Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2183-7. doi: 10.1016/j.bmcl.2007.12.056. Epub 2007 Dec 25.

Abstract

A potent sigma-2 receptor ligand, known as PB28, was tritium radiolabelled and biologically evaluated. The results showed that [(3)H]PB28 and the corresponding unlabelled PB28 had superimposed pharmacodynamic properties. This radioligand appears as a potential candidate for receptor binding and in living cells assays.

MeSH terms

  • Animals
  • Binding Sites
  • Binding, Competitive
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Liver / cytology
  • Liver / drug effects
  • Liver / metabolism
  • Molecular Structure
  • Piperazines / pharmacokinetics
  • Piperazines / pharmacology*
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Radioligand Assay
  • Rats
  • Receptors, sigma / agonists*
  • Tritium / pharmacokinetics*

Substances

  • PB28 compound
  • Piperazines
  • RNA, Messenger
  • Receptors, sigma
  • sigma-2 receptor
  • Tritium