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GABA_B receptor

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0067
    γ-Aminobutyric acid
    5 Publications Verification

    4-Aminobutyric acid

    Environmental Pollutants Endogenous Metabolite GABA Receptor Neurological Disease Metabolic Disease
    γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .
    γ-Aminobutyric acid
  • HY-B0007
    Baclofen
    Maximum Cited Publications
    12 Publications Verification

    GABA Receptor Neurological Disease
    Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist with blood-brain barrier permeability. 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 .
    Baclofen
  • HY-17354
    (R)-Baclofen
    2 Publications Verification

    Arbaclofen; STX209

    GABA Receptor Neurological Disease Cancer
    (R)-Baclofen (Arbaclofen) is a selective GABAB receptor agonist .
    (R)-Baclofen
  • HY-100813
    Saclofen
    5 Publications Verification

    GABA Receptor Neurological Disease Inflammation/Immunology
    Saclofen is an orally active and a competitive GABAB receptor antagonist with an IC50 of 7.8 μM. Saclofen has weak antagonistic effects on GABAB1b and GABAB2 heterodimeric recombinant receptors. Saclofen inhibits the binding of Baclofen (HY-B0007) to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts, and exhibits anti-inflammatory and analgesic effects in rats .
    Saclofen
  • HY-N0067S
    γ-Aminobutyric acid-d6
    2 Publications Verification

    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 , binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors) .
    γ-Aminobutyric acid-d6
  • HY-103531
    CGP52432
    5+ Cited Publications

    GABA Receptor Neurological Disease
    CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
    CGP52432
  • HY-103530
    CGP35348
    2 Publications Verification

    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 .
    CGP35348
  • HY-B0007C
    Baclofen hydrochloride
    Maximum Cited Publications
    12 Publications Verification

    GABA Receptor Neurological Disease
    Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research .
    Baclofen hydrochloride
  • HY-N0067R
    γ-Aminobutyric acid (Standard)
    5 Publications Verification

    4-Aminobutyric acid (Standard)

    Endogenous Metabolite GABA Receptor Reference Standards 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 (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system .
    γ-Aminobutyric acid (Standard)
  • HY-108403

    β-Phenyl-GABA; 4-Amino-3-phenylbutanoic acid

    GABA Receptor Neurological Disease
    Phenibut (β-Phenyl-GABA) is a GABA-B agonist . Phenibut acts as a GABA-mimetic, primarily at GABAB receptors. Phenibut has anxiolytic and nootropic (cognition enhancing) effects .
    Phenibut
  • HY-W041333

    β-Phenyl-GABA hydrochloride; 4-Amino-3-phenylbutanoic acid hydrochloride; 4-Amino-3-phenylbutyric acid hydrochloride

    GABA Receptor Neurological Disease
    Phenibut (β-Phenyl-GABA) hydrochloride is an orally active GABA-B agonist . Phenibut hydrochloride acts as a GABA-mimetic, primarily at GABAB?receptors. Phenibut hydrochloride has anxiolytic and nootropic (cognition enhancing) effects .
    Phenibut hydrochloride
  • HY-103516
    CGP55845 hydrochloride
    1 Publications Verification

    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 .
    CGP55845 hydrochloride
  • HY-121599
    CGP 36742
    1 Publications Verification

    SGS-742

    GABA Receptor Neurological Disease
    CGP 36742 (SGS-742) is an orally active and selective antagonist of GABAB receptor (IC50 = 36 µM). CGP 36742 is a brain-penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study .
    CGP 36742
  • HY-101378
    CGP 54626 hydrochloride
    2 Publications Verification

    GABA Receptor Neurological Disease
    CGP 54626 (hydrochloride) is a selective antagonist of GABAB receptor with an IC50 value of 4 nM. CGP 54626 (hydrochloride) can be used to investigate the role of GABAB receptors in neurological signaling .
    CGP 54626 hydrochloride
  • HY-103519

    GABA Receptor Neurological Disease
    rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor .
    rac-BHFF
  • HY-100798

    GABA Receptor Neurological Disease
    Phaclofen is a selective GABAB 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 .
    Phaclofen
  • HY-118301

    GABA Receptor 5-HT Receptor Neurological Disease
    ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABAB receptor. ADX71441 potentiates the activity of endogenous GABA at GABAB receptor, with an EC50 of 96 nM. ADX71441 functionally inhibits adenosine transporters and 5-HT2B receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity .
    ADX71441
  • HY-100812

    GABA Receptor Neurological Disease Endocrinology
    2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) 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 .
    2-Hydroxysaclofen
  • HY-12783A

    GABA Receptor Neurological Disease
    SCH 50911 is a selective, orally active, blood-brain barrier permeable GABA-B receptor (GABA-B Receptor) antagonist with an IC50 of 1.1 μM in rats. SCH 50911 blocks baclofen-induced antitussive effects, regulates neuronal firing and GABA release. SCH 50911 promotes spontaneous seizures during withdrawal in ethanol-dependent rats, alters reward-related neurotransmission, and reduces or suppresses lever responding and self-administration behaviors of alcohol and sucrose in rats. SCH 50911 is applicable to research related to ethanol withdrawal syndrome, absence epilepsy and alcohol use disorder .
    SCH 50911
  • HY-10061B

    AZD-3355 hydrochloride

    GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA 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 .
    Lesogaberan hydrochloride
  • HY-103668A

    GABA Receptor Neurological Disease
    SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
    SSD114 hydrochloride
  • HY-103503

    GABA Receptor Neurological Disease
    CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol .
    CGP13501
  • HY-N0067S3

    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 , binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors) .
    γ-Aminobutyric acid-13C4
  • HY-101359

    GABA Receptor Neurological Disease
    TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells .
    TPMPA
  • HY-N0067S1

    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].
    γ-Aminobutyric acid-d2
  • HY-129636

    (E)-GABAB receptor antagonist 1

    GABA Receptor ERK Neurological Disease
    CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
    CLH304a
  • HY-103502
    CGP7930
    1 Publications Verification

    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 .
    CGP7930
  • HY-17354A
    (R)-Baclofen hydrochloride
    2 Publications Verification

    Arbaclofen hydrochloride; STX 209 hydrochloride

    GABA Receptor Neurological Disease
    (R)-Baclofen hydrochloride (Arbaclofen hydrochloride) is a selective GABAB receptor agonist .
    (R)-Baclofen hydrochloride
  • HY-W105694

    (3-Aminopropyl)phosphonic acid

    GABA Receptor Neurological Disease
    3-Aminopropylphosphonic acid ((3-Aminopropyl)phosphonic acid) is a phosphonic acid analogue of GABA and a GABAB receptor agonist .
    3-Aminopropylphosphonic acid
  • HY-174147

    GABA Receptor Neurological Disease
    GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist. GABAB receptor antagonist 4 can inhibit GABA-induced G protein activation. GABAB receptor antagonist 4 competitively binds to the orthosteric site of GABAB receptor. GABAB receptor antagonist 4 can be used to study GABAB receptor-related neurological diseases .
    GABAB receptor antagonist 4
  • HY-10061

    AZD-3355

    GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA 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 .
    Lesogaberan
  • HY-123301

    GABA Receptor Others
    GABAB receptor antagonist 2 is a GABAB receptor/b> antagonist .
    GABAB receptor antagonist 2
  • HY-168977

    RL-007; FSV7-007

    GABA Receptor Neurological Disease
    Inidascamine is the modulator for cholinergic, glutamatergic, and GABAB receptor, and can be used for researchs of schizophrenia .
    Inidascamine
  • HY-B0007A

    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 .
    (S)-Baclofen hydrochloride
  • HY-174152

    GABA Receptor Neurological Disease
    GABAB receptor antagonist 5 (Compound 23) is a competitive GABAB receptor antagonist. GABAB receptor antagonist 5 is promising for research of neuropsychiatric diseases, such as epilepsy, depression, and addiction .
    GABAB receptor antagonist 5
  • HY-160105

    GABA Receptor Neurological Disease
    GABAB receptor antagonist 3 (example 3) is a antagonist of GABAB receptor .
    GABAB receptor antagonist 3
  • HY-14735

    XP 19986

    GABA Receptor Neurological Disease
    Arbaclofen placarbil is a novel transported proagent of the active R-isomer of baclofen. Baclofen is a racemic GABAB receptor agonist
    Arbaclofen placarbil
  • HY-115763

    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 GABAB receptor agonist .
    3-Aminopropylphosphinic acid
  • HY-B0007S2

    GABA Receptor Isotope-Labeled Compounds Neurological Disease
    Baclofen-d5 hydrochloride is deuterated labeled Baclofen (HY-B0007). 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 .
    Baclofen-d5 hydrochloride
  • HY-B0007R

    Reference Standards 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 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 .
    Baclofen (Standard)
  • HY-103518

    GABA Receptor Neurological Disease
    CGP36216 is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .
    CGP36216
  • HY-103532

    GABA Receptor Neurological Disease
    CGP 46381 is an orally active GABAB receptor antagonist with IC50 of 4.9 μM. CGP 46381 blocks the neuronal depression induced by iontophoretically applied baclofen (HY-B0007) .
    CGP46381
  • HY-P10898

    nAChR Calcium Channel GABA Receptor Neurological Disease
    GeX-2 is a truncated analogue of αO-conotoxin. GeX-2 activates GABAB receptor. GeX-2 inhibits α9α10 nAChR and CaV2.2 channels. GeX-2 alleviates pain in the rat model of chronic constriction injury .
    GeX-2
  • HY-115856

    GABA Receptor Neurological Disease
    Sch 50910 is a GABA(B) receptor antagonist with some activity in inhibiting GABA(B) autoreceptors. Sch 50910 had no effect on electrically stimulated release at a concentration of 100 μM. The activity of Sch 50910 suggests that it may not have a significant role in studies of GABA(B) receptor function .
    Sch 50910
  • HY-129636A

    GABAB receptor antagonist 1

    GABA Receptor ERK Neurological Disease
    (E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
    (E/Z)-CLH304a
  • HY-123222

    GABA Receptor Neurological Disease
    CGP 56999 is a potent antagonist GABA(B) receptor, with the IC50 of 0.002 μM. CGP 56999 increased the levels of BDNF mRNA in the brain in vivo and in vitro .
    CGP 56999
  • HY-12783

    GABA Receptor Neurological Disease
    SCH 50911 dihydrochloride is a selective, orally active, blood-brain barrier permeable GABA-B receptor (GABA-B Receptor) antagonist with an IC50 of 1.1 μM in rats. SCH 50911 dihydrochloride blocks baclofen-induced antitussive effects, regulates neuronal firing and GABA release. SCH 50911 dihydrochloride promotes spontaneous seizures during withdrawal in ethanol-dependent rats, alters reward-related neurotransmission, and reduces or suppresses lever responding and self-administration behaviors of alcohol and sucrose in rats. SCH 50911 dihydrochloride is applicable to research related to ethanol withdrawal syndrome, absence epilepsy and alcohol use disorder .
    SCH 50911 hydrochloride
  • HY-119256

    GABA Receptor Neurological Disease
    COR627 is a GABA receptor positive allosteric modulator with the ability to enhance GABA activity. COR627 exhibits effects on GABA and baclofen stimulation in rat cortical membranes and can increase its affinity for GABA(B) receptors. In vivo experiments have shown that COR627 can enhance the sedative/hypnotic effects of baclofen at pretreatment ineffective doses .
    COR627
  • HY-130670

    GABA Receptor Neurological Disease
    CGP 54626 is a GABAB receptor modulator, which is essential in the central and peripheral nervous systems. It is used as a tool to identify and characterize GABAB receptor agonists and antagonists, which will aid in the development of drugs targeting diseases related to these systems. This discovery involves purified GABAB receptors, receptor proteins and their encoding nucleic acids, facilitating the study of new members of the GABAB receptor family through DNA cloning technology and sequence-derived probes .
    CGP 54626
  • HY-123525

    GABA Receptor Neurological Disease
    COR628 is a positive allosteric modulator of GABA(B) receptors with the activity of enhancing GABA-induced GTPγS stimulation. COR628 showed significant activity in in vitro studies but did not exhibit endogenous agonist activity. COR628 has shown efficacy in experiments in mice by enhancing the sedation/hypnosis induced by baclofen, shortening the onset time and extending the duration of loss of righting reflex when combined with non-sedating doses of baclofen . The cytotoxic effect of COR628 is comparable to or higher than that of GS39783 or BHF177 in concentration .
    COR628

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