Abstract
A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain penetration in mice.
MeSH terms
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Amides / chemistry
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Animals
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Humans
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Ligands
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Mice
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Molecular Structure
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Piperazine
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Piperazines / chemical synthesis
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Piperazines / chemistry*
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Piperazines / pharmacokinetics
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Piperazines / pharmacology*
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Receptor, Melanocortin, Type 4 / antagonists & inhibitors*
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Receptor, Melanocortin, Type 4 / metabolism*
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Structure-Activity Relationship
Substances
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Amides
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Ligands
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Piperazines
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Receptor, Melanocortin, Type 4
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Piperazine