Abstract
We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor 1 (MCHR-1). Synthesis and structure-activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity has been demonstrated in animal models of food intake and depression.
MeSH terms
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Animals
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Chemistry, Pharmaceutical / methods*
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Depression / drug therapy
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Disease Models, Animal
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Drug Design
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Feeding Behavior / drug effects
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Hydantoins / chemistry*
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Kinetics
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Melanins / chemistry*
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Models, Biological
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Models, Chemical
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Models, Molecular
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Receptors, Pituitary Hormone / antagonists & inhibitors*
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Receptors, Pituitary Hormone / chemistry*
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Receptors, Somatostatin / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Hydantoins
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Melanins
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Receptors, Pituitary Hormone
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Receptors, Somatostatin
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melanin-concentrating hormone receptor