Abstract
The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are detailed along with the demonstration of the effectiveness of an MCH R1 antagonist in an animal model of obesity.
MeSH terms
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Animals
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Benzimidazoles / pharmacokinetics
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Benzimidazoles / pharmacology*
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Biological Availability
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Body Composition
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Dose-Response Relationship, Drug
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Mice
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Models, Animal
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Obesity / drug therapy*
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Receptors, Somatostatin / antagonists & inhibitors*
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Structure-Activity Relationship
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Weight Loss / drug effects
Substances
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Benzimidazoles
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Mchr1 protein, mouse
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Receptors, Somatostatin
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benzimidazole