GABA Receptor Modulator
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Lofendazam
0 ImagesCat. No.: HY-184368CAS No.: 29176-29-2Lofendazam is a major metabolite of Arfendazam. Lofendazam acts as a positive allosteric modulator/partial agonist of GABAa receptor, with IC50 values of 10.1 nM and 9.1 nM in bovine cerebral cortex and bovine cerebellum, respectively; its in vivo ED50 via oral administration is 233 µmol/kg.
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Androst-16-en-3-ol
0 ImagesCat. No.: HY-W644305CAS No.: 7148-51-8Synonyms: 3β-AndrostenolAndrost-16-en-3-ol is a pheromone derived from boars that triggers mating responses in estrous sows. It also exists in human urine, plasma, saliva and sweat. As an endogenous neurosteroid, Androst-16-en-3-ol acts as a positive allosteric modulator of GABAA receptors (GABAA receptor) and exerts anxiolytic, antidepressant and anticonvulsant activities in mice.
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Saripidem
0 ImagesCat. No.: HY-106875CAS No.: 103844-86-6Saripidem is a non-selective ligand for ω modulatory sites of GABA receptor.
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CL 218872 (Standard)
0 ImagesCat. No.: HY-103505RCAS No.: 66548-69-4CL 218872 (Standard) is the analytical standard of CL 218872 (HY-103505). This product is intended for research and analytical applications. CL 218872 is an orally active and selective ligand for the benzodiazepine receptor subtype BZ1. CL 218872 exhibits anxiolytic, sedative and anticonvulsant activities. CL 218872 can be used in researches of anxiety related disorders and epilepsy.
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α-Thujone (Standard)
0 ImagesCat. No.: HY-121618RCAS No.: 546-80-5α-Thujone (Standard) is the analytical standard of α-Thujone. This product is intended for research and analytical applications. α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
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Alpidem (Standard)
0 ImagesCat. No.: HY-W013150RCAS No.: 82626-01-5Alpidem (Standard) is the analytical standard of Alpidem (HY-W013150). This product is intended for research and analytical applications. Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
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Imidazenil
0 ImagesImidazenil is a partial positive allosteric modulator of GABAA receptors with anxiolytic, antipanic and anticonvulsant activities.
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NS11394 (Standard)
0 ImagesCat. No.: HY-11048RCAS No.: 951650-22-9NS11394 (Standard) is the analytical standard of NS11394 (HY-11048). This product is intended for research and analytical applications. NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
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Chlorothymol
0 ImagesChlothymol is a potent positive modulator of the GABAA receptor subunit LGC-37, anticonvulsant, and antibacterial agent. Chlothymol inhibits Pentylenetetrazol-induced c-fos expression. Chlothymol inhibits the growth of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA) strains, including LAC, with an MIC of 32 μg/mL. Chlorothymol has protective effects against epileptic seizures in various mouse models.
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7-Keto-DHEA (Standard)
0 ImagesSynonyms: 7-Oxo-DHEA (Standard); 7-Ketodehydroepiandrosterone (Standard); 7-Oxodehydroepiandrosterone (Standard)7-Keto-DHEA (Standard) (7-Oxo-DHEA (Standard)) is the analytical standard of 7-Keto-DHEA (HY-N9483). This product is intended for research and analytical applications. 7-Keto-DHEA binds to GABA Receptor, and reduces the ethanol intake in rats. 7-Keto-DHEA exhibits potential in investigation of alcohol dependence disorders.
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L-838417 (Standard)
0 ImagesCat. No.: HY-W009009RCAS No.: 286456-42-6L-838417 (Standard) is the analytical standard of L-838417 (HY-W009009). This product is intended for research and analytical applications. L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2. L-838417 has anti-anxiety activity.
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SGE-516
0 ImagesCat. No.: HY-129408CAS No.: 1430064-74-6SGE-516 is a neuroactive steroid that is a potent positive allosteric modulator of synaptic and extra-synaptic GABAA receptors. SGE-516 has anticonvulsant activity.
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Gaboxadol hydrochloride (Standard)
0 ImagesCat. No.: HY-10233RCAS No.: 85118-33-8Synonyms: Lu 02-030 hydrochloride (Standard); THIP hydrochloride (Standard)Gaboxadol (hydrochloride) (Standard) is the analytical standard of Gaboxadol (hydrochloride). This product is intended for research and analytical applications. Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent.
