Abstract
Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC(50)=24 nM) and selective MC4-R agonists. We report the SAR of this series of compounds using in vitro cAMP functional assays in cells transfected with the MC4 or other melancortin receptors.
MeSH terms
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Cell Line
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Cyclic AMP / metabolism
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Cyclic AMP / physiology
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Heterocyclic Compounds / chemical synthesis
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Heterocyclic Compounds / pharmacology
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Humans
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Hydrogen Bonding
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Indicators and Reagents
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Piperazines / chemical synthesis*
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Piperazines / pharmacology*
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Receptor, Melanocortin, Type 4 / agonists*
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Receptor, Melanocortin, Type 4 / genetics
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Structure-Activity Relationship
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Transfection
Substances
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Heterocyclic Compounds
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Indicators and Reagents
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Piperazines
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Receptor, Melanocortin, Type 4
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Cyclic AMP