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Results for "

GABAA receptor modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) AP-1 (1) Apoptosis (2) Bacterial (1) Chloride Channel (2) COX (1) Cytochrome P450 (2) Endogenous Metabolite (12) Environmental Pollutants (1) GABA Receptor (104) iGluR (8) Interleukin Related (1) Isotope-Labeled Compounds (8) Keap1-Nrf2 (1) Phosphodiesterase (PDE) (1) Potassium Channel (3) Reference Standards (11) Sirtuin (1) Taste Receptor (1)
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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1494

Picrotoxinin 4 Publications Verification	Chloride Channel GABA Receptor	Neurological Disease
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive **GABA_A receptor** antagonist, which negatively modulates the action of GABA on GABA_A receptors. Picrotoxinin inhibits α₁β₂γ_2L GABA_A receptor with an IC₅₀ of 1.15 μM .

HY-111052

AZD7325	GABA Receptor Cytochrome P450	Neurological Disease Inflammation/Immunology
AZD7325 is a potent and orally active partial selective PAM of **GABAAα2 and Aα3 receptor (K_i*=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor* subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.

HY-113320

Etiocholanolone 5β-Androsterone	GABA Receptor Endogenous Metabolite	Neurological Disease
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the *GABA_A* receptor than its enantiomer form .

HY-116152

Cipepofol Ciprofol; HSK3486	GABA Receptor Sirtuin Keap1-Nrf2 Apoptosis	Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the **GABA_A receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis** .

HY-16716

Basmisanil 1 Publications Verification RG1662; RO5186582	GABA Receptor	Neurological Disease
Basmisanil (RG1662) is a highly selective orally active *α subunit-containing GABAA* receptors (GABAAα5)** negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a K_i value of 5 nM and IC₅₀ value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .

HY-W013150

Alpidem	GABA Receptor	Neurological Disease
Alpidem, an anxiolytic agent, is an orally active and brain-penetrant *GABAA* receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC₅₀ of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC₅₀ of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions .

HY-110143

CLP257	Potassium Channel	Neurological Disease
CLP257 is a selective K ⁺-Cl cotransporter KCC2 activator with an EC₅₀ of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally .

HY-105042

Selank Selanc; TP-7	GABA Receptor	Neurological Disease
Selank (Selanc; TP-7) is a *GABAA* receptor modulator with anxiolytic activity. Selank allosterically modulates the specific binding of GABA to *GABAA* receptors and alters the affinity of endogenous ligands for these receptors. Selank reduces elevated anxiety levels, attenuates stress-induced exacerbation of anxiety, and produces a synergistic anxiolytic effect with diazepam. Selank can be used in the research of anxiety disorders .

HY-103524

Valerenic acid 1 Publications Verification (-)-Valerenic Acid	GABA Receptor 5-HT Receptor	Neurological Disease
Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of *GABA_A* receptors. Valerenic acid is also a partial agonist of the 5-HT_5a receptor. Valerenic acid mediates anxiolytic activity via GABA_A receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .

HY-N2096

Kavain 2 Publications Verification	GABA Receptor	Neurological Disease
Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .

HY-108584

Flindokalner BMS-204352	Potassium Channel	Neurological Disease
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (K_i=3.7 μM), and acts as a negative modulator of *GABAA* receptors. Flindokalner shows anxiolytic efficacy in vivo .

HY-16579

Etifoxine hydrochloride 3 Publications Verification HOE 36-801 hydrochloride	GABA Receptor	Neurological Disease
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing **GABA_A receptors**. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .

HY-N6084

Humulone α-Lupulic acid	COX GABA Receptor Apoptosis	Cardiovascular Disease
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of **GABA_A receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis**-inducing properties .

HY-101165

Cyclothiazide 2 Publications Verification	iGluR GABA Receptor	Neurological Disease
Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits *GABA_A* receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .

HY-16579A

Etifoxine 3 Publications Verification HOE 36-801	GABA Receptor	Neurological Disease
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing **GABA_A receptors**. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .

HY-120874

Darigabat PF-06372865; CVL-865	GABA Receptor	Neurological Disease
Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective *GABA_A* positive allosteric modulator (PAM). Darigabat is a high affinity ligand at GABA_A receptors containing α1/α2/α3/α5 subunits (K_is of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy .

HY-W677042

α-Androstenol 5α-Androst-16-en-3α-ol	GABA Receptor	Neurological Disease
α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and male axillary sweat. α-Androstenol is also a positive allosteric modulator of **GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC₅₀** of 0.4 μM). α-Androstenol produces anxiolytic-like, antidepressant-like, and anticonvulsant effects in mice. α-Androstenol can be used for the research of seizures .

HY-105042A

Selank diacetate Selanc diacetate; TP-7 diacetate	GABA Receptor	Neurological Disease
Selank diacetate (Selanc diacetate; TP-7 diacetate) is a *GABAA* receptor modulator with anxiolytic activity. Selank diacetate allosterically modulates the specific binding of GABA to *GABAA* receptors and alters the affinity of endogenous ligands for these receptors. Selank diacetate reduces elevated anxiety levels, attenuates stress-induced exacerbation of anxiety, and produces a synergistic anxiolytic effect with diazepam. Selank diacetate can be used in the research of anxiety disorders .

HY-100991

FG 7142 ZK 39106; LSU-65	GABA Receptor	Neurological Disease
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing **GABAA receptor (K_i*=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates* GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC₅₀= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex .

HY-105272

Loreclezole R 72063	GABA Receptor	Neurological Disease
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 .

HY-113346

Tetrahydrodeoxycorticosterone Tetrahydro-11-deoxycorticosterone	GABA Receptor Endogenous Metabolite	Neurological Disease
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of **GABA_A receptor**. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-123489

3α,21-Dihydroxy-5α-pregnan-20-one THDOC	GABA Receptor	Neurological Disease
3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of *GABA_A* receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABA_A receptors in vitro.

HY-113346S

Tetrahydrodeoxycorticosterone-d3 1 Publications Verification Tetrahydro-11-deoxycorticosterone-d₃	Isotope-Labeled Compounds GABA Receptor Endogenous Metabolite	Neurological Disease
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 .

HY-N8852

6-Methoxyflavanone 6-MeOF	GABA Receptor Taste Receptor	Neurological Disease Metabolic Disease
6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of *GABA_A* receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABA_A receptors, and is relatively inactive on the α1β2 GABA_A receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain .

HY-W015793

6-Aminonicotinic acid	GABA Receptor	Others
6-Aminonicotinic acid is a **GABA_A receptor agonist with K_i** value of 4.4 nM. 6-Aminonicotinic acid can be formed via electrocatalytic synthesis at silver cathodes. 6-Aminonicotinic acid has a variety of biological properties, such as protein synthesis inhibitor, vitamin B₃ agonist, and modulating agent in chemotherapy .

HY-103520

DS2	GABA Receptor	Neurological Disease
DS2 is a selective positive allosteric modulator of **δ-GABA_A 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 .

HY-B1803A

Tracazolate hydrochloride ICI 136753 hydrochloride	GABA Receptor	Neurological Disease
Tracazolate (ICI 136753) hydrochloride is a potent *GABA_A* receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC₅₀=13.2 μM), α1β3γ2 (EC₅₀=1.5 μM). Tracazolate hydrochloride has the potency (EC₅₀) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity .

HY-19872

AZD6280	GABA Receptor	Neurological Disease
AZD6280 is a selective **GABAA(α2/3) receptor** modulator, used for treatment of generalized anxiety disorder.

HY-153584

MRK-898	GABA Receptor	Neurological Disease
MRK-898 is an orally active **GABA(A) receptor** modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with K_i values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s) .

HY-W001692

Ocinaplon DOV 273547	GABA Receptor	Neurological Disease
Ocinaplon (DOV 273547) is an orally active positive allosteric modulator of **GABA_A receptor, with an EC₅₀** ranging from 3.07 μM (α1β2γ2 subtype) to 10.03 μM (α1β2γ3 subtype). Ocinaplon enhances GABA-stimulated chloride currents across multiple GABA_A receptor subtypes, with varying potency between different subtypes. Ocinaplon exerts anxiolytic and anticonvulsant effects, and causes motor impairment at high doses. Ocinaplon can be used for research on generalized anxiety disorder .

HY-168758

Delta3,5-cholestadien-7-one	GABA Receptor	Neurological Disease
Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of **GABAA receptors*. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA* receptors with IC₅₀ values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons .

HY-109572

GABAA receptor modulator-1	GABA Receptor	Neurological Disease
GABAA receptor modulator-1 (9eey) is a **GABAA receptor** modulator that can be used in the study of central nervous system diseases .

HY-19371

Lorediplon	GABA Receptor	Neurological Disease
Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.

HY-129408

SGE-516	GABA Receptor	Neurological Disease
SGE-516 is a neuroactive steroid that is a potent positive allosteric modulator of synaptic and extra-synaptic *GABAA* receptors. SGE-516 has anticonvulsant activity .

HY-B1606

Chlorothymol Chlorthymol; 6-Chlorothymol	Environmental Pollutants Bacterial AP-1 GABA Receptor	Infection Neurological Disease
Chlothymol is a potent positive modulator of the *GABA_A* receptor subunit LGC-37, anticonvulsant, and antibacterial agent. Chlothymol inhibits Pentylenetetrazol-induced c-fos expression. Chlothymol inhibits the growth of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA) strains, including LAC, with an MIC of 32 μg/mL. Chlorothymol has protective effects against epileptic seizures in various mouse models .

HY-170902

GABAA receptor modulator-4	GABA Receptor	Neurological Disease
GABAA receptor modulator-4 (Compound 4) is the negative allosteric modulator for **GABAA receptor*. GABAA* receptor modulator-4 inhibits α1β3γ2 GABAA receptor-mediated peak and steady currents with IC₅₀ of 10 μM and 10 μM .

HY-172588

GABAA receptor modulator-7	GABA Receptor	Neurological Disease
GABAA receptor modulator-7 (compound 1m), a spiro-Barbiturate, is a **GABAA receptor** modulator. GABAA receptor modulator-7 reverses the action of anesthetics without affecting GABA-induced desensitization and can be used for study of antiepileptics and anxiolytics .

HY-175670

GABAA receptor modulator-10	GABA Receptor	Neurological Disease
GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 **GABAA receptor** with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy .

HY-173616

GABAA receptor modulator-8	GABA Receptor	Neurological Disease
GABAA receptor modulator-8 (10c) is a blood-brain barrier penetrated, selective and positive modulator of **GABAA receptor**, with excellent antiepileptic activity .

HY-161784

GABAA receptor modulator-5	GABA Receptor	Neurological Disease
GABAA receptor modulator-5 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA *receptor), with EC₅₀* of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modulator-5 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modulator-5 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression .

HY-147657

GABAA receptor modulator-2	GABA Receptor	Neurological Disease
GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABA_AR negative allosteric modulator (NAM) with a K_i of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .

HY-175251

GABAA receptor modulator-9	GABA Receptor	Neurological Disease
GABAA receptor modulator-9 is and positive allosteric modulator of a1β2y2 subtype *GABA_A* that can cross the blood-brain barrier. GABAA receptor modulator-9 exhibits comparable activity on α1β2γ2 (EC₅₀: 0.9 μM in oocytes, 0.2 μM in CHO cells) and on α1β2, α3β2γ2 and α1β3γ2 (EC₅₀s of 1.3, 3.4 and 1.1 μM). GABAA receptor modulator-9 significantly suppresses seizure progression and reduces delayed mortality. GABAA receptor modulator-9 can be used for the study of status epilepticus (SE) .

HY-170903

GABAA receptor modulator-3	GABA Receptor	Neurological Disease
GABAA receptor modulator-3 (compound 3b) is a positive allosteric modulator (PAM). GABAA receptor modulator-3 inhibits α1β3γ2 GABAAR at peak and steady state currents with IC₅₀s of 671 and 64 μM, respectively .

HY-170771

*α5-GABAA* receptor modulator 1**	GABA Receptor	Neurological Disease
α5-GABAA receptor modulator 1 (Compound A-4) is a silencing allosteric modulator (SAM) specifically targeting the a5 subunit of the **GABA_A receptor**, suitable for research into central nervous system (CNS) disorders .

HY-159826

Brexanolone caprilcerbate	GABA Receptor	Neurological Disease
Brexanolone caprilcerbate is a potent *GABAA* receptor positive allosteric modulator .

HY-181552

GABAA receptor modulator-13	GABA Receptor	Neurological Disease
GABAA receptor modulator-13 is an orally active, blood-brain barrier-permeable α₄β₁δ GABA_A receptor modulator (IC₅₀ = 9.02 μM). GABAA receptor modulator-13 reduces GABA-induced currents, impairs the stability of the transmembrane domain M2-M3 loop of α₄β₁δ GABA_A receptors, and exhibits selectivity for γ₂-containing GABA_A receptor subtypes and α₆β₃δ GABA_A receptor subtypes. GABAA receptor modulator-13 is applicable to the research of nervous system diseases with altered tonic inhibition, such as neurodevelopmental disorders and epilepsy .

HY-121393

Imidazenil	GABA Receptor	Neurological Disease
Imidazenil is a partial positive allosteric modulator of *GABA_A* receptors with anxiolytic, antipanic and anticonvulsant activities.

HY-147421

Xilmenolone	GABA Receptor	Neurological Disease
Xilmenolone is a **GABAA receptor** positive allosteric modulator .

HY-120276

Golexanolone GR3027	GABA Receptor	Neurological Disease
Golexanolone is a **GABA_A receptor** modulating steroid antagonist. Golexanolone reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in hyperammonemic rats .

HY-103501

SB-205384	GABA Receptor	Neurological Disease
SB-205384 is a *GABAA* receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist .

Cat. No.	Product Name	Target	Research Area

HY-105042

Selank Selanc; TP-7	GABA Receptor	Neurological Disease
Selank (Selanc; TP-7) is a *GABAA* receptor modulator with anxiolytic activity. Selank allosterically modulates the specific binding of GABA to *GABAA* receptors and alters the affinity of endogenous ligands for these receptors. Selank reduces elevated anxiety levels, attenuates stress-induced exacerbation of anxiety, and produces a synergistic anxiolytic effect with diazepam. Selank can be used in the research of anxiety disorders .

HY-105042A

Selank diacetate Selanc diacetate; TP-7 diacetate	GABA Receptor	Neurological Disease
Selank diacetate (Selanc diacetate; TP-7 diacetate) is a *GABAA* receptor modulator with anxiolytic activity. Selank diacetate allosterically modulates the specific binding of GABA to *GABAA* receptors and alters the affinity of endogenous ligands for these receptors. Selank diacetate reduces elevated anxiety levels, attenuates stress-induced exacerbation of anxiety, and produces a synergistic anxiolytic effect with diazepam. Selank diacetate can be used in the research of anxiety disorders .

HY-P5860

MmTx1 toxin Micrurotoxin 1	GABA Receptor	Neurological Disease
MmTx1 toxin (Micrurotoxin 1) is an allosteric *GABA_A* receptor modulator that increases GABA_A receptor susceptibility to agonist .

HY-P5857

MmTx2 toxin Micrurotoxin 2	GABA Receptor	Neurological Disease
MmTx2 toxin is a *GABA_A* receptor modulator that enhances *GABA_A* receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .

Cat. No.	Product Name	Target	Research Area	Image

HY-P992360

GT-002	GABA Receptor	Neurological Disease Cancer
GT-002 is a partial positive allosteric modulator targeting the α3 subtype of *GABAA* receptors, as well as a specific binder of tumor-associated TF-glycosylated LYPD3. GT-002 mildly enhances GABA-induced chloride currents by binding to the benzodiazepine site of GABAA receptors, thereby alleviating prefrontal hypofunction and improving cognitive, memory and social interaction abilities. GT-002 can be used in research related to schizophrenia spectrum disorders, various squamous cell carcinomas, colorectal cancer, non-small cell lung cancer, and aromatic L-amino acid decarboxylase deficiency .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B1494

Picrotoxinin 4 Publications Verification	Structural Classification other families Terpenoids Sesquiterpenes Plants Source Classification	Chloride Channel GABA Receptor
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive **GABA_A receptor** antagonist, which negatively modulates the action of GABA on GABA_A receptors. Picrotoxinin inhibits α₁β₂γ_2L GABA_A receptor with an IC₅₀ of 1.15 μM .

HY-B0504

Creatinine Maximum Cited Publications 6 Publications Verification NSC13123	Infection Structural Classification Natural Products Classification of Application Fields Disease markers Endocrine diseases Metabolic Disease Nervous System Disorder Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite GABA Receptor iGluR
Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of *GABAA* and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure .

HY-113320

Etiocholanolone 5β-Androsterone	Microorganisms Endogenous metabolite Steroids Source Classification	GABA Receptor Endogenous Metabolite
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the *GABA_A* receptor than its enantiomer form .

HY-N2096

Kavain 2 Publications Verification	Natural Products Piper methysticum G.Forst. Piperaceae Plants Source Classification	GABA Receptor
Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .

HY-N6084

Humulone α-Lupulic acid	Cardiovascular Disease Classification of Application Fields Ketones, Aldehydes, Acids Humulus lupulus L. Plants Moraceae Disease Research Fields Source Classification	COX GABA Receptor Apoptosis
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of **GABA_A receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis**-inducing properties .

HY-B0504R

Creatinine (Standard) NSC13123 (Standard)	Infection Structural Classification Natural Products Microorganisms Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite iGluR GABA Receptor
Creatinine (Standard) is the analytical standard of Creatinine. This product is intended for research and analytical applications. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of *GABAA* and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure .

HY-113346

Tetrahydrodeoxycorticosterone Tetrahydro-11-deoxycorticosterone	Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification	GABA Receptor Endogenous Metabolite
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of **GABA_A receptor**. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-B1494R

Picrotoxinin (Standard)	Structural Classification Natural Products other families Plants Source Classification	Reference Standards Chloride Channel GABA Receptor
Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. 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. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC₅₀ of 1.15 μM .

HY-N2096R

Kavain (Standard)	Structural Classification Natural Products Piper methysticum G.Forst. Piperaceae Plants Source Classification	Reference Standards GABA Receptor
Kavain (Standard) is the analytical standard of Kavain. This product is intended for research and analytical applications. Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .

HY-N15436

5-Deoxykievitone	Structural Classification Flavonoids Leguminosae Phaseolus lunatus L. Plants Isoflavones Source Classification	GABA Receptor
5-Deoxykievitone, an isoflavanone found in Phaseolus species, is a GABA receptor modulator. 5-Deoxykievitone potentiates GABA-induced chloride current through α₁β₂γ_2s GABA_A receptors. 5-Deoxykievitone can be used for the research of epilepsy and anxiety .

Cat. No.	Product Name	Chemical Structure

HY-B0504S

Creatinine-d3

5 Publications Verification

Creatinine-d₃ is a deuterium labeled Creatinine. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure .

HY-B0504S2

Creatinine-d5

Creatinine-d₅ is the deuterium labeled Creatinine. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure .

HY-B0504S1

Creatinine-13C

Creatinine- ¹³C is the ¹³C-labeled Creatinine. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure .

HY-113346S

Tetrahydrodeoxycorticosterone-d3 1 Publications Verification
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 .

HY-B0504S5

Creatinine-15N

Creatinine- ¹⁵N (NSC13123- ¹⁵N) is the ¹⁵N-labeled Creatinine (HY-B0504). Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure .

HY-113320S

Etiocholanolone-d5
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .

HY-W013150S

Alpidem-d14

Alpidem-d₁₄ is the deuterium labeled Alpidem (HY-W013150) . Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC₅₀ of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC₅₀ of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.

HY-113320S1

Etiocholanolone-d2
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .

HY-16579AS2

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 .

HY-123489S

3α,21-Dihydroxy-5α-pregnan-20-one-d3
3α,21-Dihydroxy-5α-pregnan-20-one-d₃ is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.

HY-173251S

ENX-101
ENX-101 is an orally active (GABA_A) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC₅₀ = 0.76 nM), α2β3γ2L (EC₅₀ = 0.61 nM), α3 (EC₅₀ = 1.97 nM), α5 (EC₅₀ = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models .

Cat. No.	Product Name		Classification