Abstract
Melanin concentrating hormone (MCH) plays an important role in the regulation of food intake and energy balance in mammals. MCH-1 receptor (MCH1R) deficient mice are lean and resistant to diet-induced obesity. As such, MCH1R antagonists are believed to have potential as possible treatments for obesity. The discovery of a novel class of tetralin ureas as potent MCH1R antagonists is described herein.
MeSH terms
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Animals
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Binding, Competitive / drug effects
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CHO Cells
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Cricetinae
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Cricetulus
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Drug Design
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Humans
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Mice
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Mice, Knockout
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Rats
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Receptors, Somatostatin / antagonists & inhibitors*
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Receptors, Somatostatin / genetics
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Structure-Activity Relationship
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Tetrahydronaphthalenes / chemical synthesis*
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Tetrahydronaphthalenes / pharmacokinetics
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Tetrahydronaphthalenes / pharmacology*
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Tissue Distribution
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Urea / analogs & derivatives*
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Urea / pharmacokinetics
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Urea / pharmacology*
Substances
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Mchr1 protein, mouse
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Receptors, Somatostatin
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Tetrahydronaphthalenes
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Urea