GABA Receptor Modulator
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Inidascamine
0 ImagesCat. No.: HY-168977CAS No.: 903884-71-9Synonyms: RL-007; FSV7-007Inidascamine is the modulator for cholinergic, glutamatergic, and GABAB receptor, and can be used for researchs of schizophrenia.
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GL-II-73
0 ImagesCat. No.: HY-185978CAS No.: 2133456-91-2GL-II-73 is a selective, orally active and blood-brain barrier permeable positive allosteric modulator of α5GABAA receptor, acting on the benzodiazepine-binding site of GABAA receptors. The binding selectivity of GL-II-73 for the α5 subtype is 6-, 11- and 12.5-fold higher than that for the α2, α1 and α3 subtypes, respectively. GL-II-73 reverses pilocarpine-induced hyperactivation of dopamine neurons in the ventral tegmental area, improves working memory and pyramidal neuron dendritic morphology in 5xFAD mice, but does not reduce β-amyloid load. GL-II-73 can be used in research related to Alzheimer's disease and temporal lobe epilepsy with comorbid psychosis.
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ENX-101
0 ImagesCat. No.: HY-173251SENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models.
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DOV51892
0 ImagesCat. No.: HY-118502CAS No.: 864673-91-6DOV51892 is a GABAA receptor modulator. DOV51892 has a specific effect on GABAA receptors containing the α1 subunit. DOV51892 exhibits non-sedative anti-anxiety effects. DOV51892 can be used for in-depth research on the function of GABAA receptors.
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GABAA receptor modulator-13
0 ImagesCat. No.: HY-181552GABAA receptor modulator-13 is an orally active, blood-brain barrier-permeable α4β1δ GABAA receptor modulator (IC50 = 9.02 μM). GABAA receptor modulator-13 reduces GABA-induced currents, impairs the stability of the transmembrane domain M2-M3 loop of α4β1δ GABAA receptors, and exhibits selectivity for γ2-containing GABAA receptor subtypes and α6β3δ GABAA receptor subtypes. GABAA receptor modulator-13 is applicable to the research of nervous system diseases with altered tonic inhibition, such as neurodevelopmental disorders and epilepsy.
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GMA-839
0 ImagesCat. No.: HY-117955CAS No.: 162882-76-0Synonyms: WAY 141839; Co 2-6749GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics.
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Brallobarbitone
0 ImagesCat. No.: HY-W742312CAS No.: 561-86-4Synonyms: UcedormBrallobarbitone is a positive allosteric modulator of GABAA receptor. Brallobarbitone can be used in the research of β-cell dysfunction.
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GABAA receptor modulator-9
0 ImagesCat. No.: HY-175251GABAA receptor modulator-9 is and positive allosteric modulator of a1β2y2 subtype GABAA that can cross the blood-brain barrier. GABAA receptor modulator-9 exhibits comparable activity on α1β2γ2 (EC50: 0.9 μM in oocytes, 0.2 μM in CHO cells) and on α1β2, α3β2γ2 and α1β3γ2 (EC50s of 1.3, 3.4 and 1.1 μM). GABAA receptor modulator-9 significantly suppresses seizure progression and reduces delayed mortality. GABAA receptor modulator-9 can be used for the study of status epilepticus (SE).
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BHF177
0 ImagesCat. No.: HY-11058CAS No.: 917896-43-6BHF177 is a positive modulator of GABAB receptors that can block the interaction between nicotine and the brain's dopamine system, thereby reducing the addictive properties of nicotine. BHF177 is expected to be used in research related to smoking cessation.
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Anticonvulsant agent 5
0 ImagesCat. No.: HY-162757Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABAA receptors and NaV1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED50 of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC50 of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable.
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GT-002
0 ImagesCat. No.: HY-P992360GT-002 is a partial positive allosteric modulator targeting the α3 subtype of GABAA receptors, as well as a specific binder of tumor-associated TF-glycosylated LYPD3. GT-002 mildly enhances GABA-induced chloride currents by binding to the benzodiazepine site of GABAA receptors, thereby alleviating prefrontal hypofunction and improving cognitive, memory and social interaction abilities. GT-002 can be used in research related to schizophrenia spectrum disorders, various squamous cell carcinomas, colorectal cancer, non-small cell lung cancer, and aromatic L-amino acid decarboxylase deficiency.
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GABAA receptor modulator-12
0 ImagesCat. No.: HY-W070739CAS No.: 6252-98-8GABAA receptor modulator-12 (Compound 5) is a GABAA receptor modulator. GABAA receptor modulator-12 inhibits anesthetic-induced desensitization of GABAA α3β3γ2 receptors with an IC50 of 0.2 μM. GABAA receptor modulator-12 can be used in the research of central nervous system disorders.
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(Rac)-Acetoxyvalerenic acid
0 ImagesCat. No.: HY-167702CAS No.: 81397-67-3(Rac)-Acetoxyvalerenic acid is a derivative of valerenic acid that acts as a GABA (A) receptor modulator, potentially providing sedative and sleep-enhancing effects. (Rac)-Acetoxyvalerenic acid exhibits slower permeability across the blood-brain barrier compared to diazepam, indicating that its transport may rely on an unidentified pathway rather than transcellular passive diffusion.
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Clazolam
0 ImagesCat. No.: HY-W754627CAS No.: 7492-29-7Synonyms: Isoquinazepon; SAH-1123Clazolam (Isoquinazepon; SAH-1123) is a GABA Receptor modulator. Clazolam can be used in research on neurological diseases.
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Etazolate
0 ImagesCat. No.: HY-106044CAS No.: 51022-77-6Synonyms: SQ 64442Etazolate (SQ 64442) is a α-secretase activator, selective PDE4 inhibitor, selective GABAA receptor modulator. Etazolate reduces IL-1β levels Etazolate exerts a dose-dependent anti-inflammatory and anti-œdematous effect accompanied by lasting memory improvement. Etazolate produces an antidepressant-like effect.
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Xilmenolone
0 ImagesCat. No.: HY-147421CAS No.: 2368807-26-3Xilmenolone is a GABAA receptor positive allosteric modulator.
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MmTx2 toxin
0 ImagesCat. No.: HY-P5857Synonyms: Micrurotoxin 2MmTx2 toxin is a GABAA receptor modulator that enhances GABAA receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain.
