

(+)-Kavain  Cat. No.: HY-B1671

(-)-Borneol (L-Borneol) Cat. No.: HY-N1368B

(-)-Securinine  Cat. No.: HY-N2079

(R)-Baclofen (STX209) Cat. No.: HY-17354

(R)-Baclofen hydrochloride (STX 209 hydrochloride) Cat. No.: HY-17354A

(S)-SNAP5114  Cat. No.: HY-103504

3,4,5-Trimethoxycinnamic acid  Cat. No.: HY-W012123

4-Acetamidobutanoic acid (N-acetyl GABA) Cat. No.: HY-101411

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Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg

Purity: 98.21%Clinical Data: LaunchedSize: 1 g, 5 g

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

1 g

Purity: 99.99%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

1 g, 5 g

Purity: 98.0%Clinical Data: Phase 3Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: 98.0%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

100 mg

Purity: 98.0%Clinical Data: LaunchedSize: 10mM x 1mL in Water,

50 mg

Purity: 99.85%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

100 mg

Purity: 99.10%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

50 mg

 

Bioactivity: 6,2'-Dihydroxyflavone is a novel antagonist of GABAA.receptor

Bioactivity: 6-methylflavone is an activator of α β γ and α β 1 2 2L 1 2 receptors.GABAA

Bioactivity: Acamprosate calcium(Campral EC) is a GABA receptor agonist andmodulator of glutamatergic systems; reduces alcoholconsumption in animal models of alcohol addiction. IC50 value:Target: GABA receptor Acamprosate, or N-acetyl homotaurine, isan N-methyl-D-aspartate receptor modulator approved by the…

Bioactivity: Afloqualone is a agonist of GABA receptor .

Bioactivity: Allopregnanolone is a progesterone metabolite.Allopregnanolone is an allosteric modulator of the GABAreceptor. Used to treat postpartum depression.

Bioactivity: Alpha-Asarone is one of the main psychoactive compounds, andpossesses an antidepressant-like activity in mice.

Bioactivity: Aminooxyacetic acid hemihydrochloride is a malate-aspartate ( ) inhibitor which also inhibits the GABAshuttle MAS

degradating enzyme .GABA-T

Bioactivity: AZD-6280 is a selective modulator, usedGABAA(α2/3) receptorfor treatment of generalized anxiety disorder.

Bioactivity: Baclofen is a gamma-amino-butyric acid (GABA) derivative usedas a skeletal muscle relaxant. Target: GABA Receptor Baclofen,a lipophilic analog of gamma-aminobutyric acid, is clinicallyused to control spasticity. Baclofen pretreatment (3 mg/kg)not only prolonged the time taken for animals to reach a core…

Bioactivity: Bamaluzole is a agonist extracted from patentGABA receptorWO 2012064642 A1.

6,2'-Dihydroxyflavone  Cat. No.: HY-N6628

6-Methylflavone  Cat. No.: HY-N6630

Acamprosate calcium (Calcium N-acetylhomotaurinate) Cat. No.: HY-17030

Afloqualone  Cat. No.: HY-B1833

Allopregnanolone (3α,5α-THP; SAGE-547; Brexanolone) Cat. No.: HY-101107

alpha-Asarone (α-Asarone; trans-Asarone) Cat. No.: HY-N0700

Aminooxyacetic acid hemihydrochloride (Carboxymethoxylamine Hemihydrochloride) Cat. No.: HY-107994

AZD-6280  Cat. No.: HY-19872

Baclofen  Cat. No.: HY-B0007

Bamaluzole  Cat. No.: HY-100124

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Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 250 mg

Purity: 99.85%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

100 mg

Purity: 98.50%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: >98%Clinical Data: No Development ReportedSize: 250 mg, 500 mg

Purity: 99.91%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

100 mg, 500 mg, 1 g

Purity: 99.91%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

100 mg, 500 mg

Purity: 99.49%Clinical Data: Phase 2Size: 10mM x 1mL in DMSO,

1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

 

Bioactivity: Basmisanil is a highly selective negative allostericGABAAα5modulator.

Bioactivity: Bemegride is a central nervous system stimulant and antidotefor barbiturate poisoning.

Bioactivity: Bifenazate is a carbazate acaricide that control 100% of mitesat a concentration of 25 ppm . Bifenazate is a positive[1]

allosteric modulator of .GABA receptor [2]

Bioactivity: Broflanilide is a potential insecticide and metabolized todesmethyl-broflanilide, which is a potent antagonist at theinsect resistant-to-dieldrin (RDL) , andGABA receptorinhibits RDL GABAR, with an value of 1.3 nM.S. litura IC50

Bioactivity: Carburazepam is a drug which derives from benzodiazepine.Benzodiazepines (BZD, BZs) are a class of psychoactive drugswhose core chemical structure is the fusion of a benzene ringand a diazepine ring.

Bioactivity: CGP11952 is a triazolyl-Benzaphenon resembling thebenzodiazepines in its pharmacological action. CGP11952 is anexperimental derivative.benzodiazepine

Bioactivity: CGP52432 is a antagonist, with an of 85GABA receptorB IC50nM.

Bioactivity: Chlormezanone resembles . The action ofbenzodiazepineChlormezanone is similar to benzodiazepine-type agents.Chlormezanone is used as an anxiolytic and a muscle relaxant.

Bioactivity: Cholesterol myristate is a natural steroid present intraditional Chinese medicine. Cholesterol myristate binds toseveral ion channels such as the nicotinic acetylcholine

, , and the inward-rectifierreceptor GABAA receptor.potassium ion channel

Bioactivity: Cirsimaritin binds weakly to the benzodiazepine site on receptors, with antidepressant, anxiolytic andGABAA

antinociceptive activities.

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Basmisanil (RG1662; RO5186582) Cat. No.: HY-16716

Bemegride (3-Ethyl-3-methylglutarimide; Bemegrid) Cat. No.: HY-B1326

Bifenazate  Cat. No.: HY-119687

Broflanilide  Cat. No.: HY-108689

Carburazepam (RGH 3331; Uxepam) Cat. No.: HY-U00241

CGP11952  Cat. No.: HY-U00192

CGP52432  Cat. No.: HY-103531

Chlormezanone  Cat. No.: HY-B0353

Cholesterol myristate (Cholesteryl myristate; Cholesteryl tetradecanoate) Cat. No.: HY-N2338

Cirsimaritin  Cat. No.: HY-N6648

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Purity: 99.33%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Purity: 99.96%Clinical Data: Phase 3Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: 99.94%Clinical Data: Phase 3Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: 94.77%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

100 mg, 500 mg

Purity: 98.14%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

1 g, 5 g

Purity: 98.0%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

100 mg

Purity: 99.96%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

2 mg, 5 mg, 10 mg, 25 mg, 50 mg

Purity: >98%Clinical Data: No Development ReportedSize: 500 mg, 250 mg, 100 mg

 

Bioactivity: CP-409092 is a partial agonist, used for theGABA(A)treatment of anxiety.

Bioactivity: DAA1106 is a potent and selective ligand for peripheralbenzodiazepine receptor (PBR), as a potent and selectiveagonist at the peripheral benzodiazepine receptor. Target:PBRin vitro: DAA1106 binding to PBR was significantly increasedin widespread areas in MCI subjects when compared to healthy…

Bioactivity: Dihydroergotoxine mesylate is a complex of closely relatedalkaloid salts; Binds with high affinity to the GABAA receptorCl- channel, producing an allosteric interaction with thebenzodiazepine site. IC50 value: Target: Dihydroergotoxinemesylate also interacts with central dopaminergic,…

Bioactivity: DL-Borneol is a racemic mixture of D-Borneol and L-Borneol.DL-Borneol is widely used for the treatment of cardiovascularand cerebrovascular diseases in China.

Bioactivity: DMCM (hydrochloride) is Benzodiazepine inverse agonist thatdisplays anxiogenic and potent convulsant activity. Thereference for administration is ranging 0.4 from 0.8 mg/kg .DMCM (hydrochloride) was shown to bind toGABAA/benzodiazepinereceptors in the rat brain with high affinity. DMCM…

Bioactivity: Emamectin Benzoate (MK-244) works as a chloride channelactivator by binding gamma aminobutyric acid (GABA) receptorand glutamate-gated chloride channels disrupting nerve signalswithin arthropods.

Bioactivity: Ethyl dirazepate is a drug which is a benzodiazepinederivative. It has anxiolytic and hypnotic and possibly othercharacteristic benzodiazepine properties.

Bioactivity: Etifoxine(HOE 36-801) is potentiator of GABAA receptorfunction in cultured neurons. Etifoxine preferentially acts onβ2 or β3 subunit-containing GABAA receptors.

Bioactivity: Etifoxine hydrochloride (HOE 36-801 hydrochlorid) ispotentiator of GABAA receptor function in cultured neurons.Etifoxine preferentially acts on β2 or β3 subunit-containingGABAA receptors. IC50 value: Target: GABAA receptor Etifoxineexhibits anxiolytic activity in rodents and humans with no…

Bioactivity: Etomidate(R-16659) is a GABAA receptors agonist, which is ashort acting intravenous anaesthetic agent used for theinduction of general anaesthesia.

CP-409092  Cat. No.: HY-101639

DAA-1106  Cat. No.: HY-19945

Dihydroergotoxine mesylate (Ergoloid mesylates) Cat. No.: HY-B0799

DL-Borneol ((±)-Borneol) Cat. No.: HY-N1368

DMCM hydrochloride  Cat. No.: HY-100369A

Emamectin Benzoate (MK-244) Cat. No.: HY-B0837

Ethyl dirazepate  Cat. No.: HY-101596

Etifoxine (HOE 36-801) Cat. No.: HY-16579A

Etifoxine hydrochloride (HOE 36-801 (hydrochloride)) Cat. No.: HY-16579

Etomidate (R 16659) Cat. No.: HY-B0100

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Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

5 mg, 10 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

10 mg, 50 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: 99.74%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg

Purity: >98%Clinical Data: No Development ReportedSize:

Purity: 99.98%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: 99.09%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

10 mg, 50 mg, 100 mg, 200 mg, 500 mg

 

Bioactivity: Etomidate Hcl(R16659 Hcl) is a GABAA receptors agonist, whichis a short acting intravenous anaesthetic agent used for theinduction of general anaesthesia.

Bioactivity: FG8119 is a novel agonist extracted from patentbenzodiazepineUS 4745112 A.

Bioactivity: Flumazenil is a competitive antagonist, usedGABAA receptorin the treatment of benzodiazepine overdoses.

Bioactivity: Flumazenil acid is a metabolite of Flumazenil . Flumazenil[1]

is a GABAA receptor antagonist .[2]

Bioactivity: Fluxametamide is an insecticide with wide spectrum, acts as anantagonist of ,GABA- and glutamate-gated chloride channelswith of 1.95 nM and 225 nM for GABAClsIC50 M. domestica

and GluCls.

Bioactivity: Gabazine is a selective and competitive antagonist of GABAA, with an of ~0.2 μM for GABA receptor.receptor IC50

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

Bioactivity: Ginkgolide A (BN-52020) is an extract from in Ginkgo bilobaand a g-aminobutyric acid (GABA) antagonist.

Bioactivity: Ginsenoside Rc, one of major Ginsenosides from ,Panax ginsengenhances GABA receptor ( )-mediated ion channelA GABAAcurrents (I ). Ginsenoside Rc inhibits the expression ofGABA

and .TNF-α IL-1β

Bioactivity: Guvacine hydrochloride is an alkaloid from the nut of Areca, acts as an inhibitor of , andcatechu GABA transporter

dispalys modest selectivity for cloned GABA transporters withs of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (ratIC50

GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM…

6 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Etomidate hydrochloride (R16659 hydrochloride) Cat. No.: HY-B0100A

FG8119 (NNC13-8119) Cat. No.: HY-U00233

Flumazenil (Ro 15-1788) Cat. No.: HY-B0009

Flumazenil acid (Ro 15-3890) Cat. No.: HY-118844

Fluxametamide  Cat. No.: HY-108690

Gabazine (SR95531) Cat. No.: HY-103533

Gidazepam (Gidasepam; Hidazepam; Hydazepam) Cat. No.: HY-U00315

Ginkgolide A (BN-52020) Cat. No.: HY-B0355

Ginsenoside Rc (Panaxoside Rc) Cat. No.: HY-N0042

Guvacine hydrochloride  Cat. No.: HY-100809

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Purity: 97.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

1 g

Purity: >98%Clinical Data: No Development ReportedSize:

Purity: 99.78%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

100 mg

Purity: 99.50%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

10 mg, 50 mg, 100 mg

Purity: 99.25%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg

Purity: 98.18%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

5 mg, 10 mg, 25 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

25 mg, 50 mg, 100 mg

Purity: 99.52%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

 

Bioactivity: Imepitoin (AWD 131-138) is a new low-affinity partialbenzodiazepine receptor agonist with potent anticonvulsant andanxiolytic properties in rodent models.

Bioactivity: Isoguvacine hydrochloride is a receptor agonist.GABA

Bioactivity: Jujuboside A is a glycoside extracted from Semen Ziziphi, a Chinese herbal medicine used to treat insomnia andSpinosae

anxiety.

Bioactivity: L-655708 is a potent α5 subunit-selective GABAA receptorinverse agonist (Ki = 0.45 nM). IC50: 0.45 nM (Ki) Target:GABA in vitro: L-655708 is a potent, selective inverse agonistfor the benzodiazepine site of GABAA receptors containing theα5 subunit (Ki = 0.45 nM). Displays 50-100-fold selectivity…

Bioactivity: L-cycloserine irreversibly inhibit GABA pyridoxal5′-phosphate-dependent aminitransferase in E. coli, as well inthe brains of various animals in a time-dependent manner,results in increased levels of gamma-aminobutyric acid (GABA),which is an inhibitory neurotransmitter in vivo.

Bioactivity: L-DABA (L-2,4-Diaminobutyric acid) is a week GABAtransaminase inhibitor with an of larger than 500 μM;IC50exhibits antitumor activity and .in vivo in vitro

Bioactivity: Loreclezole, an antiepileptic compound, is a selective GABAA modulator and acts as a positive allostericreceptor

modulator of β2 or β3-subunit containing receptors .[1] [2]

Bioactivity: Lorediplon is a novel non-benzodiazepine, hypnotic drug actingas a GABAA receptor modulator, differentially active at thealpha1-subunit, associated with promoting sleep.

Bioactivity: Lotilaner is a , acts as a potent non-competitiveparasiticideantagonist of insects , with an of 23.84GABACl receptors IC50nM for GABA receptor. No effect on aDrosophila melanogasterdog GABAA receptor .[1]

Bioactivity: Methionine (MRX-1024) is an effective chemoprotective agentwhich can also inhibit the neuronal activity through GABAAreceptor activation.

Imepitoin (AWD 131-138) Cat. No.: HY-14953

Isoguvacine hydrochloride  Cat. No.: HY-100810

Jujuboside A  Cat. No.: HY-N0659

L-655708  Cat. No.: HY-14426

L-Cycloserine ((S)-4-Amino-3-isoxazolidone; (S)-Cycloserine) Cat. No.: HY-B1122

L-DABA (L-2,4-Diaminobutyric acid) Cat. No.: HY-101414

Loreclezole (R 72063) Cat. No.: HY-105272

Lorediplon  Cat. No.: HY-19371

Lotilaner  Cat. No.: HY-116564

Methionine (MRX-1024; D-Methionine) Cat. No.: HY-13694

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Purity: >98%Clinical Data: No Development ReportedSize:

Purity: 98.61%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

100 mg

Purity: 98.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 g

Purity: 99.76%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

10 mg, 50 mg, 100 mg

Purity: 99.85%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: 99.84%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: 99.96%Clinical Data: Phase 2Size: 10mM x 1mL in DMSO,

50 mg, 100 mg

Purity: 98.29%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg

 

Bioactivity: MRK-016 is a selective, orally bioavailable inverse agonist of, with an of 3 nM for GABA α5,GABA α5 receptorA EC50 A

and s of 0.83, 0.85, 0.77and 1.4nM for humanGABAKiα1β3γ2, GABA α2β3γ2, GABA α3β3γ2, and GABA α5β3…A A A A

Bioactivity: Nefiracetam is a GABAergic, cholinergic, and monoaminergicneuronal systems enhancer for Ro 5-4864-induced convulsions.

Bioactivity: NEO 376 is a selective modulator of , 5-HT1 receptor GABA and , with anti-psychoticreceptor dopamine receptor

actively.

Bioactivity: NS11394 is a potent and subtype-selective GABA(A)receptor-positive modulator; possesses a functional efficacyselectivity profile of alpha(5) > alpha(3) > alpha(2)> alpha(1) at GABA(A) alpha subunit-containing receptors.

Bioactivity: ONO-8590580 is a negative allosteric modulator.GABA α5A Bioactivity: Oxiracetam is a cyclic derivative of (γ-aminobutyric acid) which has been commonly used as nootropic drug to treatGABA

cognitive impairments.

Bioactivity: p-Hydroxybenzaldehyde is a one of the major components inDendrocalamus asper bamboo shoots, with antagonistic effect on

of the α β γ S subtype at highGABA receptorA 1 2 2concentrations.

Bioactivity: Picrotoxin is a noncompetitive antagonist of .GABAA receptor

Bioactivity: Pipequaline (PK 8165) is a partial benzodiazepine receptoragonist with anxiolytic activity .[1] [2]

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

.[2]

8 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

MRK-016  Cat. No.: HY-100370

Nefiracetam (DM9384; DZL-221) Cat. No.: HY-B0340

NEO 376 (SPI-376) Cat. No.: HY-101583

NS11394  Cat. No.: HY-11048

ONO-8590580  Cat. No.: HY-112788

Oxiracetam (ISF2522) Cat. No.: HY-B1715

p-Hydroxybenzaldehyde  Cat. No.: HY-Y0313

Picrotoxin (Cocculin) Cat. No.: HY-101391

Pipequaline (PK-8165) Cat. No.: HY-100140

Pipequaline hydrochloride (PK-8165 (hydrochloride)) Cat. No.: HY-100140A

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Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: 99.94%Clinical Data: LaunchedSize: 10mM x 1mL in Water,

50 mg, 100 mg, 500 mg

Purity: 99.83%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

50 mg, 100 mg, 500 mg, 1 g

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: >98%Clinical Data: LaunchedSize: 500 mg, 100 mg, 250 mg

Purity: 97.78%Clinical Data: Phase 3Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 250 mg, 500 mg

Purity: 99.95%Clinical Data: LaunchedSize: 1 g, 5 g

Purity: 99.07%Clinical Data: LaunchedSize: 1 g, 5 g

Purity: 99.74%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

100 mg

 

Bioactivity: Primidone is an anticonvulsant of the pyrimidinedione class. Bioactivity: Procaine is a local anesthetic drug of the amino ester group,which acts through multiple targets. Target: Others Procaineis a local anesthetic of the ester type that has a slow onsetand a short duration of action.Procaine (0.01-100 microM)inhibited the 5-HT3 receptor-mediated inward current in the…

Bioactivity: Procaine Hydrochloride is a local anesthetic drug of the aminoester group. Target: Others Procaine is a local anesthetic ofthe ester type that has a slow onset and a short duration ofaction.Procaine (0.01-100 microM) inhibited the 5-HT3receptor-mediated inward current in the whole-cell patch clamp…

Bioactivity: Radequinil (AC-3933) is a benzodiazepine receptor (BzR)partial inverse agonist. AC-3933 binds to andGABA(-)

with s of 5.15 and 6.11 nM, respectivelyGABA(+) ligand Ki

.[1]

Bioactivity: Remimazolam benzenesulfonate is a GABA agonist. Bioactivity: Rilmazafone is a benzodiazepine ω ligand with sedative andhypnotic effects .[1]

Bioactivity: Rilmazafone hydrochloride (450191S) is a benzodiazepine ωligand with sedative and hypnotic effects .[1]

Bioactivity: Riluzole is an anticonvulsant drug and belongs to the familyof use-dependent blocker which can also inhibitNa channel+

uptake with an of 43 μM.GABA IC50

Bioactivity: Riluzole hydrochloride is an anticonvulsant drug and belongsto the family of use-dependent blocker which canNa channel+

also inhibit uptake with an of 43 μM.GABA IC50

Bioactivity: Ro 41-3290 is the desethylated derivative of Ro 41-3696, whichis a nonbenzodiazepine partial agonist at the benzodiazepine

. Ro 41-3290 is an investigational hypnotic.receptor

Primidone  Cat. No.: HY-B0339

Procaine  Cat. No.: HY-B0546

Procaine hydrochloride  Cat. No.: HY-B0546A

Radequinil (AC-3933) Cat. No.: HY-106025

Remimazolam benzenesulfonate (CN-7056 benzenesulfonate) Cat. No.: HY-14867A

Rilmazafone  Cat. No.: HY-106547

Rilmazafone hydrochloride (450191S) Cat. No.: HY-U00228

Riluzole (PK 26124) Cat. No.: HY-B0211

Riluzole hydrochloride (PK 26124 hydrochloride) Cat. No.: HY-B0211A

Ro 41-3290  Cat. No.: HY-U00215

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Purity: 98.20%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: LaunchedSize: 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg

Purity: 99.07%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Purity: 98.15%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg

Purity: >98%Clinical Data: No Development ReportedSize: 250 mg, 500 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: >98%Clinical Data: No Development ReportedSize: 250 mg, 500 mg

 

Bioactivity: RO 4938581 is a potent and selective inverseGABA α5Aagonist, with a of 4.6 nM for , and shows aKi GABA α5β3γ2aAlower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a ( , 174, 185, 80KinM, respectively); RO 4938581 is used in the research…

Bioactivity: Ru-32514 is an agonist of benzodiazepine receptor.

Bioactivity: RWJ-51204 is a partial agonist of , with GABA(A) receptor Kiof 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

Bioactivity: S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptoragonist, with K s of 34.6 nM, 36.2 nM for –GABA and +GABAirespectively.

Bioactivity: Sarmazenil is a antagonist.benzodiazepine receptor Bioactivity: SKF89976A hydrochloride is a selective (GABA transporter) inhibitor with s of 0.28 μM, 137.34 μM and 202.8GAT-1 IC50

μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

Bioactivity: SSD114 hydrochloride is a novel positiveGABA receptorBallosteric modulator.

Bioactivity: SX-3228 is a selective ( ) receptor agonistbenzodiazepine1 BZ1with an of 17 nM.IC50

Bioactivity: Tiagabine (NO050328) is a potent and selective GABA reuptakeinhibitor, used as an anticonvulsant agent, with s of 67,IC50

446 and 182 nM for [ H]GABA uptake in Synaptosomes, Neurons3

and Glia, respectively .[1]

Bioactivity: Tiagabine hydrochloride is a potent and selective GABA inhibitor, used as an anticonvulsant agent, withreuptake

s of 67, 446 and 182 nM for [ H]GABA uptake inIC503

Synaptosomes, Neurons and Glia, respectively .[1]

10 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

RO 4938581  Cat. No.: HY-107489

Ru-32514  Cat. No.: HY-19065

RWJ-51204  Cat. No.: HY-19308

S-8510 phosphate (SB-737552 phosphate) Cat. No.: HY-103225

Sarmazenil (Ro 15-3505) Cat. No.: HY-100248

SKF89976A hydrochloride (d,l-SKF89976A hydrochloride) Cat. No.: HY-100228A

SSD114 hydrochloride  Cat. No.: HY-103668A

SX-3228  Cat. No.: HY-100291

Tiagabine (NO050328; NO328; TGB) Cat. No.: HY-B0696

Tiagabine hydrochloride (NO050328 hydrochloride; NO328

hydrochloride; TGB hydrochloride) Cat. No.: HY-B0696A

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Purity: 97.0%Clinical Data: No Development ReportedSize: 10mM x 1mL in Water,

100 mg

Purity: 99.93%Clinical Data: Phase 2Size: 10mM x 1mL in DMSO,

1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Purity: 98.0%Clinical Data: LaunchedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg

Purity: 98.0%Clinical Data: LaunchedSize: 10mM x 1mL in Water,

5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg

Purity: 99.92%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mg

Purity: 99.71%Clinical Data: No Development ReportedSize: 10mM x 1mL in DMSO,

1 mg, 5 mg, 10 mg, 20 mg

Purity: >98%Clinical Data: LaunchedSize: 10 mg, 50 mg

 

Bioactivity: Tiagabine hydrochloride hydrate is a potent and selective inhibitor, used as an anticonvulsant agent, withGABA uptake

s of 67, 446 and 182 nM for [ H]GABA uptake inIC503

Synaptosomes, Neurons and Glia, respectively .[1]

Bioactivity: TPA 023 is a subtype-selective agonist, with GABAA α2/α3 Kiof 0.19-0.41 nM.

Bioactivity: U-101017 is a partial agonist of andbenzodiazepine receptor, with anxiolytic effects.GABAA receptor

Bioactivity: U93631 is a GABAA receptor ligand of novel chemical structurewith IC50 of 100 nM,and has been shown to induce a rapid,time-dependent decay of GABA-induced whole-cell Cl-currents inrecombinant GABAA receptors. target: GABAA receptor IC 50:GABAA receptor[1] In vitro: In the presence of U93631 at 5 UM,…

Bioactivity: Uldazepam is a benzodiazepine derivative and can be used totreat patients with anxiety syndromes as tranquilizer.

Bioactivity: Vigabatrin(γ-Vinyl-GABA; Sabril) is a structural analog of theinhibitory neurotransmitter γ-aminobutyric acid (GABA) thatirreversibly inhibits the catabolism of GABA by GABAtransaminase. IC50 value: Target: GABA transaminase Clinicalstudies have shown that vigabatrin is superior to placebo in…

Bioactivity: Vigabatrin Hcl(γ-Vinyl-GABA; Sabril) is a structural analog ofthe inhibitory neurotransmitter γ-aminobutyric acid (GABA)that irreversibly inhibits the catabolism of GABA by GABAtransaminase. IC50 value: Target: GABA transaminase Clinicalstudies have shown that vigabatrin is superior to placebo in…

Bioactivity: Zuranolone (SAGE-217) is a potent agonistGABA receptorAwith s of 296 and 163 nM for and EC50 α β γ1 2 2 α β δ4 3

, respectively.GABA receptorsA

Bioactivity: γ-Aminobutyric acid (4-Aminobutyric acid) is a majorinhibitory neurotransmitter in the adult mammalian brain [1]

, binding to the ionotropic GABA receptors ( [2] GABAA) and metabotropic receptors ( receptors GABA receptorsB

Tiagabine hydrochloride hydrate (NO050328 hydrochloride

hydrate; NO328 hydrochloride hydrate; …) Cat. No.: HY-B0696B

TPA 023  Cat. No.: HY-101640

U-101017 (PNU 101017) Cat. No.: HY-19250

U93631  Cat. No.: HY-100686

Uldazepam (U31920) Cat. No.: HY-100264

Vigabatrin (γ-Vinyl-GABA) Cat. No.: HY-15399

Vigabatrin Hydrochloride (γ-Vinyl-GABA hydrochloride) Cat. No.: HY-B0033

Zuranolone (SAGE-217) Cat. No.: HY-103040

γ-Aminobutyric acid (4-Aminobutyric acid) Cat. No.: HY-N0067