Abstract
A series of 2-aminoquinoline compounds was prepared and evaluated in MCH1R binding and functional antagonist assays. Small dialkyl, methylalkyl, methylcycloalkyl, and cyclic amines were tolerated at the quinoline 2-position. The in vivo efficacy of compound 12 was explored and compared to that of a related inactive analog to determine their effects on food intake and body weight in rodents.
MeSH terms
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Animals
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Binding, Competitive
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Biological Assay
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Eating
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Energy Metabolism / drug effects
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Humans
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Male
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Molecular Structure
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Quinolines / chemical synthesis
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Quinolines / chemistry
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Quinolines / pharmacology*
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Quinuclidines / chemical synthesis
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Quinuclidines / chemistry
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Quinuclidines / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Receptors, Somatostatin / antagonists & inhibitors*
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Receptors, Somatostatin / chemistry
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Receptors, Somatostatin / genetics
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Stereoisomerism
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Structure-Activity Relationship
Substances
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6-(12-(2-fluoromethylpyridin-5-yl)dodecanamido)-2-(1-quinuclidinyl)quinoline
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MCHR1 protein, human
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MCHR1 protein, rat
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Quinolines
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Quinuclidines
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Receptors, Somatostatin