Design and synthesis of melatonin receptors agonists and antagonists

Farmaco. 2000 Mar;55(3):184-7. doi: 10.1016/s0014-827x(00)00017-3.

Abstract

We review our work towards the design and synthesis of high-affinity melatonin (N-acetyl-5-methoxytryptamine) agonist and antagonist compounds. High affinity melatonergic agonists were obtained by shifting the melatonin side chain from C3 to N1 of the indole ring system. Conversely, by moving the side chain from C3 to C2 it was possible to obtain melatonin antagonist compounds, albeit of moderate affinity.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Design
  • Humans
  • Melatonin / metabolism*
  • Receptors, Cell Surface / agonists*
  • Receptors, Cell Surface / antagonists & inhibitors*
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors*
  • Receptors, Melatonin
  • Structure-Activity Relationship

Substances

  • Receptors, Cell Surface
  • Receptors, Cytoplasmic and Nuclear
  • Receptors, Melatonin
  • Melatonin