Abstract
Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry optimization and SAR studies, orally active proline amides with robust efficacy in a rodent food intake inhibition model were uncovered.
2010. Published by Elsevier Ltd.
MeSH terms
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Administration, Oral
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Amides / pharmacokinetics
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Amides / pharmacology
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Amides / therapeutic use
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Animals
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Anti-Obesity Agents / pharmacokinetics*
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Anti-Obesity Agents / pharmacology
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Anti-Obesity Agents / therapeutic use*
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Brain / metabolism
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Dogs
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Eating / drug effects
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Humans
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Obesity / drug therapy*
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Proline / analogs & derivatives
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Proline / pharmacokinetics*
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Proline / pharmacology
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Proline / therapeutic use*
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Rats
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Receptor, Serotonin, 5-HT2C / metabolism
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Serotonin 5-HT2 Receptor Agonists*
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Structure-Activity Relationship
Substances
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Amides
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Anti-Obesity Agents
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Receptor, Serotonin, 5-HT2C
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Serotonin 5-HT2 Receptor Agonists
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Proline