Abstract
A series of chiral heterocyclic aminopyrrolidine derivatives was synthesized as novel melatoninergic ligands. Binding affinity assays were performed on cloned human MT(1) and MT(2) receptors, stably expressed in NIH3T3 cells. Compound 16 was identified as an orally bioavailable agonist at MT(1) and MT(2) melatonin receptors with low vasoconstrictive activity.
MeSH terms
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3T3 Cells
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Aminoquinolines / chemical synthesis*
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Aminoquinolines / pharmacology*
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Animals
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Cloning, Molecular
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Colforsin / pharmacology
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Cyclic AMP / metabolism
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Heterocyclic Compounds / chemical synthesis*
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Heterocyclic Compounds / pharmacology*
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Humans
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Kinetics
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Ligands
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Melatonin / agonists*
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Melatonin / pharmacology
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Mice
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Receptor, Melatonin, MT1 / drug effects
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Receptor, Melatonin, MT1 / metabolism
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Receptor, Melatonin, MT2 / drug effects
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Receptor, Melatonin, MT2 / metabolism
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Recombinant Proteins / metabolism
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Structure-Activity Relationship
Substances
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Aminoquinolines
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Heterocyclic Compounds
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Ligands
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Receptor, Melatonin, MT1
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Receptor, Melatonin, MT2
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Recombinant Proteins
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Colforsin
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Cyclic AMP
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Melatonin