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GABAB

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Calcium Channel (1) Endogenous Metabolite (6) GABA Receptor (45) Isotope-Labeled Compounds (3) nAChR (1)
By Research Areas:	Metabolic Disease (3) Neurological Disease (41)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-129636

*(E)-GABAB* receptor antagonist 1**	GABA Receptor	Neurological Disease
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC₅₀ of 37.9 μM .

HY-103516

CGP55845 hydrochloride	GABA Receptor	Neurological Disease
CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC₅₀ of 6 nM. CGP55845 hydrochloride can be used for neurological research .

HY-160105

GABAB receptor antagonist 3

GABA Receptor Neurological Disease

GABAB receptor antagonist 3 (example 3) is a antagonist of GABAB receptor .
HY-123301

GABAB receptor antagonist 2

GABA Receptor Others

GABAB receptor antagonist 2 is a GABAB receptor/b> antagonist .

GABAB receptor antagonist 3	GABA Receptor	Neurological Disease
GABAB receptor antagonist 3 (example 3) is a antagonist of GABAB receptor .

GABAB receptor antagonist 2	GABA Receptor	Others
GABAB receptor antagonist 2 is a GABAB receptor/b> antagonist .

HY-129636A

GABAB receptor antagonist 1	GABA Receptor	Neurological Disease
GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC₅₀ of 37.9 μM .

HY-10061

Lesogaberan AZD-3355	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan 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 inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

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-10061A

Lesogaberan napadisylate AZD-3355 napadisylate	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan napadisylate 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 napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

HY-115763

3-Aminopropylphosphinic acid 3-APPA; CGP 27492; CGA 147823	GABA Receptor	Neurological Disease
3-Aminopropylphosphinic acid (3-APPA) is a phosphonic analog of GABA. 3-Aminopropylphosphinic acid is a potent, selective *GABA_B* receptor agonist .

HY-128469

Inaperisone	GABA Receptor	Neurological Disease
Inaperisone is a centrally acting muscle relaxant. Inaperisone can inhibit the micturition reflex by acting indirectly on GABAB receptors in the brainstem .

HY-103530

CGP35348	GABA Receptor	Neurological Disease
CGP 35348 is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC₅₀ of 34 μM. CGP 35348 shows affinity for the GABAB receptor only . CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage .

HY-103502

CGP7930	GABA Receptor	Neurological Disease
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive *metabotropic GABAB* receptor** allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons .

HY-101378

CGP 54626 hydrochloride	GABA Receptor	Neurological Disease
CGP 54626 (hydrochloride) is a selective antagonist of GABA_B receptor with an IC₅₀ value of 4 nM. CGP 54626 (hydrochloride) can be used to investigate the role of GABA_B receptors in neurological signaling .

HY-100813

Saclofen 3 Publications Verification
Saclofen is a competitive antagonist of the GABA_B receptor with an IC₅₀ of 7.8 μM. Saclofen can be used to determine the functional roles for the GABA_B receptor as a mediator of slow inhibitory postsynaptic potentials in the brain .

HY-12783

SCH 50911 hydrochloride	GABA Receptor	Neurological Disease
SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B *GABA(B)* receptor antagonist, binds to GABA(B) receptor with IC₅₀ of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated ³H overflow with an IC₅₀ of 3 μM.

HY-103531

CGP52432

3 Publications Verification

GABA Receptor Neurological Disease

CGP52432 is a GABA_B receptor antagonist, with an IC₅₀ of 85 nM.

CGP52432 3 Publications Verification	GABA Receptor	Neurological Disease
CGP52432 is a GABA_B receptor antagonist, with an IC₅₀ of 85 nM.

HY-12783A

SCH 50911	GABA Receptor	Neurological Disease
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B *GABA(B)* receptor antagonist, binds to GABA(B) receptor with IC₅₀ of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated ³H overflow with an IC₅₀ of 3 μM .

HY-17354

(R)-Baclofen

2 Publications Verification

Arbaclofen; STX209
GABA Receptor Neurological Disease

(R)-Baclofen (Arbaclofen) is a selective GABAB receptor agonist .
HY-103668A

SSD114 hydrochloride

GABA Receptor Neurological Disease

SSD114 hydrochloride is a novel GABA_B receptor positive allosteric modulator.

(R)-Baclofen 2 Publications Verification Arbaclofen; STX209	GABA Receptor	Neurological Disease
(R)-Baclofen (Arbaclofen) is a selective GABAB receptor agonist .

SSD114 hydrochloride	GABA Receptor	Neurological Disease
SSD114 hydrochloride is a novel GABA_B receptor positive allosteric modulator.

HY-17354A

(R)-Baclofen hydrochloride Arbaclofen hydrochloride; STX 209 hydrochloride	GABA Receptor	Neurological Disease
(R)-Baclofen hydrochloride (Arbaclofen hydrochloride) is a selective GABAB receptor agonist .

HY-103519

rac-BHFF

GABA Receptor Neurological Disease

rac-BHFF is a potent and orally active allosteric enhancer of GABA_B receptor .
HY-W105694

3-Aminopropylphosphonic acid

(3-Aminopropyl)phosphonic acid
GABA Receptor Neurological Disease

3-Aminopropylphosphonic acid is a GABAB receptor agonist with IC₅₀ value of 1.5 μM .
HY-103503

CGP13501

GABA Receptor Neurological Disease

CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol .

rac-BHFF	GABA Receptor	Neurological Disease
rac-BHFF is a potent and orally active allosteric enhancer of GABA_B receptor .

3-Aminopropylphosphonic acid (3-Aminopropyl)phosphonic acid	GABA Receptor	Neurological Disease
3-Aminopropylphosphonic acid is a *GABAB* receptor agonist with IC₅₀ value of 1.5 μM .

CGP13501	GABA Receptor	Neurological Disease
CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol .

HY-14735

Arbaclofen placarbil XP 19986	GABA Receptor	Neurological Disease
Arbaclofen placarbil is a novel transported proagent of the active R-isomer of baclofen. Baclofen is a racemic GABA_B receptor agonist

HY-B0007

Baclofen 4 Publications Verification	GABA Receptor	Neurological Disease
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA_B receptor (GABA_BR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

HY-B0007C

Baclofen hydrochloride	GABA Receptor	Neurological Disease
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA_B receptor (GABA_BR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research .

HY-137204

COR659	GABA Receptor	Neurological Disease
COR659 is a potent and effective GABA_B positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats .

HY-100915

SKF 97541 CGP 35024	GABA Receptor	Neurological Disease
SKF 97541 (CGP 35024) is a potent and selective *GABA_B* agonist that can induce hyperpotential. SKF 97541 has antiepileptic activity .

HY-B0007S

Baclofen-d4	GABA Receptor	Neurological Disease
Baclofen-d₄ is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].

HY-B0007R

Baclofen (Standard)	GABA Receptor	Neurological Disease
Baclofen (Standard) is the analytical standard of Baclofen. This product is intended for research and analytical applications. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA_B receptor (GABA_BR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

HY-137429

Valiloxibic acid Acidum valiloxibicum; XWL-008	GABA Receptor	Neurological Disease
Valiloxibic acid is a proagent of γ-Hydroxybutyric acid (GHB).GHB is a naturally occurring neurotransmitter and a psychoactive agent, it acts on the GHB receptor and is a weak agonist at the GABAB receptor .

HY-121599

CGP 36742 SGS-742	GABA Receptor	Neurological Disease
CGP 36742 is a selective GABA_B receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC₅₀ of 32 μM. CGP 36742 is useful in treatment of depression .

HY-103532

CGP46381	GABA Receptor	Neurological Disease
CGP 46381 is an orally active *GABA_B* receptor antagonist with IC₅₀ of 4.9 μM. CGP 46381 blocks the neuronal depression induced by iontophoretically applied baclofen (HY-B0007) .

HY-118301

ADX71441	GABA Receptor	Neurological Disease
ADX71441 is a potent and selective positive allosteric modulator of the *GABA_B* receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity .

HY-103518

CGP36216	GABA Receptor	Neurological Disease
CGP36216 is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a K_i value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .

HY-103518A

CGP36216 hydrochloride	GABA Receptor	Neurological Disease
CGP36216 hydrochloride is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a K_i value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .

HY-100798

Phaclofen
Phaclofen is a selective GABA_B receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact .

HY-135034

UMB68 sodium	GABA Receptor	Neurological Disease
UMB68 sodium is a selective GHB receptor ligand. UMB68 sodium displaces [ ³H]NCS-382 with an IC₅₀ of 38 nM in rat cerebrocortical membranes. UMB68 sodium has no significant affinity at GABAB receptors, cannot be metabolized to GABA-active compounds .

HY-N0067

γ-Aminobutyric acid 3 Publications Verification 4-Aminobutyric acid	GABA Receptor Endogenous Metabolite	Neurological Disease
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-101359

TPMPA	GABA Receptor	Neurological Disease
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABA_C receptor (K_B = 2.1 μM), but not to interact with GABA_A (K_B = 320 μM) or GABA_B receptors (EC₅₀ = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells .

HY-100812

2-Hydroxysaclofen
2-Hydroxysaclofen is a potent *γ-amino-butyric-acid-B (GABA_B)* receptor** antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats .

HY-N0067S1

γ-Aminobutyric acid-d2 4-Aminobutyric acid-d₂	Isotope-Labeled Compounds GABA Receptor Endogenous Metabolite	Neurological Disease
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-N0067S

γ-Aminobutyric acid-d6 4-Aminobutyric acid-d₆	GABA Receptor Endogenous Metabolite	Neurological Disease
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[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

HY-N0067S3

γ-Aminobutyric acid-13C4 4-Aminobutyric acid-¹³C₄	Isotope-Labeled Compounds GABA Receptor Endogenous Metabolite	Neurological Disease
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[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

HY-N0067S2

γ-Aminobutyric acid-4,4-d2 4-Aminobutyric acid-4,4-d₂	Isotope-Labeled Compounds GABA Receptor Endogenous Metabolite	Neurological Disease
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-P5146

α-Conotoxin PeIA	nAChR Calcium Channel GABA Receptor	Neurological Disease
α-Conotoxin PeIA is an analgesic α-conotoxin.α-Conotoxin PeIA inhibits the α6β4, α9α10 and α3β2 nAChR.α-Conotoxin PeIA is also a potent inhibitor of N-type calcium channel via GABAB receptor activation .

HY-N0067R

γ-Aminobutyric acid (Standard) 4-Aminobutyric acid (Standard)	Endogenous Metabolite GABA Receptor	Neurological Disease
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 (GABA_A receptors) and metabotropic receptors (GABA_B receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .

HY-103475

GS39783	GABA Receptor	Neurological Disease
GS39783 is a positive allosteric modulator (PAM) of GABA_BR. Positive modulation of the GABA_BR can be used for the research of Nicotine addiction .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0067

γ-Aminobutyric acid 3 Publications Verification 4-Aminobutyric acid	Structural Classification Animals Ketones, Aldehydes, Acids Source classification Endogenous metabolite	GABA Receptor Endogenous Metabolite
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-N0067R

γ-Aminobutyric acid (Standard) 4-Aminobutyric acid (Standard)	Structural Classification Animals Ketones, Aldehydes, Acids Source classification Endogenous metabolite	Endogenous Metabolite GABA Receptor
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 (GABA_A receptors) and metabotropic receptors (GABA_B receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .

Cat. No.	Product Name	Chemical Structure

HY-B0007S

Baclofen-d4

Baclofen-d₄ is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].

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-N0067S

γ-Aminobutyric acid-d6
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[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

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[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].

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].

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GABAB

Inhibitors & Agonists

Screening Libraries

Peptides

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Isotope-Labeled Compounds

Antibodies

Natural
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