Abstract
Cannabinoid CB2 receptor has emerged as a very promising target over the last decades. We have synthesized and evaluated a new fluorescent probe designated NMP6 based on 6-methoxyisatin scaffold, which exhibited selectivity and K(i) value at hCB2 of 387 nM. We have demonstrated its ability to be an effective probe for visualization of CB2 receptor binding using confocal microscopy and a flow cytometry probe for the analysis of CB2 protein expression. Furthermore, NMP6 was easily obtained in two chemical steps from commercially available building blocks.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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B-Lymphocytes
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CHO Cells
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Cricetinae
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Drug Design
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Drug Evaluation, Preclinical
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Fluorescence
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Fluorescent Dyes / chemical synthesis*
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Fluorescent Dyes / chemistry
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Fluorescent Dyes / metabolism*
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Humans
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Hydrazines / chemistry
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Hydrazines / metabolism
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Hydrazones / chemical synthesis*
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Hydrazones / chemistry
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Hydrazones / metabolism*
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Isatin / analogs & derivatives*
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Isatin / chemical synthesis
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Isatin / chemistry
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Isatin / metabolism
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Ligands
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Lung
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Mice
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Mice, Inbred BALB C
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Microscopy, Confocal
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Molecular Structure
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Oxadiazoles / chemistry
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Oxadiazoles / metabolism
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Protein Binding
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Pyrans / pharmacology
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Pyrimidines / pharmacology
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Receptor, Cannabinoid, CB2 / agonists
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Receptor, Cannabinoid, CB2 / analysis*
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Receptor, Cannabinoid, CB2 / metabolism
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Structure-Activity Relationship
Substances
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2-((2,4-dichlorphenyl)amino)-N-((tetrahydro-2H-pyran-4-yl)methyl)-4-(trifluoromethyl)-5-pyrimidinecarboxamide
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Fluorescent Dyes
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Hydrazines
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Hydrazones
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Ligands
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N-(4-nitro-2,1,3-benzoxadiazol-7-yl)-N-methyl-2-aminoacetohydrazide
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Oxadiazoles
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Pyrans
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Pyrimidines
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Receptor, Cannabinoid, CB2
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Isatin