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GABAA α1 receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Chloride Channel (2) Cytochrome P450 (2) Endogenous Metabolite (6) GABA Receptor (71) Isotope-Labeled Compounds (5) NKCC (5) Reactive Oxygen Species (ROS) (1) Reference Standards (12) Sodium Channel (1) Taste Receptor (1)
By Research Areas:	Cancer (6) Cardiovascular Disease (3) Infection (1) Inflammation/Immunology (3) Metabolic Disease (6) Neurological Disease (62)

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Isotope-Labeled Compounds

Cat. No.	Nom du produit	Target	Áreas de investigación	Chemical Structure

HY-B0135

Furosemide Maximum Cited Publications 8 Publications Verification	NKCC GABA Receptor	Cardiovascular Disease Metabolic Disease Cancer
Furosemide is a potent and orally active inhibitor of Na ⁺/K ⁺/2Cl ^- (NKCC) cotransporter, NKCC1 and NKCC2 ^[1]. Furosemide is also a GABA_A 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-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 ^[1].

HY-111052

AZD7325	GABA Receptor Cytochrome P450	Neurological Disease Inflammation/Immunology
AZD7325 is a potent and orally active partial selective PAM of **GABAAα2 and Aα3 receptor (K_i*=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor* subtypes ^[1] . AZD7325 is a moderate CYP1A2* and* a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.

HY-Y0313

p-Hydroxybenzaldehyde	Endogenous Metabolite GABA Receptor	Neurological Disease
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-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 ^[1] .

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 ^[1] .

HY-16579

Etifoxine hydrochloride 3 Publications Verification HOE 36-801 hydrochloride	GABA Receptor	Neurological Disease
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing **GABA_A receptors**. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents ^[1] .

HY-120874

Darigabat PF-06372865; CVL-865	GABA Receptor	Neurological Disease
Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective *GABA_A* positive allosteric modulator (PAM). Darigabat is a high affinity ligand at GABA_A receptors containing α1/α2/α3/α5 subunits (K_is of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy ^[1].

HY-B0135A

Furosemide sodium Maximum Cited Publications 8 Publications Verification	NKCC GABA Receptor	Cardiovascular Disease Metabolic Disease Cancer
Furosemide sodium is a potent and orally active inhibitor of Na ⁺/K ⁺/2Cl ^- (NKCC) cotransporter, NKCC1 and NKCC2 ^[1]. Furosemide sodium is also a GABA_A receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .

HY-16579A

Etifoxine 3 Publications Verification HOE 36-801	GABA Receptor	Neurological Disease
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing **GABA_A receptors**. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents ^[1] .

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 ^[1].

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 ^[1].

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 ^[1].

HY-15831

L-838417-d9	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
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 ^[1].

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-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 ^[1].

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 ^[1] .

HY-B0135S

Furosemide-d5	NKCC GABA Receptor	Metabolic Disease Cancer
Furosemide-d₅ is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl-?(NKCC) cotransporter, NKCC1 and NKCC2 ^[1].?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-N6630

6-Methylflavone 2 Publications Verification	GABA Receptor	Neurological Disease
6-Methylflavone is an activator of α₁β₂γ_2L and α₁β₂ *GABA_A* receptors.

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 ^[1] .

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 ^[1] .

HY-B0135R

Furosemide (Standard) Maximum Cited Publications 8 Publications Verification	Reference Standards NKCC GABA Receptor	Metabolic Disease Cancer
Furosemide (Standard) is the analytical standard of Furosemide. This product is intended for research and analytical applications. Furosemide is a potent and orally active inhibitor of Na ⁺/K ⁺/2Cl ^- (NKCC) cotransporter, NKCC1 and NKCC2 ^[1]. Furosemide is also a GABA_A 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-W009009

L-838417	GABA Receptor	Neurological Disease
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 ^[1] .

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 ^[1] .

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) ^[1].

HY-103520

DS2	GABA Receptor	Neurological Disease
DS2 is a selective positive allosteric modulator of **δ-GABA_A receptor*. DS2 selectively potentiates GABA* responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research ^[1].

HY-B1803A

Tracazolate hydrochloride ICI 136753 hydrochloride	GABA Receptor	Neurological Disease
Tracazolate (ICI 136753) hydrochloride is a potent *GABA_A* receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC₅₀=13.2 μM), α1β3γ2 (EC₅₀=1.5 μM). Tracazolate hydrochloride has the potency (EC₅₀) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity ^[1] .

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 ^[1] .

HY-Y0313R

p-Hydroxybenzaldehyde (Standard)	Reference Standards Endogenous Metabolite GABA Receptor	Neurological Disease
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-168758

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

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 ^[1].

HY-19371

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

HY-Y0313S

p-Hydroxybenzaldehyde-d4	Isotope-Labeled Compounds Endogenous Metabolite GABA Receptor	Neurological Disease
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-118502

DOV51892	GABA Receptor	Neurological Disease
DOV51892 is a **GABA_A receptor** modulator. DOV51892 has a specific effect on GABA_A receptors containing the α1 subunit. DOV51892 exhibits non-sedative anti-anxiety effects. DOV51892 can be used for in-depth research on the function of GABA_A receptors ^[1].

HY-Y0313S1

p-Hydroxybenzaldehyde-13C	Isotope-Labeled Compounds Endogenous Metabolite GABA Receptor	Neurological Disease
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	Isotope-Labeled Compounds GABA Receptor Endogenous Metabolite	Neurological Disease
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-103512

TP003	GABA Receptor	Neurological Disease
TP003 is a non-selective benzodiazepine site agonist with EC₅₀s of 20.3, 10.6, 3.24, 5.64 nM for *α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABA_A* receptors ^[1].

HY-100991R

FG 7142 (Standard) ZK 39106 (Standard); LSU-65 (Standard)	Reference Standards GABA Receptor	Neurological Disease
FG 7142 (Standard) is the analytical standard of FG 7142. This product is intended for research and analytical applications. FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=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 ^[1].

HY-103510

TB-21007	GABA Receptor	Neurological Disease
TB-21007 is a selective and brain penetrant α5 subunit-containing **GABAA receptor inverse agonist with K_i**s of 1.6 nM, 20 nM, 16 nM, and 20 nM for α5, α1, α2 and α3 subtypes, respectively. TB-21007 enhances cognition in rats ^[1].

HY-100369AR

DMCM hydrochloride (Standard)	Reference Standards GABA Receptor	Neurological Disease
DMCM (hydrochloride) (Standard) is the analytical standard of DMCM (hydrochloride). This product is intended for research and analytical applications. DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively ^[1].

HY-B0135AR

Furosemide sodium (Standard)	NKCC GABA Receptor Reference Standards	Cardiovascular Disease Metabolic Disease Cancer
Furosemide (sodium) (Standard) is the analytical standard of Furosemide (sodium). This product is intended for research and analytical applications. Furosemide sodium is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2 ^[1]. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .

HY-115857

SH-053-S-CH3-2'F	GABA Receptor	Neurological Disease
SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs ^[1].

HY-131997

2'MeO6MF	GABA Receptor	Neurological Disease Inflammation/Immunology
2'MeO6MF is a brain-penetrant positive allosteric modulator at *α2β1γ2L* and all α1-containing **GABA_A receptors. 2'MeO6MF also can directly activate α2β2/3** and α2β2/3γ2L GABA_A receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response ^[1] .

HY-111052R

AZD7325 (Standard)	GABA Receptor Cytochrome P450	Neurological Disease Inflammation/Immunology
AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes ^[1] . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.

HY-W009009R

L-838417 (Standard)	Reference Standards GABA Receptor	Neurological Disease
L-838417 (Standard) is the analytical standard of L-838417 (HY-W009009). This product is intended for research and analytical applications. 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 ^[1] .

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 ^[1].

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 ^[1].

HY-135482

GABAA receptor agent 2 TFA	GABA Receptor	Neurological Disease
GABAA receptor agent 2 TFA is a potent and high-affinity **GABA_A receptor antagonist with an IC₅₀** of 24 nM (human α1β2γ2 GABA_A-expressing tsA201 cells) and a K_i of 28 nM (rat GABA_A receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) ^[1].

HY-B1494R

Picrotoxinin (Standard)	Reference Standards Chloride Channel GABA Receptor	Neurological Disease
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 ^[1].

HY-175251

GABAA receptor modulator-9	GABA Receptor	Neurological Disease
GABAA receptor modulator-9 is and positive allosteric modulator of a1β2y2 subtype *GABA_A* that can cross the blood-brain barrier. GABAA receptor modulator-9 exhibits comparable activity on α1β2γ2 (EC₅₀: 0.9 μM in oocytes, 0.2 μM in CHO cells) and on α1β2, α3β2γ2 and α1β3γ2 (EC₅₀s of 1.3, 3.4 and 1.1 μM). GABAA receptor modulator-9 significantly suppresses seizure progression and reduces delayed mortality. GABAA receptor modulator-9 can be used for the study of status epilepticus (SE) ^[1].

Cat. No.	Nom du produit	Category	Target	Chemical Structure

HY-B1494

Picrotoxinin 4 Publications Verification	Structural Classification other families Terpenoids Sesquiterpenes Plants Source Classification	Chloride Channel GABA Receptor
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive **GABA_A receptor** antagonist, which negatively modulates the action of GABA on GABA_A receptors. Picrotoxinin inhibits α₁β₂γ_2L GABA_A receptor with an IC₅₀ of 1.15 μM ^[1].

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-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-B1494R

Picrotoxinin (Standard)	Structural Classification Productos naturales 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 ^[1].

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 ^[1] .

Cat. No.	Compare	Nom du produit	Species	Source	Image

HY-P703130

	GABRA1-GABRB2-GABRG2 Protein, Human (HEK293, Strep) Gamma-aminobutyric acid receptor subunit alpha-1; GABA(A) receptor subunit alpha-1; GABAAR subunit alpha-1; GABRA1; Homo sapiens; Human; Chloride channel; Ion channel; Ligand-gated ion channel; receptor	Human	HEK293

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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 ^[1].

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 ^[1].?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-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-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-W013150S

Alpidem-d14

Alpidem-d₁₄ is the deuterium labeled Alpidem (HY-W013150) ^[1]. 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-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 ^[1] .

HY-Y0313S2

p-Hydroxybenzaldehyde-d5
p-Hydroxybenzaldehyde-d₅ is the deuterium labeled p-Hydroxybenzaldehyde ^[1]. 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 .

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