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经验公式(希尔记法):
C18H10Br2ClN3OS
化学文摘社编号:
分子量:
511.62
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
InChI
1S/C18H10Br2ClN3OS/c19-11-8-13(20)16-22-15(14-2-1-7-26-14)17(24(16)9-11)23-18(25)10-3-5-12(21)6-4-10/h1-9H,(H,23,25)
SMILES string
Clc1ccc(cc1)C(=O)Nc2c(nc3c(Br)cc(Br)cn23)-c4cccs4
InChI key
MEWSBNIVOLYKGU-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
off-white to tan
solubility
DMSO: >10 mg/mL
storage temp.
2-8°C
Biochem/physiol Actions
δ-GABAA receptors are emerging as an important pharmacological target. DS1 potently (low nM) enhances GABA-evoked currents mediated by α4β3δ receptors. It had little effect on GABA responses mediated by α4β3γ2 receptors. At similar concentrations DS1 directly activates this receptor and is the most potent known agonist of α4β3δ receptors. This compound has an opportunity to be become an agonist golden stardard for δ-GABAA receptors.
DS1 potently (low nM) enhances GABA-evoked currents mediated by α4β3δ receptors.
DS1 potently (low nM) enhances GABA-evoked currents mediated by GABAA α4β3δ receptor subtype. At similar concentrations, it acts as a direct agonist at this receptor and is the most potent agonist known. It has little effect on GABA responses mediated by α4β3γ2 receptors.
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