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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
41 Results for "
α1β2γ2
" in MedChemExpress (MCE) Product Catalog:
Products (41)
41 Results for "α1β2γ2" in MCE Product Catalog:
4
4 Cited Publications
Cat. No.: HY-B1494
CAS No.: 17617-45-7
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3
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Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
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Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
2
2 Cited Publications
Cat. No.: HY-N6630
CAS No.: 29976-75-8
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6-Methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
1
1 Cited Publications
Synonyms: Lu 02-030 hydrochloride; THIP hydrochloride
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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 .
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Paramacrolobium coeruleum (Taub.) J.Léonard Labiatae Ketones, Aldehydes, Acids Phenols Plants Endogenous metabolite
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Cat. No.: HY-W013150
CAS No.: 82626-01-5
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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 .
Cat. No.: HY-W001692
CAS No.: 96604-21-6
Synonyms: DOV 273547
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Ocinaplon (DOV 273547) is an orally active positive allosteric modulator of GABAA receptor, with an EC50 ranging from 3.07 μM (α1β2γ2 subtype) to 10.03 μM (α1β2γ3 subtype). Ocinaplon enhances GABA-stimulated chloride currents across multiple GABAA receptor subtypes, with varying potency between different subtypes. Ocinaplon exerts anxiolytic and anticonvulsant effects, and causes motor impairment at high doses. Ocinaplon can be used for research on generalized anxiety disorder .
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6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABAA receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABAA receptors, and is relatively inactive on the α1β2 GABAA receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain .
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TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors .
Cat. No.: HY-Y0313S
CAS No.: 284474-52-8
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GMQ is an acid-sensing ion channel modulator, competitive GABAAR antagonist. GMQ preferentially, potently, competitively inhibits GABAARs. GMQ inhibits α1β2, α1β2γ2, α4β2γ2 and α5β2γ2 GABAARs. GMQ enhances neuronal excitation through inhibition of GABAergic transmission. GMQ has anti-histamine effects in the enteric system, inhibiting gastric acid secretion .
Cat. No.: HY-175670
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GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy .
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U93631 is a GABAA receptor inhibitor targeting the picrotoxin (HY-101391) site, which exhibits higher inhibitory potency in receptors lacking α subunits. U93631 blocks GABA-induced chloride currents, exerts a mild initial stimulatory effect on activated currents, but its activity decreases in β2T246F mutant receptors. U93631 can serve as a ligand for the convulsant site of GABAA receptors in relevant studies .
Cat. No.: HY-135482
CAS No.: 1781880-44-1
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GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) .
Cat. No.: HY-170930
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Anticonvulsant agent 9 (compound 4f) is an α1β2γ2 GABAA receptors activator. Anticonvulsant agent 9 activatesα1β2γ2 GABAA receptors with an EC50 of 1.24 μM. Anticonvulsant agent 9 inhibits the inactivation of Nav1.2 channels. Anticonvulsant agent 9 exhibits significant anticonvulsant activities .
Cat. No.: HY-129431
CAS No.: 157013-32-6
Synonyms: PNU-89843
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U-89843A (PNU-89843) is a GABAA receptors positive allosteric modulator (PAM). U-89843A enhances GABA-induced Cl - currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A shows antioxidant and sedative effects .
Cat. No.: HY-103497
CAS No.: 157013-85-9
Synonyms: PNU-89843 hydrochloride
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U-89843A (PNU-89843) hydrochloride is a GABAA receptors positive allosteric modulator (PAM). U-89843A hydrochloride enhances GABA-induced Cl - currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A hydrochloride shows antioxidant and sedative effects .
Cat. No.: HY-117106
CAS No.: 200266-76-8
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PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
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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
