Abstract
A series of piperazinephenethylamines were synthesized to study the contribution of a basic amine to binding affinity at the melanocortin-4 receptor. Several potent compounds from this series possessed subnanomolar K(i) values in a competition binding assay.
MeSH terms
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Animals
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Benzylamines / metabolism
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Inhibitory Concentration 50
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Kinetics
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Phenethylamines / chemistry*
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Phenethylamines / metabolism
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Phenethylamines / pharmacology*
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Piperazines / chemistry*
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Piperazines / metabolism
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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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Benzylamines
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Phenethylamines
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Piperazines
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Receptor, Melanocortin, Type 4