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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
68 Results for "
GABA binding
" in MedChemExpress (MCE) Product Catalog:
Products (68)
68 Results for "GABA binding" in MCE Product Catalog:
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CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 enhances GABA in Xenopus laevis oocytes . CGS 20625 can be used for the research of pentylenetetrazol-induced seizures and anxiety .
Cat. No.: HY-D2341
CAS No.: 3055969-34-8
Cat. No.: HY-13031
CAS No.: 146135-18-4
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GW 841819X is a benzodiazepine inhibitor of bromodomains of the BET family (BRD2, BRD3, BRD4) that inhibits the binding of Diazepam to central GABA receptors. GW 841819X can be used in the research of BET bromodomain-related diseases, such as cancer .
Cat. No.: HY-B0696B
CAS No.: 145821-57-4
Synonyms: NO050328 hydrochloride hydrate; NO328 hydrochloride hydrate; TGB hydrochloride hydrate
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Tiagabine (NO050328; NO328; TGB) hydrochloride hydrate is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride hydrate exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride hydrate is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .
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Cat. No.: HY-167822
CAS No.: 1531600-36-8
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Caramboxin is a phenylalanine-like α-amino acid neurotoxin found in star fruit (Averrhoa carambola) with glutamatergic ionotropic action. Caramboxin activates NMDA, AMPA, and kainate receptors while inhibiting GABA binding to synaptic membranes, shifting the CNS toward an excitatory state and exerting neurotoxic effects linked to star fruit ingestion. Caramboxin can be used for research on neurotoxicity and as a reference standard for toxicological studies .
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-W722556
CAS No.: 7657-50-3
Synonyms: 3α,5α-Androstanol
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5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. 5α-Androstan-3α-ol can inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). 5α-Androstan-3α-ol negatively regulates the activity of CAR by binding to CAR and promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol can be used to study nuclear receptor-mediated hormone metabolism and drug detoxification mechanisms .
Cat. No.: HY-W103105R
CAS No.: 53786-28-0
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R 29676 is a neuroleptic agent and inhibits sodium-dependent GABA binding (GABA uptake) .
Cat. No.: HY-103513
CAS No.: 1236105-75-1
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GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
Cat. No.: HY-111298
CAS No.: 850339-33-2
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TG 41 is positive modulator of GABAA receptor. TG 41 enhances the binding both of GABA and of Flunitrazepam to rat cerebral cortical membranes .
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-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-106469
CAS No.: 81428-04-8
Synonyms: MY-117
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Taltrimide (MY-117), a lipophilic derivative of Taurine (HY-B0351), strongly inhibits the sodium-independent binding of Taurine to synaptic membranes of brain, the effects on the binding of GABA being less pronounced. Taltrimide exhibits definitive anticonvulsive effects in experimental epilepsy models .
Cat. No.: HY-P5305A
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Cat. No.: HY-N0067S2
CAS No.: 107022-06-0
Synonyms: 4-Aminobutyric acid-4,4-d2
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γ-Aminobutyric acid-4,4-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
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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-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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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
