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Results for "

GABAA receptor

" in MedChemExpress (MCE) Product Catalog:

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クリックケミストリー:	Azide (1) Alkynes (2)
Oligonucleotides:	Cholesterol (1)

325

阻害剤およびアゴニスト

スクリーニングライブラリ

生化学アッセイ試薬

ペプチド

阻害性抗体

天然物

組換えタンパク質

同位体標識化合物

抗体

クリックケミストリー

オリゴヌクレオチド

製品番号	製品名	Target	研究分野	構造式

HY-103533

Gabazine 5+ Cited Publications SR95531	GABA Receptor	Neurological Disease
Gabazine is a selective and competitive antagonist of **GABA_A receptor, with an IC₅₀** of ~0.2 μM for GABA receptor.

HY-B0009

Flumazenil 4 Publications Verification Ro 15-1788	GABA Receptor	Neurological Disease
Flumazenil is a competitive **GABAA receptor** antagonist, used in the treatment of benzodiazepine overdoses.

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-B0504

Creatinine 5+ Cited Publications NSC13123	Endogenous Metabolite GABA Receptor iGluR	Infection Neurological Disease Metabolic Disease Cancer
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-N2079

(-)-Securinine 1 Publications Verification	GABA Receptor	Neurological Disease Cancer
(-)-Securinine is plant-derived alkaloid and also a **GABA_A receptor** antagonist.

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-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-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-B1095

Chlormadinone acetate 1 Publications Verification	Progesterone Receptor Androgen Receptor Glucocorticoid Receptor GABA Receptor	Neurological Disease Metabolic Disease
Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and *GABA_A* receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders .

HY-Y1176

Isonipecotic acid	GABA Receptor	Neurological Disease
Isonipecotic acid is a GABAA receptor partial agonist .

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-116564

Lotilaner 1 Publications Verification	Parasite GABA Receptor	Infection
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC₅₀ of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor .

HY-124467

Difludiazepam Ro 07-4065	GABA Receptor	Neurological Disease
Difludiazepam (Ro 07-4065), a benzodiazepine derivative, is a *GABAA* receptor ligand with an IC₅₀ of 4.1 nM. Difludiazepam binds to an allosteric site on the *GABAA* receptor to potentiate the receptor's response to GABA, reducing neuron excitability. Difludiazepam contains halogenated groups at the ortho position of its phenyl ring .

HY-N2080

Songorine	GABA Receptor	Neurological Disease Cancer
Songorine is a BBB-permeable diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a **GABAA receptor** antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .

HY-P2602

α-Casozepine	GABA Receptor	Neurological Disease
α-Casozepine is an orally effective anxiolytic that binds to the benzodiazepine site of the *GABAA* receptor in bovine samples with an IC₅₀ of 88 μM. α-Casozepine exerts anxiolytic and anti-stress effects on cats exposed to unfamiliar environments and dogs undergoing road transport . α-Casozepine exhibits significant anxiolytic activity in rats. α-Casozepine can be used in studies related to fear, anxiety and stress .

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-100369A

DMCM hydrochloride	GABA Receptor	Neurological Disease
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant **GABAA αxβ3γ2 receptor subtypes with K_i*s of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors*, respectively .

HY-118844

Flumazenil acid Ro 15-3890	GABA Receptor Drug Metabolite	Neurological Disease
Flumazenil acid is a metabolite of Flumazenil . Flumazenil is a GABAA receptor antagonist .

HY-19945

DAA-1106 1 Publications Verification	GABA Receptor	Neurological Disease
DAA1106 is a peripheral benzodiazepine receptor (PBR) agonist that is permeable to the blood-brain barrier, but has no affinity for GABAA receptors.

HY-100370

MRK-016 2 Publications Verification	GABA Receptor	Cancer
MRK-016 is a selective, orally bioavailable inverse agonist of **GABA_A α5 receptor, with an EC₅₀** of 3 nM for GABA_A α5, and K_is of 0.83, 0.85, 0.77 and 1.4 nM for human GABA_A α1β3γ2, GABA_A α2β3γ2, GABA_A α3β3γ2, and GABA_A α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.

HY-124463

Epiallopregnanolone 5α,3β-THDOC	GABA Receptor iGluR	Neurological Disease
Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at **GABAA receptors** and a NMDA receptor enhancer .

HY-124030

3-Hydroxyphenazepam	Drug Metabolite	Neurological Disease
3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAA receptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ ³H]GABA uptake .

HY-107782

Picrotin	GABA Receptor	Neurological Disease
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

HY-114871

SL651498	GABA Receptor	Neurological Disease
SL651498 is a full agonist of α2 and α3 GABAA receptors, and a partial agonist of α1 and α5 GABAA receptors. SL651498 shows anxiolytic and anticonvulsant activities .

HY-116813

ZK 93423	GABA Receptor	Neurological Disease
ZK 93423 is a potent benzodiazepine *GABAA* receptor agonist with a certain cooling effect on rodents .

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-11048

NS11394 3 Publications Verification	GABA Receptor	Neurological Disease
NS11394 is an orally active and unique subtype-selective *GABA_A* positive allosteric receptor (PAM), with a K_i of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABA_A-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .

HY-N6648

Cirsimaritin	GABA Receptor	Neurological Disease
Cirsimaritin binds weakly to the benzodiazepine site on *GABA_A* receptors, with antidepressant, anxiolytic and antinociceptive activities.

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-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-101639A

CP-409092 hydrochloride	GABA Receptor	Neurological Disease
CP-409092 hydrochloride is a partial agonist of **GABA_A receptor**, with anti-anxiety activity .

HY-101665

Pagoclone (+)-RP-59037; IP-456; RP-62955	GABA Receptor	Neurological Disease
Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial **GABA(A) receptor** agonist used for the treatment of panic and anxiety disorders.

HY-133486

GABAA receptor agent 1	GABA Receptor	Neurological Disease
GABAA receptor agent 1 is a high affinity ligand for **GABAA receptor**, with potent anticonvulsant activity .

HY-Y1176R

Isonipecotic acid (Standard)	Reference Standards GABA Receptor	Neurological Disease
Isonipecotic acid is a GABAA receptor partial agonist .

HY-100686

U93631	GABA Receptor	Neurological Disease
U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.

HY-P5964A

K1 peptide TFA	GABA Receptor	Neurological Disease
K1 peptide TFA is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP) .

HY-145257

GABAA receptor agent 5	GABA Receptor	Neurological Disease
GABAA receptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an K_i of 0.020 µM. GABAA receptor agent 5 shows γ-GABAAR antagonist activity with low cellular membrane permeability .

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-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-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-172433

Refisolone	GABA Receptor	Neurological Disease
Refisolone is an antagonist of the **GABA_A receptor** .

HY-19250

U-101017 PNU 101017	GABA Receptor	Neurological Disease
U-101017 is a partial agonist of benzodiazepine receptor and **GABAA receptor**, with anxiolytic effects.

HY-159826

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

HY-123249

HZ166	GABA Receptor	Neurological Disease
HZ166 is a **GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2-** and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-P5964

K1 peptide	GABA Receptor	Neurological Disease
K1 peptide is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP) .

HY-145258

GABAA receptor agent 6	GABA Receptor	Neurological Disease
GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an K_i of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability .

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-147735

GABAA receptor agonist 1	GABA Receptor	Neurological Disease
GABAA receptor agonist 1 (compound 3e) is a potent **GABAA receptor** agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .

HY-147736

GABAA receptor agonist 2	GABA Receptor	Neurological Disease
GABAA receptor agonist 2 (compound 4c) is a potent **GABAA receptor** agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .

製品番号	製品名	Category	Target	構造式

HY-N0067

γ-Aminobutyric acid 5 Publications Verification 4-Aminobutyric acid	Structural Classification Animals Ketones, Aldehydes, Acids Endogenous metabolite	Environmental Pollutants Endogenous Metabolite GABA Receptor
γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABA_A *receptors) and metabotropic receptors* (GABA_B receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .

HY-B0649

Propofol 20+ Cited Publications 2,6-Diisopropylphenol	Structural Classification Monophenols Neurological Disease Classification of Application Fields Phenols Endogenous metabolite Disease Research Fields Source Classification Cancer	Environmental Pollutants Endogenous Metabolite GABA Receptor
Propofol potently and directly activates *GABA_A* receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .

HY-N0219

Bicuculline Maximum Cited Publications 37 Publications Verification (+)-Bicuculline	Alkaloids Lamprocapnos spectabilis (L.) Fukuhara Plants Isoquinoline Alkaloids Papaveraceae Source Classification	GABA Receptor
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter *GABA_A* receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca ²⁺ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .

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-113416

Dehydroepiandrosterone sulfate 5 Publications Verification DHEA sulfate; Prasterone sulfate	Human Gut Microbiota Metabolites Microorganisms Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Source Classification	GABA Receptor Sigma Receptor iGluR PPAR NF-κB
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of **GABA_A receptor** and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-113329

Guanidinoethyl sulfonate 5 Publications Verification Taurocyamine	天然物 Other disease Classification of Application Fields Disease markers Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC₅₀=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABA_A receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .

HY-13694

Methionine 5+ Cited Publications MRX-1024; D-Methionine	Human Gut Microbiota Metabolites Neurological Disease Classification of Application Fields Amino acids Endogenous metabolite Disease Research Fields Source Classification Cancer	GABA Receptor Endogenous Metabolite
Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through *GABA_A* receptor activation.

HY-B0504

Creatinine 5+ Cited Publications NSC13123	Infection Structural Classification 天然物 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-Y0313

p-Hydroxybenzaldehyde	Paramacrolobium coeruleum (Taub.) J.Léonard Ketones, Aldehydes, Acids Labiatae Phenols Plants Endogenous metabolite Source Classification	Endogenous Metabolite GABA Receptor
p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on **GABA_A receptor** of the α₁β₂γ₂S subtype at high concentrations.

HY-B0765

Dehydroepiandrosterone sulfate sodium 5 Publications Verification DHEA sulfate sodium; Prasterone sulfate sodium	Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Steroids Source Classification	GABA Receptor Sigma Receptor iGluR PPAR NF-κB
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of **GABA_A receptor** and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-N2079

(-)-Securinine 1 Publications Verification	Flueggea suffruticosa (Pall.) Baill. Alkaloids Structural Classification Neurological Disease Classification of Application Fields Pyridine Alkaloids Euphorbiaceae Plants Disease Research Fields Source Classification Cancer	GABA Receptor
(-)-Securinine is plant-derived alkaloid and also a **GABA_A receptor** antagonist.

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-113413

Imidazoleacetic acid 2 Publications Verification Imidazolyl-4-acetic acid	Structural Classification Human Gut Microbiota Metabolites Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite GABA Receptor
Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the *GABA_A receptor*. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .

HY-N2096

Kavain 2 Publications Verification	天然物 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-N0067R

γ-Aminobutyric acid (Standard) 5 Publications Verification 4-Aminobutyric acid (Standard)	Structural Classification Animals Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Endogenous Metabolite GABA Receptor Reference Standards
γ-Aminobutyric acid (Standard) is the analytical standard of γ-Aminobutyric acid. This product is intended for research and analytical applications. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .

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-N7110

6-Hydroxyflavone 2 Publications Verification	Monophenols Flavonoids Classification of Application Fields Flavones Labiatae Phenols Plants Medicago truncatula Gaertn. Inflammation/Immunology Disease Research Fields Source Classification	Akt ERK JNK GABA Receptor
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABA_A) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .

HY-N2080

Songorine	Alkaloids Structural Classification Aconitum soongaricum Stapf Classification of Application Fields Other Alkaloids Ranunculaceae Plants Disease Research Fields Source Classification Cancer	GABA Receptor
Songorine is a BBB-permeable diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a **GABAA receptor** antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC) .

HY-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate	Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification Cancer	nAChR GABA Receptor Potassium Channel Endogenous Metabolite
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, **GABAA receptor, and the inward-rectifier potassium ion channel**.

HY-W012123

3,4,5-Trimethoxycinnamic acid	Simple Phenylpropanols Polygalaceae Phenylpropanoids Plants Endogenous metabolite Polygala tenuifolia Willd. Source Classification	GABA Receptor Endogenous Metabolite
3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals . 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits .

HY-B1671

(+)-Kavain	Structural Classification Other Phenylpropanoids Piper methysticum G.Forst. Piperaceae Phenylpropanoids Plants Source Classification	GABA Receptor Sodium Channel Calcium Channel
(+)-Kavain, a main kavalactone that can be extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na ⁺ and Ca ²⁺ channels . (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

HY-B0504R

Creatinine (Standard) NSC13123 (Standard)	Infection Structural Classification 天然物 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-107782

Picrotin	Structural Classification other families Iridoids Terpenoids Marine natural products Plants Source Classification	GABA Receptor
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

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-114457

Phosphatidylinositol 4,5-bisphosphate L-alpha-Phosphatidylinositol-4,5-bisphosphate; (PtdIns)-(4,5)-P2	Structural Classification Human Gut Microbiota Metabolites Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Lipid Source Classification	Phospholipase
Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate) is a plasma membrane lipid that is enriched in the cytoplasmic leaflet of the plasma membrane. Phosphatidylinositol 4,5-bisphosphate serves as a substrate for phospholipase C and class I PI3K, generating diacylglycerol, inositol (1,4,5)-trisphosphate, and phosphatidylinositol (3,4,5)-trisphosphate. Phosphatidylinositol 4,5-bisphosphate contributes to lamellipodial protrusion, directional cell migration, focal adhesion lipid generation, and trafficking of the *GABA_A* receptor. Phosphatidylinositol 4,5-bisphosphate can be used in research related to acute lung injury and pulmonary edema .

HY-N6648

Cirsimaritin	Flavonoids Flavones Leguminosae Phenols Polyphenols Abrus precatorius Linn. Plants Source Classification	GABA Receptor
Cirsimaritin binds weakly to the benzodiazepine site on *GABA_A* receptors, with antidepressant, anxiolytic and antinociceptive activities.

HY-Y0313R

p-Hydroxybenzaldehyde (Standard)	Structural Classification Paramacrolobium coeruleum (Taub.) J.Léonard Ketones, Aldehydes, Acids Labiatae Phenols Plants Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite GABA Receptor
p-Hydroxybenzaldehyde (Standard) is the analytical standard of p-Hydroxybenzaldehyde. This product is intended for research and analytical applications. p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.

HY-113416R

Dehydroepiandrosterone sulfate (Standard) 1 Publications Verification DHEA sulfate (Standard); Prasterone sulfate (Standard)	Human Gut Microbiota Metabolites Microorganisms Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Source Classification	Reference Standards GABA Receptor Sigma Receptor iGluR PPAR NF-κB
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) (Standard) is the analytical standard of Dehydroepiandrosterone sulfate (HY-113416). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of **GABA_A receptor** and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-113329R

Guanidinoethyl sulfonate (Standard) Taurocyamine (Standard)	Structural Classification 天然物 Other disease Disease markers Endogenous metabolite	Endogenous Metabolite Reference Standards
Guanidinoethyl sulfonate (Standard) is the analytical standard of Guanidinoethyl sulfonate. This product is intended for research and analytical applications. Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .

HY-B0649R

Propofol (Standard) 2,6-Diisopropylphenol (Standard)	Structural Classification Monophenols Phenols Endogenous metabolite Source Classification	Reference Standards GABA Receptor Endogenous Metabolite
Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates *GABA_A* receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .

HY-W028263

6-Hydroxyflavanone	Flavonoids Flavonones Muntingia calabura L. Plants Muntingiaceae Source Classification	COX Opioid Receptor GABA Receptor Lipoxygenase
6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-A receptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes .

HY-W012123R

3,4,5-Trimethoxycinnamic acid (Standard)	Structural Classification Simple Phenylpropanols Polygalaceae Phenylpropanoids Plants Endogenous metabolite Polygala tenuifolia Willd. Source Classification	Reference Standards GABA Receptor Endogenous Metabolite
3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals . 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits .

HY-N0219R

Bicuculline (Standard) (+)-Bicuculline (Standard)	Alkaloids Structural Classification Lamprocapnos spectabilis (L.) Fukuhara Plants Isoquinoline Alkaloids Papaveraceae Source Classification	Reference Standards GABA Receptor
Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .

HY-B1494R

Picrotoxinin (Standard)	Structural Classification 天然物 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-N10887

Withasomniferolide B	Withania somnifera Plants Solanaceae Steroids Source Classification	GABA Receptor
Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .

HY-107782R

Picrotin (Standard)	Structural Classification other families Iridoids Terpenoids Plants Source Classification	GABA Receptor Reference Standards
Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

HY-N10884

Withasomniferolide A	Withania somnifera Plants Solanaceae Steroids Source Classification	Others
Withasomniferolide A is a withanolide, isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .

HY-N2079R

(-)-Securinine (Standard)	Flueggea suffruticosa (Pall.) Baill. Alkaloids Structural Classification Pyridine Alkaloids Euphorbiaceae Plants Source Classification	Reference Standards GABA Receptor
(-)-Securinine (Standard) is the analytical standard of (-)-Securinine. This product is intended for research and analytical applications. (-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.

HY-Y1683R

DL-Menthol (Standard) Racementhol (Standard)	Structural Classification 天然物 Leguminosae Labiatae Erythrina poeppigiana Plants Glycyrrhiza uralensis Fisch. Source Classification	Reference Standards GABA Receptor
DL-Menthol (Standard) is the analytical standard of DL-Menthol. This product is intended for research and analytical applications. DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol relates to the activation of GABAA receptor .

HY-13694R

Methionine (Standard) MRX-1024 (Standard); D-Methionine (Standard)	Structural Classification Human Gut Microbiota Metabolites Amino acids Endogenous metabolite Source Classification	Reference Standards GABA Receptor Endogenous Metabolite
Methionine (Standard) is the analytical standard of Methionine. This product is intended for research and analytical applications. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.

HY-N2096R

Kavain (Standard)	Structural Classification 天然物 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-B0765R

Dehydroepiandrosterone sulfate sodium (Standard) DHEA sulfate sodium (Standard); Prasterone sulfate sodium (Standard)	Structural Classification Endogenous metabolite Steroids Source Classification	Reference Standards GABA Receptor Sigma Receptor iGluR PPAR NF-κB
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of **GABA_A receptor** and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-B1671R

(+)-Kavain (Standard)	Structural Classification Other Phenylpropanoids Piper methysticum G.Forst. Piperaceae Phenylpropanoids Plants Source Classification	Reference Standards GABA Receptor Sodium Channel Calcium Channel
(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

HY-113413R

Imidazoleacetic acid (Standard) Imidazolyl-4-acetic acid (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite GABA Receptor
Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid (HY-113413). This product is intended for research and analytical applications. Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the *GABA_A receptor*. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .

HY-N6648R

Cirsimaritin (Standard)	Structural Classification Flavonoids Flavones Leguminosae Phenols Polyphenols Abrus precatorius Linn. Plants Source Classification	GABA Receptor Reference Standards
Cirsimaritin (Standard) is the analytical standard of Cirsimaritin (HY-N6648). This product is intended for research and analytical applications. Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.

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 .

HY-N18341

Ginkgolide M	Structural Classification Ginkgoaceae Terpenoids Sesquiterpenes Plants Ginkgo biloba Source Classification	GABA Receptor Drug Derivative
Ginkgolide M (GM) is a ginkgolide that can be isolated from Ginkgo biloba. Ginkgolide M acts as an inhibitor of ligand-gated ion channels in the central nervous system and exerts inhibitory effects on the *GABAA* receptor. Ginkgolide M can be used for the research of neurodegenerative diseases such as Alzheimer's disease .

製品番号	製品名	構造式

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-N0067S

γ-Aminobutyric acid-d6 2 Publications Verification
γ-Aminobutyric acid-d₆ is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain , binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors) .

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-13694S

Methionine-d3
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.

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-15831

L-838417-d9
L-838417-d₉ is the deuterium labeled L-838417 (HY-W009009). L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the *GABA_A* receptor and an antagonist at the α1, with binding K_i values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2. L-838417 has anti-anxiety activity .

HY-N0067S3

γ-Aminobutyric acid-13C4
γ-Aminobutyric acid- ¹³C₄ is the ¹³C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain , binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors) .

HY-141921S

Dehydroepiandrosterone sulfate sodium-d6

Dehydroepiandrosterone sulfate sodium salt-d₆ (DHEA sulfate sodium salt-d₆; Prasterone sulfate sodium salt-d₆) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

HY-B0135S

Furosemide-d5

Furosemide-d₅ is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl-?(NKCC) cotransporter, NKCC1 and NKCC2 .?Furosemide is also a GABAA?receptors antagonist and displays 100-fold selectivity for?α6-containing receptors than?α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .

HY-143831S

Cefepime-d8 sulfate

Cefepime-d₈ (BMY-28142-d₈) sulfate is deuterium labeled Cefepime sulfate. Cefepime sulfate is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC₅₀ of 21.115 mM and a K_i of 35.092 mM. Cefepime sulfate inhibits hPON1 via a non-competitive mechanism and blocks GABA_A receptors. Cefepime sulfate penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.

HY-B0649S

Propofol-d17
Propofol-d₁₇ is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties .

HY-N0067S1

γ-Aminobutyric acid-d2
γ-Aminobutyric acid-d₂ is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

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-13694S1

Methionine-d4
Methionine-d₄ 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.

HY-W654100

Cefepime-d3 sulfate

Cefepime-d₃ (BMY-28142-d₃) sulfate is deuterium labeled Cefepime sulfate. Cefepime sulfate is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC₅₀ of 21.115 mM and a K_i of 35.092 mM. Cefepime sulfate inhibits hPON1 via a non-competitive mechanism and blocks GABA_A receptors. Cefepime sulfate penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.

HY-B0649S1

Propofol-d18
Propofol-d₁₈ is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission .

HY-113416AS

Dehydroepiandrosterone sulfate-d6 sodium dihydrate

Dehydroepiandrosterone sulfate sodium dihydrate-d₆ sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABA_A receptor and agonist activity of σ₁ receptor. Dehydroepiandrosterone sulfate sodium dihydrate can partially penetrate the blood-brain barrier, inhibit GABA_A receptor-mediated chloride influx, enhance NMDA receptor activity through σ₁ receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium dihydrate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .

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-Y0313S

p-Hydroxybenzaldehyde-d4
p-Hydroxybenzaldehyde-d₄ is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.

HY-10232S

THIP-d4

THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC₅₀ value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .

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-Y0313S1

p-Hydroxybenzaldehyde-13C
p-Hydroxybenzaldehyde- ¹³C is the ¹³C-labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.

HY-W747264

P-Hydroxybenzaldehyde-13C6
P-Hydroxybenzaldehyde- ¹³C₆ is the ¹³C-labeled p-Hydroxybenzaldehyde (HY-Y0313). p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.

HY-Y1176S

Isonipecotic acid-d9
Isonipecotic acid-d₉ is the deuterium labeled Isonipecotic acid . Isonipecotic acid is a GABAA receptor partial agonist .

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-139145S

Etbicyphat-13C3
Etbicyphat- ¹³C₃ is the ¹³C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .

HY-N0067S2

γ-Aminobutyric acid-4,4-d2
γ-Aminobutyric acid-4,4-d₂ is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

HY-121877S

Valnoctamide-d5
Valnoctamide-d₅ is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors .

HY-W707528

Propofol-d14
Propofol-d₁₄ (2,6-Diisopropylphenol-d₁₄) is the deuterium labeled Propofol (HY-B0649). Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .

HY-124463S1

Epiallopregnanolone-d5
Epiallopregnanolone-d₅ (5α,3β-THDOC-d₅) is deuterium labeled Epiallopregnanolone. Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at **GABAA receptors** and a NMDA receptor enhancer .

HY-Y0313S2

p-Hydroxybenzaldehyde-d5
p-Hydroxybenzaldehyde-d₅ is the deuterium labeled p-Hydroxybenzaldehyde . p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations .

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-B1095S1

Chlormadinone acetate-d6-1

Chlormadinone acetate-d₆-1 is deuterium labeled Chlormadinone acetate (HY-B1095). Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABA_A receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders .

HY-B1095S2

Chlormadinone acetate-d3

Chlormadinone acetate-d₃ is the deuterium labeled Chlormadinone acetate (HY-B1095). Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABA_A receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders .

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-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-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 .

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Species:	Human (9)
Tag:	His (6) Strep (3) Avi (1) GST (1) MBP (1) Fc (1)
Source:	HEK293 (3) E. coli (6)


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Host:	Rabbit (3)
Reactivity:	Human (3) Rat (3) Mouse (3)
Application:	IHC-P (1) WB (3) FC (1)
Isotype:	IgG (3)
Conjugation:	Non-conjugated (3)
Clonality:	polyclonal (1) Monoclonal (2) Recombinant (2)
Modification:	Unmodified (3)


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