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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
88 Results for "
GABAB
" in MedChemExpress (MCE) Product Catalog:
Products (88)
88 Results for "GABAB" in MCE Product Catalog:
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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 .
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13 Publications Verification
Cat. No.: HY-B0007C
CAS No.: 28311-31-1
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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 .
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8 Cited Publications
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CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
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5 Cited Publications
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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 .
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(R)-Baclofen (Arbaclofen) is a selective GABAB receptor agonist .
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2 Cited Publications
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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 .
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2 Cited Publications
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CGP55845 hydrochloride is a potent and selective GABAB receptor antagonist with an IC50 of 6 nM. CGP55845 hydrochloride can be used for neurological research .
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2 Cited Publications
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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 .
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2 Cited Publications
Cat. No.: HY-17354A
CAS No.: 63701-55-3
Synonyms: Arbaclofen hydrochloride; STX 209 hydrochloride
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(R)-Baclofen hydrochloride (Arbaclofen hydrochloride) is a selective GABAB receptor agonist .
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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 .
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1 Cited Publications
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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 .
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1 Cited Publications
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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 .
Synonyms: β-Phenyl-GABA; 4-Amino-3-phenylbutanoic acid
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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 .
Cat. No.: HY-W041333
CAS No.: 3060-41-1
Synonyms: β-Phenyl-GABA hydrochloride; 4-Amino-3-phenylbutanoic acid hydrochloride; 4-Amino-3-phenylbutyric acid hydrochloride
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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 .
Cat. No.: HY-118301
CAS No.: 1207440-88-7
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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 .
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rac-BHFF is a potent and orally active allosteric enhancer of GABAB receptor .
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
