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Baclofen

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ERK (2) GABA Receptor (17) Isotope-Labeled Compounds (1)
By Research Areas:	Endocrinology (1) Inflammation/Immunology (1) Neurological Disease (20)

Inhibitors & Agonists

Biochemical Assay Reagents

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0007

*Baclofen* Maximum Cited Publications 6 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-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-17354

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

HY-100798

Phaclofen	GABA Receptor	Neurological Disease
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-100813

Saclofen 3 Publications Verification	GABA Receptor	Neurological Disease Inflammation/Immunology
Saclofen is an orally available competitive GABA_B receptor antagonist with an IC₅₀ of 7.8 μM, but it has a weaker antagonistic effect on GABA_B1b and GABA_B2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats .

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-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-B0007S2

Baclofen-d5 hydrochloride	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 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-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-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-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-119256

COR627	Others	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 .

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-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-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-123525

COR628	Others	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 .

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 .

HY-114076

CGP55845	Others	Neurological Disease
CGP55845 is a potent and selective GABAB receptor antagonist with activity that blocks agonist binding. The IC50 value of CGP55845 is 5 nM, indicating that it exhibits significant activity in inhibiting GABA and glutamate release. The apparent Kd of CGP55845 when forming a complex with the GABAB receptor is 30 nM, indicating its high affinity for this receptor. CGP55845 is as potent as 100 μM CGP 35348 in relieving the inhibitory effect of (R)-(-)-baclofen .

HY-129636A

(E/Z)-CLH304a 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 GABA_B receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .

HY-129636

CLH304a (E)-GABAB receptor antagonist 1	GABA Receptor ERK	Neurological Disease
CLH304a (compound 14) is a specific and noncompetitive GABA_B 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 GABA_B receptor .

3-Amino-3-phenylpropionic acid DL-β-Phenylalanine	Biochemical Assay Reagents
3-Amino-3-phenylpropionic acid (DL-β-Phenylalanine) is a structural GABA analogue. 3-Amino-3-phenylpropionic acid inhibits baclofen (HY-B0007) induced gastric acid secretion .

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].

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-B0007S2

Baclofen-d5 hydrochloride
Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). 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 .

Baclofen-d5 hydrochloride

Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). 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 .

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