Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.

Academic Article

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.
  • Keywords

  • 3T3 Cells, Aminoquinolines, Animals, Cloning, Molecular, Colforsin, Cyclic AMP, Heterocyclic Compounds, Humans, Kinetics, Ligands, Melatonin, Mice, Receptor, Melatonin, MT1, Receptor, Melatonin, MT2, Recombinant Proteins, Structure-Activity Relationship
  • Digital Object Identifier (doi)

    Author List

  • Sun L-Q; Chen J; Mattson RJ; Epperson JR; Deskus JA; Li WS; Takaki K; Hodges DB; Iben L; Mahle CD
  • Start Page

  • 4381
  • End Page

  • 4384
  • Volume

  • 13
  • Issue

  • 24