Evaluation of carbon-11-labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-iodoethenyl)phenyl]nortropane as a potential radioligand for imaging the serotonin transporter by PET

J Med Chem. 2006 Feb 9;49(3):942-6. doi: 10.1021/jm050799v.

Abstract

The nortropane cocaine analogue, 2beta-carbomethoxy-3beta-[4'-((Z)-2-iodoethenyl)phenyl]nortropane (ZIENT), is a high affinity, selective serotonin transporter (SERT) ligand that has shown promise as a SERT imaging agent for single photon computed tomography (SPECT) when labeled with I-123. Synthesis of the labeling precursor, radiosynthesis of [(11)C]ZIENT, and in vivo evaluation in anesthetized and awake monkeys have been performed to determine the suitability of [(11)C]ZIENT as a PET agent for SERT imaging.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Brain / diagnostic imaging
  • Brain / metabolism
  • Carbon Radioisotopes
  • Isotope Labeling
  • Macaca fascicularis
  • Macaca mulatta
  • Male
  • Nortropanes / chemical synthesis*
  • Nortropanes / chemistry
  • Nortropanes / pharmacokinetics
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacokinetics
  • Serotonin Plasma Membrane Transport Proteins / metabolism*

Substances

  • 2-carbomethoxy-3-(4'-(2-iodoethenyl)phenyl)nortropane
  • Carbon Radioisotopes
  • Nortropanes
  • Radiopharmaceuticals
  • Serotonin Plasma Membrane Transport Proteins