Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists

Bioorg Med Chem Lett. 2003 May 5;13(9):1549-52. doi: 10.1016/s0960-894x(03)00178-1.

Abstract

A series of acyclic phenethylthiocarbamate derivatives have been synthesized, and their antagonist effect against vanilloid receptor tested. Chain branching led to a significant change in antagonist activity of the parent molecule. Ethyl-branched 1e showed a 6.3 microM of IC(50) value in 45Ca(2+)-influx assay.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium / metabolism
  • Capsaicin / analogs & derivatives*
  • Capsaicin / chemistry
  • Capsaicin / pharmacology
  • Cells, Cultured
  • Neurons, Afferent / drug effects
  • Neurons, Afferent / metabolism
  • Rats
  • Receptors, Drug / agonists
  • Receptors, Drug / antagonists & inhibitors*
  • Spinal Cord / cytology
  • Structure-Activity Relationship
  • Thiocarbamates / chemical synthesis*
  • Thiocarbamates / chemistry
  • Thiocarbamates / pharmacology*

Substances

  • Receptors, Drug
  • Thiocarbamates
  • capsazepine
  • Capsaicin
  • Calcium