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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
11 Results for "
rat GABAB receptor
" in MedChemExpress (MCE) Product Catalog:
Products (11)
11 Results for "rat GABAB receptor" in MCE Product Catalog:
5
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 .
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 .
Synonyms: AZD-3355 hydrochloride
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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 .
Cat. No.: HY-10061
CAS No.: 344413-67-8
Synonyms: AZD-3355
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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 .
Cat. No.: HY-P10898
CAS No.: 2900996-95-2
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Cat. No.: HY-10061A
CAS No.: 477956-38-0
Synonyms: AZD-3355 napadisylate
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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 .
Cat. No.: HY-135034
CAS No.: 581099-89-0
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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 .
Cat. No.: HY-119256
CAS No.: 329221-34-3
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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 .
Cat. No.: HY-W1025152
CAS No.: 760947-97-5
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CPP-115 hydrochloride is an orally active, selective GABA-AT inhibitor with a Ki value of 9.7 μM. CPP-115 hydrochloride blocks GABA degradation and increases GABA levels in the brain. CPP-115 hydrochloride does not bind to GABA transporters, does not displace GABA from GABAA/GABAB receptors, and does not act as an agonist/antagonist of GABAC receptors. CPP-115 hydrochloride reduces cocaine-induced dopamine release, blocks cocaine-induced conditioned place preference, and suppresses seizure activity in a rat model of infantile spasms. CPP-115 hydrochloride can be used in research related to infantile spasms and epilepsy .
Cat. No.: HY-10061BR
CAS No.: 2925644-17-1
Synonyms: AZD-3355 hydrochloride (Standard)
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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 .
Cat. No.: HY-184060
CAS No.: 1704716-36-8
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ASP8062 is an orally active, blood-brain barrier-permeable selective GABAB receptor positive allosteric modulator. ASP8062 enhances GABA-mediated activation of GABAB receptors and strengthens GABAergic neurotransmission. ASP8062 reverses Reserpine (HY-N0480)-induced myalgia, regulates the sleep-wake cycle, increases delta wave power during non-REM sleep, and impairs motor coordination at high doses. ASP8062 penetrates the central nervous system with a half-life of 40-50 h. ASP8062 can be used in research related to opioid use disorder, fibromyalgia, chronic pain, and alcohol use disorder .
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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
