PB183, a sigma receptor ligand, as a potential PET probe for the imaging of prostate adenocarcinoma

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1990-3. doi: 10.1016/j.bmcl.2008.01.109. Epub 2008 Feb 2.

Abstract

PB183, a non-selective sigma receptor ligand displaying high sigma-1 and sigma-2 receptor affinity, was evaluated in prostate tumour cell lines for its suitability as PET radiotracer. The pharmacodynamic and pharmacokinetic properties suggested PB183 as a potential PET radiotracer to visualize prostate adenocarcinoma.

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Adenocarcinoma / diagnostic imaging*
  • Animals
  • Cell Line, Tumor
  • Chromatography, High Pressure Liquid
  • Flow Cytometry
  • Male
  • Mice
  • Mice, Transgenic
  • Molecular Structure
  • Naphthalenes* / chemistry
  • Naphthalenes* / pharmacokinetics
  • Piperazines* / chemistry
  • Piperazines* / pharmacokinetics
  • Positron-Emission Tomography*
  • Prostatic Neoplasms / diagnostic imaging*
  • Receptors, sigma / metabolism*
  • Sigma-1 Receptor

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Naphthalenes
  • PB183 compound
  • Piperazines
  • Receptors, sigma
  • sigma-2 receptor