2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor

Bioorg Med Chem Lett. 2001 Apr 23;11(8):1073-6. doi: 10.1016/s0960-894x(01)00134-2.

Abstract

A series of 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. Some para-substituents on the 4-phenylbutyl side chain attached to the tryptamine nitrogen led to compounds with potent GnRH receptor binding. The study has helped define structural requirements for GnRH receptor binding for the 2-aryltryptamine GnRH antagonists.

MeSH terms

  • Animals
  • Binding Sites / physiology
  • Drug Design
  • Female
  • Hormone Antagonists / chemistry
  • Hormone Antagonists / metabolism*
  • Hormone Antagonists / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Rats
  • Receptors, LHRH / metabolism*
  • Tryptamines / chemical synthesis*
  • Tryptamines / chemistry
  • Tryptamines / metabolism*
  • Tryptamines / pharmacology*

Substances

  • 2-(3,5-dimethylphenyl)tryptamine
  • Hormone Antagonists
  • Receptors, LHRH
  • Tryptamines
  • tryptamine