Synthesis, radiosynthesis and in vivo evaluation in mice of [123I]-(4-fluorophenyl) {1-[2-(4-iodophenyl)ethyl]piperidin-4-yl}methanone for visualization of the 5-HT2A receptor with SPECT

Appl Radiat Isot. 2005 May;62(5):737-43. doi: 10.1016/j.apradiso.2004.10.008. Epub 2004 Dec 7.

Abstract

This work reports the synthesis, radiolabelling and preliminary in vivo evaluation of [(123)I]-(4-fluorophenyl){1-[2-(4-iodophenyl)ethyl]piperidin-4-yl}methanone. The tributylstannylprecursor was synthesized with a yield of 30%. Radiolabelling was performed using an electrophilic iododestannylation. Tracer yield was 80%, radiochemical purity was >95% and specific activity was at least 55 Ci/micromol. Log P was 1.5. The tracer showed uptake in mice brain (2.72% ID/g tissue at 5 min p.i.) and therefore will be evaluated further by regional brain biodistribution and displacement studies in rabbits.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Magnetic Resonance Spectroscopy
  • Mice
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacokinetics
  • Piperidines / pharmacology*
  • Rabbits
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / pharmacology*
  • Receptor, Serotonin, 5-HT2A / metabolism*
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon / methods*

Substances

  • (123I)-(4-fluorophenyl)(1-(2-(4-iodophenyl)ethyl)piperidin-4-yl)methanone
  • Piperidines
  • Radiopharmaceuticals
  • Receptor, Serotonin, 5-HT2A