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Results for "

rat GABAB receptor

" in MedChemExpress (MCE) Product Catalog:

9

Inhibitors & Agonists

1

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-118301
    ADX71441

    		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-10061B
    Lesogaberan hydrochloride

    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-10061
    Lesogaberan

    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-P10898
    GeX-2

    		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-10061A
    Lesogaberan napadisylate

    AZD-3355 napadisylate

    		 GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) napadisylate 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 napadisylate 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 napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
    Lesogaberan napadisylate
  • 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 .
    UMB68 sodium
  • HY-119256
    COR627

    		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-10061BR
    Lesogaberan hydrochloride (Standard)

    AZD-3355 hydrochloride (Standard)

    		 GABA Receptor Reference Standards Metabolic Disease
    Lesogaberan (hydrochloride) (Standard) is the analytical standard of Lesogaberan (hydrochloride) (HY-10061B). This product is intended for research and analytical applications. 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 (Standard)

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