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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
16 Results for "
GABA binding site
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "GABA binding site" in MCE Product Catalog:
2
2 Cited Publications
Synonyms: S44819; Egis-13529
Target:
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Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .
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3-Methoxyphenol is an environmental pollutant. 3-Methoxyphenol occurs in the aroma components of dried bonito. 3-Methoxyphenol potentially enhances GABA-evoked responses of α1β1 GABAA receptors by increasing the affinity of GABA binding sites. 3-Methoxyphenol is used as a flavoring substance in food and animal feed. 3-Methoxyphenol prolongs pentobarbital-induced sleeping time and reduces elevated plus maze behavior .
Cat. No.: HY-W015050
CAS No.: 610-49-1
Synonyms: 1-Aminoanthracene
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1-Anthramine (1-aminoanthracene) is a fluorescent general anesthetic. potentiates GABAergic transmission with Kd = 0.1 mM, for binding to the general anesthetic site in horse spleen apoferritin (HSAF). 1-Anthramine fluorescence is enhanced when bound to HSAF. 1-Anthramine potentiates chloride currents elicited by GABA. 1-Anthramine can reversibly inhibit the movement of Xenopus laevis, with an EC50 value of 16 μM .
Cat. No.: HY-129927
CAS No.: 62020-54-6
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Thiomuscimol is a GABAA receptor agonist (IC50=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.
Cat. No.: HY-108035
CAS No.: 1013427-48-9
Synonyms: MR04A3
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(-)-JM-1232 (MR04A3) targets GABA A receptors and exerts its analgesic effects by binding to the benzodiazepine binding site of GABA A receptors. (-)-JM-1232 demonstrates potent analgesic effects in mice against acute thermal stimuli, mechanically induced pain, and visceral pain, with CI50 values of 2.96, 3.06, and 2.27 mg/kg, respectively. (-)-JM-1232 can be used in research related to pain and analgesia .
Cat. No.: HY-147735
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GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .
Cat. No.: HY-147736
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GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .
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3-Methoxyphenol (Standard) is the analytical standard of 3-Methoxyphenol (HY-Y1840). This product is intended for research and analytical applications. 3-Methoxyphenol is an environmental pollutant. 3-Methoxyphenol occurs in the aroma components of dried bonito. 3-Methoxyphenol potentially enhances GABA-evoked responses of α1β1 GABAA receptors by increasing the affinity of GABA binding sites. 3-Methoxyphenol is used as a flavoring substance in food and animal feed. 3-Methoxyphenol prolongs pentobarbital-induced sleeping time and reduces elevated plus maze behavior .
Cat. No.: HY-Y1840S
CAS No.: 104714-88-7
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3-Methoxyphenol-d3 is the d3-labeled 3-Methoxyphenol (HY-Y1840). 3-Methoxyphenol is an environmental pollutant. 3-Methoxyphenol occurs in the aroma components of dried bonito. 3-Methoxyphenol potentially enhances GABA-evoked responses of α1β1 GABAA receptors by increasing the affinity of GABA binding sites. 3-Methoxyphenol is used as a flavoring substance in food and animal feed. 3-Methoxyphenol prolongs pentobarbital-induced sleeping time and reduces elevated plus maze behavior .
Cat. No.: HY-129090
CAS No.: 77779-50-1
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CGS-9895 is a GABA antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors .
Cat. No.: HY-183471
CAS No.: 34966-41-1
Synonyms: SQ 65396
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Cartazolate (SQ 65396) is a pyrazolopyridine modulator with benzodiazepine receptor agonist activity and cyclic AMP phosphodiesterase inhibitory activity. Cartazolate enhances the affinity of 3H-diazepam for brain-specific binding sites, regulates the GABA/benzodiazepine receptor complex, reversibly increases Na +-independent GABA receptor binding sites, and stimulates the binding of [ 3H]flunitrazepam to cerebellar membranes. Cartazolate restores punishment-suppressed behavior and exhibits anxiolytic properties. Cartazolate is applicable to anxiety-related research .
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GABA-IN-4 (Compound 17) is a N-(indol-3-ylglyoxylyl)benzylamine derivative. GABA-IN-4 exhibits high affinity for the benzodiazepine receptor (BzR) (binding site in GABAA receptor complex) with Ki value of 67 nM. Benzodiazepines are widely used as antianxiety, sedative-hypnotic and anticonvulsant agents .
Cat. No.: HY-189042
CAS No.: 738562-57-7
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EF1500 is a potent human GABA transporter 1 (hGAT1) inhibitor and a lipophilic THPO analog. EF1500 occupies the binding site by forming a hydrogen bond with active residues of hGAT1 (such as Tyr139) through its exocyclic amino group, thereby blocking GABA reuptake. EF1500 can be used for research on central nervous system diseases .
Cat. No.: HY-114811
CAS No.: 25006-32-0
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Leptophos oxon, a metabolite of leptophos, is a GABAA receptor chloride channel inhibitor with an IC50 values of 89.6 μM. Leptophos oxon inhibits GABA-induced chloride influx, binds to GABAA receptor-associated TBPS sites, and inhibits TBPS binding to voltage-dependent chloride channels. Leptophos oxon is a insecticide. Leptophos oxon can be used for the research of neurological disease .
Cat. No.: HY-P992360
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Cat. No.: HY-L166
1,764 compounds
Ion channel is a membrane-binding enzyme whose catalytic site is an ion conduction pore, which is opened and closed in response to specific environmental stimuli (voltage, ligand concentration, membrane tension, temperature, etc.). Ion channel provide pores for the passive diffusion of ions on the biofilm. Due to their high selectivity for ion, ion channel are generally classified as sodium (Na+ ), potassium (K+ ), calcium (Ca2+ ), chloride (Cl- ), and non-specific cation channel. Ion channel is an important contributor to cell signal transduction and homeostasis. In addition to electrical signal transduction, ion channel also have many functions: regulating vascular smooth muscle contraction, maintaining normal cell volume, regulating glandular secretion, protein kinase activation, etc. Therefore, dysfunction of ion channel can lead to many diseases, and its mechanism research is particularly important.
MCE designs a unique collection of 1,764 small molecules related to ion channel, mainly targeting Na+ channel, K+ channel, Ca2+ channel, GABA receptor, iGluR, etc. It is an essential tool for research of cardiovascular diseases, Nervous system diseases and other diseases.
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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
