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Results for "

GABAA agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (5) Apoptosis (1) Cytochrome P450 (1) Dopamine Receptor (1) Drug Metabolite (1) Endogenous Metabolite (1) GABA Receptor (72) Histamine Receptor (1) Isotope-Labeled Compounds (2) Keap1-Nrf2 (1) Sirtuin (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (2) Inflammation/Immunology (3) Metabolic Disease (4) Neurological Disease (66)
Click Chemistry:	Azide (1) Alkynes (1)

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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-100991R

FG 7142 (Standard) ZK 39106 (Standard); LSU-65 (Standard)	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-100369AR

DMCM hydrochloride (Standard)	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-19308

RWJ-51204	GABA Receptor	Neurological Disease
RWJ-51204 is a partial agonist of GABA(A) receptor, with K_i of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

HY-106851

Panadiplon FG 10571; PNU 78875	GABA Receptor	Neurological Disease
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a *5GABAA* partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .

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-Y1176

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

HY-117257

PF-0713	GABA Receptor	Cancer
PF 0713 is a *GABAA* receptor agonist. .

HY-168986

Moxetomidate	GABA Receptor	Neurological Disease
Moxetomidate is a GABAA receptor agonist with hypnotic effect .

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-129927

Thiomuscimol	GABA Receptor	Others
Thiomuscimol is a GABAA receptor agonist (IC₅₀=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.

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 .

HY-103501

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

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-101639

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

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-Y1176S

Isonipecotic acid-d9	GABA Receptor	Neurological Disease
Isonipecotic acid-d₉ is the deuterium labeled Isonipecotic acid[1]. Isonipecotic acid is a GABAA receptor partial agonist[2].

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-100370

MRK-016	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-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-103498

Org20599	GABA Receptor	Neurological Disease
Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABA_A receptor with an EC₅₀ of 1.1 μM .

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 .

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-B0007B

(S)-Baclofen	GABA Receptor	Neurological Disease
(S)-Baclofen is a selective GABAB receptor agonist with the IC₅₀ values of 1.77 μM and 1564 μM for GABAB and *GABAA*, respectively .

HY-14426

L-655708 3 Publications Verification	GABA Receptor	Neurological Disease
L-655708 is a potent α5 subunit-selective *GABAA* receptor inverse agonist (K_i=0.45 nM).

HY-116622

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

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-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-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-100799

ZAPA sulfate	GABA Receptor	Neurological Disease
ZAPA sulfate is an agonist at low affinity *GABA_A-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris* muscle cell with an EC₅₀ of 10.3 μM .

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-123426

JY-XHe-053	GABA Receptor
JY-XHe-053 is a potent and selective agonist of *GABAA* receptors containing the α5 subunit (K_is of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors .

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-114706

Suritozole MDL-26479	GABA Receptor	Neurological Disease
Suritozole (MGL-26479) is a cognitive enhancer that acts as a partial inverse agonist of benzodiazepine receptor sites on *GABAA* ion channel complexes. Suritozole can be used in the study of neurodegenerative diseases .

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-103510

TB-21007	GABA Receptor	Neurological Disease
TB-21007 is an inverse agonist of α₅β₃γ₂ subunit-containing GABA_A receptor with a K_i of 1.6 nM. TB-21007 enhanced spatial memory in rats .

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-103524R

Valerenic acid (Standard) (-)-Valerenic Acid (Standard)	5-HT Receptor GABA Receptor	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-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-10232R

THIP (Standard) Gaboxadol (Standard)	GABA Receptor	Neurological Disease
THIP (Standard) is the analytical standard of THIP. This product is intended for research and analytical applications. 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[1][2][3].

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-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-10232S

THIP-d4 Gaboxadol-d₄	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
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-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-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-129105

Clomethiazole 3 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 .

Cat. No.	Product Name	Type

HY-D1704

Bodipy TMR-X muscimol	Fluorescent Dyes/Probes
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 .

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-113329

Guanidinoethyl sulfonate Taurocyamine	Structural Classification Natural Products Other disease Classification of Application Fields Disease markers Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
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 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 .

Cat. No.	Product Name	Chemical Structure

HY-15831

L-838417-d9
L-838417-d₉ is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

HY-Y1176S

Isonipecotic acid-d9
Isonipecotic acid-d₉ is the deuterium labeled Isonipecotic acid[1]. Isonipecotic acid is a GABAA receptor partial agonist[2].

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 .

Cat. No.	Product Name		Classification

HY-103476

Ro15-4513		Azide
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.