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Compound was evaluated for inhibition of rat Slc18a2 in an ex vivo assay measured by radioactivity method
Assay data:39 Active, 1 Activity ≤ 1 nM, 22 Activity ≤ 1 µM, 82 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of rat VMAT2 transfected in HEK cells using FFN206 as fluorescent substrate preincubated for 1 hr followed by substrate addition and measured after 30 mins by fluorescence plate reader assay
Assay data:12 Active, 7 Activity ≤ 1 µM, 12 Tested
Determining Vmat2 Inhibitory Activity of a Compound from US Patent US11053242: "[9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11BH-pyrido-[2,1-a]isoquinolin-2-yl]methanol and compounds, compositions and methods relating thereto"
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
[3H]TBZOH Binding Assay from Article 10.1074/jbc.M113.502971: "Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine."
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
[3H]Serotonin Uptake Assay from Article 10.1074/jbc.M113.502971: "Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine."
Inhibition of [3H]DA uptake at VMAT2 in rat striatal synaptosome incubated for 10 mins followed by [3H]DA addition and measured after 20 mins by TopCount scintillation counting method
Assay data:9 Active, 9 Activity ≤ 1 µM, 12 Tested
Inhibition of [3H]DA uptake at VMAT2 in rat striatal synaptosome at 0.1 uM incubated for 10 mins followed by [3H]DA addition and measured after 20 mins by TopCount scintillation counting method relative to control
Assay data:10 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of [3H]DA uptake at VMAT2 in rat striatal synaptosome at 1 uM incubated for 10 mins followed by [3H]DA addition and measured after 20 mins by TopCount scintillation counting method relative to control
Inhibition of [3H]DTBZ binding to VMAT2 in rat brain incubated for 30 mins by liquid scintillation spectrometry analysis
Assay data:17 Active, 24 Activity ≤ 1 µM, 24 Tested
Inhibition of VMAT2 in rat brain
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of VMAT2 in rat striatal homogenate assessed as reduction in [3H]DA uptake after 8 mins by liquid scintillation spectrometric analysis
Assay data:11 Active, 11 Activity ≤ 1 µM, 11 Tested
Inhibition of [3H]DTBZ binding to VMAT2 in rat whole brain homogenate (excluding cerebellum) after 30 mins by liquid scintillation spectrometric analysis
Assay data:11 Active, 1 Activity ≤ 1 µM, 11 Tested
Inhibition of [3H]-DHTBZ binding to VMAT2 from rat forebrain membranes
Inhibition of [3H]dopamine uptake at VMAT2 in rat synaptic vesicles after 8 mins by liquid scintillation spectrometry
Inhibition of [3H]dopamine uptake at VMAT2 in rat striatal synaptic vesicles by scintillation spectrometry
Assay data:17 Active, 17 Activity ≤ 1 µM, 17 Tested
Rat Vesicular monoamine transporter 2 (SLC18 family of vesicular amine transporters)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Potency index, ratio of lobelane Ki to compound Ki for VMAT2 in rat whole brain vesicles homogenate
Assay data:2 Tested
Inhibition of [3H]DA uptake at VMAT2 in rat striata vesicles homogenate after 8 mins by liquid scintillation counting
Assay data:29 Active, 29 Activity ≤ 1 µM, 29 Tested
Displacement of [3H]DTBZ from VMAT2 in rat whole brain vesicles homogenate after 30 mins by liquid scintillation counting
Assay data:28 Active, 20 Activity ≤ 1 µM, 28 Tested
Potency index, ratio of lobelane Ki to compound Ki for VMAT2 in rat striata vesicles homogenate
Assay data:3 Tested
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