PET and SPECT imaging of the opioid system

Receptors, radioligands and avenues for drug discovery and development

Research output: Contribution to journalArticle

Abstract

As we celebrate the bicentennial of the isolation of morphine by Sertümer, opioids continue to dominate major sectors of the analgesic market worldwide. The pharmaceutical industry stands to benefit greatly from molecular imaging in preclinical and early clinical trials of new or improved opioid drugs. At this juncture, it seems fitting to summarize the past twenty or so years of research on molecular imaging of the opioid system from the viewpoint of drug discovery and development. Opioid receptors were first imaged in human volunteers by positron emission tomography (PET) in 1984. Now, quantitative PET imaging of the major opioid receptor types (μ, δ, κ) is possible in the brain and peripheral organs of healthy persons and patient populations. Radioligands are under development for single photon emission computed tomography (SPECT) of opioid receptors as well. These functional, nuclear imaging techniques can trace the fate of radio-labeled molecules directly, but non-invasively, and allow precise pharmacokinetic and pharmacodynamic measurements. Molecular imaging provides unique data that can aid in selecting the best drug candidates, determining optimal dosing regimens, clearing regulatory hurdles and lowering risks of failure. Using a historical perspective, this review touches on opioid receptors as drug targets, and focuses on the status and use of radiotracers for opioid receptor PET and SPECT. Selected studies are discussed to illustrate the power of molecular imaging for facilitating opioid drug discovery and development.

Original languageEnglish (US)
Pages (from-to)33-49
Number of pages17
JournalCurrent Pharmaceutical Design
Volume13
Issue number1
DOIs
StatePublished - Jan 2007
Externally publishedYes

Fingerprint

Opioid Receptors
Drug Discovery
Single-Photon Emission-Computed Tomography
Molecular Imaging
Positron-Emission Tomography
Opioid Analgesics
Pharmaceutical Preparations
Drug Industry
Radio
Morphine
Analgesics
Volunteers
Pharmacokinetics
Clinical Trials
Brain
Research
Population

Keywords

  • Carbon-11
  • Carfentanil
  • Diprenorphine
  • Iodine-123
  • Naltrindole
  • Opioid receptor
  • PET
  • SPECT

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

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abstract = "As we celebrate the bicentennial of the isolation of morphine by Sert{\"u}mer, opioids continue to dominate major sectors of the analgesic market worldwide. The pharmaceutical industry stands to benefit greatly from molecular imaging in preclinical and early clinical trials of new or improved opioid drugs. At this juncture, it seems fitting to summarize the past twenty or so years of research on molecular imaging of the opioid system from the viewpoint of drug discovery and development. Opioid receptors were first imaged in human volunteers by positron emission tomography (PET) in 1984. Now, quantitative PET imaging of the major opioid receptor types (μ, δ, κ) is possible in the brain and peripheral organs of healthy persons and patient populations. Radioligands are under development for single photon emission computed tomography (SPECT) of opioid receptors as well. These functional, nuclear imaging techniques can trace the fate of radio-labeled molecules directly, but non-invasively, and allow precise pharmacokinetic and pharmacodynamic measurements. Molecular imaging provides unique data that can aid in selecting the best drug candidates, determining optimal dosing regimens, clearing regulatory hurdles and lowering risks of failure. Using a historical perspective, this review touches on opioid receptors as drug targets, and focuses on the status and use of radiotracers for opioid receptor PET and SPECT. Selected studies are discussed to illustrate the power of molecular imaging for facilitating opioid drug discovery and development.",
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