In vitro and in vivo evaluation of O-alkyl derivatives of tramadol

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1674-80. doi: 10.1016/j.bmcl.2008.01.051. Epub 2008 Jan 18.

Abstract

Tramadol is a centrally acting opioid analgesic structurally related to codeine and morphine. O-Alkyl, N-desmethyl, and non-phenol containing derivatives of tramadol were synthesized to probe their effect on metabolic stability and both in vitro and in vivo potency.

MeSH terms

  • Analgesics, Opioid / chemistry*
  • Analgesics, Opioid / metabolism
  • Analgesics, Opioid / pharmacology*
  • Animals
  • Humans
  • Microsomes, Liver / drug effects
  • Microsomes, Liver / metabolism
  • Molecular Structure
  • Pain / drug therapy
  • Protein Binding
  • Rats
  • Structure-Activity Relationship
  • Tramadol / analogs & derivatives*
  • Tramadol / chemistry
  • Tramadol / metabolism
  • Tramadol / pharmacology*

Substances

  • Analgesics, Opioid
  • Tramadol