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Results for "

GABAA agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (5) Apoptosis (1) Cytochrome P450 (3) Dopamine Receptor (1) Drug Metabolite (1) Endogenous Metabolite (4) GABA Receptor (99) Histamine Receptor (1) iGluR (6) Isotope-Labeled Compounds (4) Keap1-Nrf2 (1) NF-κB (6) Orphan GPCR (1) Phosphodiesterase (PDE) (1) PPAR (6) Reactive Oxygen Species (ROS) (1) Reference Standards (21) Sigma Receptor (6) Sirtuin (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (4) Inflammation/Immunology (9) Metabolic Disease (16) Neurological Disease (92)
Click Chemistry:	Azide (1) Alkynes (1)

104

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Natural
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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-113416

Dehydroepiandrosterone sulfate 5 Publications Verification DHEA sulfate; Prasterone sulfate	GABA Receptor Sigma Receptor iGluR PPAR NF-κB	Neurological Disease Metabolic Disease Inflammation/Immunology
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	Endogenous Metabolite	Metabolic Disease
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-B0765

Dehydroepiandrosterone sulfate sodium 5 Publications Verification DHEA sulfate sodium; Prasterone sulfate sodium	GABA Receptor Sigma Receptor iGluR PPAR NF-κB	Neurological Disease Metabolic Disease Inflammation/Immunology
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-10232

THIP 1 Publications Verification Gaboxadol	GABA Receptor	Neurological Disease
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-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-129105

Clomethiazole 4 Publications Verification	GABA Receptor Cytochrome P450	Neurological Disease
Chlormethiazole is an potent and orally active *GABA_A* agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .

HY-10233

Gaboxadol hydrochloride 1 Publications Verification Lu 02-030 hydrochloride; THIP hydrochloride	GABA Receptor	Neurological Disease
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABA_A receptor and an antagonist of GABA_C receptors (IC₅₀=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED₅₀ value of 143 μM, a full agonist efficacy at α5 subunit (ED₅₀=28-129 μM) and a superagonist efficacy at α4β3δ (ED₅₀=6 μM). Gaboxadol hydrochloride is a non-opioid agent .

HY-113413

Imidazoleacetic acid 2 Publications Verification Imidazolyl-4-acetic acid	Endogenous Metabolite GABA Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease
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-Y1176

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

HY-14426

L-655708 4 Publications Verification	GABA Receptor	Neurological Disease
L-655708 is a potent α5 subunit-selective *GABAA* receptor inverse agonist (K_i=0.45 nM).

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-N0301

Thiocolchicoside	GABA Receptor	Neurological Disease Inflammation/Immunology
Thiocolchicoside is a competitive *γ-aminobutyric acid type A (GAB_AA)* receptor antagonist and glycine receptor** agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties .

HY-132806

Alogabat RG-7816; RO-7017773	GABA Receptor	Neurological Disease
Alogabat is a positive allosteric modulator (PAM) and agonist (K_i <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction .

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_is of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively .

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-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-116622

α5IA L-822179	GABA Receptor	Neurological Disease
α5IA (L-822179) is a selective α5 *GABAA* receptor inverse agonist with neuroprotective potential .

HY-101640

TPA 023	GABA Receptor	Neurological Disease
TPA 023 is a GABAA α2/α3 subtype-selective agonist, with K_i of 0.19-0.41 nM.

HY-100800

TACA trans-4-Aminocrotonic acid	GABA Receptor	Neurological Disease
TACA (trans-4-Aminocrotonic acid) is a potent agonist of *GABA_A* and GABA_C receptors (K_D= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons .

HY-A0296

Chlormethiazole hydrochloride 4 Publications Verification Clomethiazole hydrochloride	Cytochrome P450	Neurological Disease
Clomethiazole hydrochloride is a potent and orally active *GABA_A* agonist . Clomethiazole hydrochloride inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Clomethiazole hydrochloride is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .

HY-19505

TPA-023B	GABA Receptor	Neurological Disease
TPA-023B is a high-affinity and orally active *GABA_A* receptor α2/α3 subtype (K_is of 0.73 nM/2 nM) partial agonist and a α1 subtype (K_i of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties .

HY-105056

Bretazenil Ro 16-6028	GABA Receptor	Neurological Disease
Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A *(GABA_A*) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC₅₀ (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC₅₀ of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .

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-101869

MK-0343 MRK-409	GABA Receptor	Neurological Disease
MK0343 (MRK-409) is an orally bioavailable *GABA_A* receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic .

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-103476

Ro15-4513	GABA Receptor	Neurological Disease
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-10061B

Lesogaberan hydrochloride AZD-3355 hydrochloride	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptor. The affinity (K_is) of Lesogaberan hydrochloride for rat GABA_B and GABA_A receptors, as measured by displacement of [ ³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

HY-141921S

Dehydroepiandrosterone sulfate sodium-d6 DHEA sulfate sodium-d6; Prasterone sulfate sodium-d6	Isotope-Labeled Compounds GABA Receptor Sigma Receptor iGluR PPAR NF-κB	Neurological Disease Metabolic Disease Inflammation/Immunology
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-138014

Cinazepam	GABA Receptor	Neurological Disease
Cinazepam is a partial GABA_A receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders .

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-103511

TCS1105	GABA Receptor	Neurological Disease
TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion .

HY-D1704

Bodipy TMR-X muscimol	GABA Receptor	Neurological Disease
Bodipy TMR-X muscimol is a Bodipy labeled Muscimol (HY-N2313) (Ex=543 nm, Em=572 nm). Muscimol is a GABAA agonist. Bodipy TMR-X muscimol can be used for imaging the spread of reversible brain inactivations .

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-113416R

Dehydroepiandrosterone sulfate (Standard) 1 Publications Verification DHEA sulfate (Standard); Prasterone sulfate (Standard)	Reference Standards GABA Receptor Sigma Receptor iGluR PPAR NF-κB	Neurological Disease Metabolic Disease Inflammation/Immunology
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-113416AS

Dehydroepiandrosterone sulfate-d6 sodium dihydrate DHEA sulfate-d6 sodium dihydrate; Prasterone sulfate-d6 sodium dihydrate	Isotope-Labeled Compounds GABA Receptor Sigma Receptor iGluR PPAR NF-κB	Neurological Disease Metabolic Disease Inflammation/Immunology
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-113329R

Guanidinoethyl sulfonate (Standard) Taurocyamine (Standard)	Endogenous Metabolite Reference Standards	Metabolic Disease
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-Y1176R

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

HY-19271

NS-2710	GABA Receptor	Neurological Disease
NS-2710 is a high-efficacy GABAAα3 agonist with a K_i of 9.2 nM. NS-2710 can be used for anxiety research .

HY-116457

Propanidid Sombrevin; Fabantol	GABA Receptor	Cardiovascular Disease Neurological Disease
Propanidid (Sombrevin; Fabantol) is a *γ-aminobutyric acid type A (GABA_A)* receptor** agonist and a short-acting non-barbiturate general agent that can suppress or relieve pain. Propanidid can decrease the arterial pressure .

HY-107489

RO 4938581	GABA Receptor	Neurological Disease
RO 4938581 is a potent and selective GABA_A α5 inverse agonist, with a K_i of 4.6 nM for GABA_A α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (K_i, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.

HY-123840

MRK-623	GABA Receptor	Neurological Disease
MRK-623 (Compound 14k) is an orally active, high-affinity GABA_A receptor agonist, with the K_i values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect .

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 .

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-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-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-103524R

Valerenic acid (Standard) (-)-Valerenic Acid (Standard)	5-HT Receptor GABA Receptor Reference Standards	Neurological Disease
Valerenic acid (Standard) is the analytical standard of Valerenic acid. This product is intended for research and analytical applications. 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-B0007A

(S)-Baclofen hydrochloride	GABA Receptor	Neurological Disease
(S)-Baclofen hydrochloride is a GABAB receptor agonist that crosses the blood-brain barrier and is orally active, with IC₅₀ values of 1.77 μM for GABAB and 1564 μM for GABAA. (S)-Baclofen hydrochloride can be used in research on muscle disorders such as spasticity .

Cat. No.	Product Name	Target	Research Area

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	Category	Target	Chemical Structure

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	Natural Products 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-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-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-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 Natural Products 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-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-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-179519

Umbelopsisin A	Structural Classification Alkaloids Microorganisms Indole Alkaloids Source Classification	GABA Receptor Reactive Oxygen Species (ROS)
Umbelopsisin A is a *GABA_A* and GABA_B non-selective agonist. Umbelopsisin A activates the GABAergic pathway, including notch signaling and fatty acid metabolism. Umbelopsisin A shows dual neuroprotection against glutamate excitotoxicity in vitro (reducing ROS and cell death) and in vivo. Umbelopsisin A can be used for the study of glaucoma and broader neurodegenerative disease applications .

Cat. No.	Product Name	Chemical Structure

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-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-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-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-Y1176S

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

Cat. No.	Product Name		Classification