Abstract
We have developed and characterized [(35)S]4a as a potent and selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R). Compound [(35)S]4a showed appreciable specific signals in brain slices prepared from wild-type mice but not from MCH1R deficient mice, confirming the specificity and utility of [(35)S]4a as a selective MCH1R radioligand for ex vivo receptor occupancy assays.
MeSH terms
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Amino Acid Sequence
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Animals
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Benzofurans / chemical synthesis
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Benzofurans / chemistry*
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Benzofurans / pharmacology
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Brain / metabolism
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CHO Cells
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Cricetinae
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Cricetulus
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Humans
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Kinetics
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Mice
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Mice, Knockout
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Receptors, Somatostatin / antagonists & inhibitors
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Receptors, Somatostatin / deficiency
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Receptors, Somatostatin / metabolism*
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Spiro Compounds / chemical synthesis
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Spiro Compounds / chemistry*
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Spiro Compounds / pharmacology
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology
Substances
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Benzofurans
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MCHR1 protein, human
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Mchr1 protein, mouse
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Receptors, Somatostatin
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Spiro Compounds
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Sulfonamides