GABA Receptor Inhibitor
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Bicyclo-GABA
0 ImagesCat. No.: HY-181135CAS No.: 1615763-33-1Bicyclo-GABA is a selective betaine/GABA transporter 1 (BGT1) competitive, non-transported inhibitor with an IC50 of 590 nM. Bicyclo-GABA exhibits low micromolar agonistic activity at α1β2γ2 GABAA receptors with an EC50 of 5.1 μM. Bicyclo-GABA displays 129 times higher activity for BGT1 than GAT3. Bicyclo-GABA serves as a valuable tool compound for deciphering its elusive pharmacological role in the brain and periphery.
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Fipronil sulfone (Standard)
0 ImagesCat. No.: HY-125296RCAS No.: 120068-36-2Fipronil sulfone (Standard) is the analytical standard of Fipronil sulfone. This product is intended for research and analytical applications. Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits
GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
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L-Cycloserine (Standard)
0 ImagesSynonyms: (S)-Cycloserine (Standard); (S)-4-Amino-3-isoxazolidone (Standard)L-Cycloserine (Standard) is the analytical standard of L-Cycloserine. This product is intended for research and analytical applications. L-Cycloserine ((S)-4-Amino-3-isoxazolidone) is an oral inhibitor of the enzyme gamma-aminobutyric acid (GABA) transaminase (GABA-t) and branched-chain transaminases in Mycobacterium tuberculosis. L-Cycloserine has anticonvulsant properties and inhibits the synthesis of neurotensin in mouse brains[1][2][3][4].
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Denzimol
0 ImagesCat. No.: HY-105059CAS No.: 73931-96-1Denzimol is an orally active anticonvulsant agent. Denzimol inhibits cytochrome P450, and interacts with benzodiazepine receptors. Denzimol selectively antagonizes tonic components of Metrazol-induced seizures in rats and mice. Denzimol can be used for the research of epilepsy and convulsions.
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Insecticidal agent 31
0 ImagesCat. No.: HY-182041Insecticidal agent 31 is an insecticide targeting the γ-aminobutyric acid receptor (GABAR). Insecticidal agent 31 exhibits insecticidal activity against Plutella xylostella, Spodoptera frugiperda and Spodoptera exigua. Insecticidal agent 31 can serve as a lead compound for the design and synthesis of novel isoxazole-based insecticides.
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Afoxolaner-d6
0 ImagesCat. No.: HY-16974SAfoxolaner-d6 is the deuterium labeled Afoxolaner (HY-16974). Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
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Ro 15-1310
0 ImagesCat. No.: HY-115854CAS No.: 78756-33-9Ro 15-1310 is an imidazobenzodiazepine that exhibits high affinity and selectivity for alpha 5-containing GABAA receptors. Ro 15-1310 is promising for research of convulsions.
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GABAA receptor agent 7
0 ImagesCat. No.: HY-146099CAS No.: 2376841-18-6GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy.
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mGAT3/4-IN-2
0 ImagesCat. No.: HY-146281CAS No.: 2556833-68-0mGAT3/4-IN-2 (compound 27b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.44 and 5.25, respectively.
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Thiazesim
0 ImagesThiazesim is a CNS-penetrant GABAA receptor inhibitor, exerting anticonvulsant and antidepressant effects. Thiazesim depresses amygdala output, disrupts conditioned avoidance response in rats. Thiazesim can be used for the research of depression and epilepsy.
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EF1500
0 ImagesCat. No.: HY-189042CAS No.: 738562-57-7EF1500 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.
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GPR61 Inverse agonist 3
0 ImagesCat. No.: HY-182271GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia.
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Tiagabine hydrochloride hydrate
0 ImagesCat. No.: HY-B0696BCAS No.: 145821-57-4Synonyms: NO050328 hydrochloride hydrate; NO328 hydrochloride hydrate; TGB hydrochloride hydrateTiagabine (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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NO-711
0 ImagesCat. No.: HY-114040CAS No.: 159094-94-7Synonyms: NNC-711 free acidNO-711 (NNC-711) free acid is a novel potent and selective inhibitor of γ-aminobutyric acid uptake. NO-711 inhibits synaptosomal (IC50 = 47 nM), neuronal (IC50 = 1238 nM) and glial (IC50 = 636 nM) GABA uptake in vitro.
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SR-THAP
0 ImagesCat. No.: HY-181961CAS No.: 3098361-74-8SR-THAP is a γ-aminobutyric acid transporter 3 (GAT3) inhibitor with an IC50 of 4.9 μM, and exhibits 42-fold and 23-fold selectivity over GAT1 and GlyT1, respectively. SR-THAP inhibits GABA uptake in mammalian cells. SR-THAP is applicable to the research of epilepsy, Alzheimer's disease and ischemic stroke.
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Vigabatrin-13C,d2 hydrochloride
0 ImagesCat. No.: HY-B0033SSynonyms: γ-Vinyl-GABA-13C,d2 hydrochlorideVigabatrin-13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
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Org 21465
0 ImagesCat. No.: HY-106965CAS No.: 167946-96-5Org 21465 is an agent that can relieve pain. Org 21465 causes no cardiovascular or respiratory depression. Org 21465 can inhibit GABAA receptor in vivo.
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NO-711ME
0 ImagesCat. No.: HY-129464CAS No.: 127586-66-7NO-711ME is a prodrug of NO-711. NO-711 is a potent and selective GABA uptake inhibitor.
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α,β-Thujone
0 ImagesCat. No.: HY-W751152CAS No.: 76231-76-0α,β-Thujone is a component of the essential oils of some plants. α,β-Thujone causes cancers in male rats and induces seizures in the highest doses.
