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Cited by 214Neuropeptides and Animal PhysiologyNeurotransmitter Receptor Influence on BehaviorPharmacological Receptor Mechanisms and Effects

Imaging of opioid receptors in the central nervous system

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Henriksen, Gjermund, Willoch, Frode·2008·Brain
DOI 10.1093/brain/awm255PMC PMC2367693
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Abstract

In vivo functional imaging by means of positron emission tomography (PET) is the sole method for providing a quantitative measurement of mu-, kappa and delta-opioid receptor-mediated signalling in the central nervous system. During the last two decades, measurements of changes to the regional brain opioidergic neuronal activation--mediated by endogenously produced opioid peptides, or exogenously administered opioid drugs--have been conducted in numerous chronic pain conditions, in epilepsy, as well as by stimulant- and opioidergic drugs. Although several PET-tracers have been used clinically for depiction and quantification of the opioid receptors changes, the underlying mechanisms for regulation of changes to the availability of opioid receptors are still unclear. After a presentation of the general signalling mechanisms of the opioid receptor system relevant for PET, a critical survey of the pharmacological properties of some currently available PET-tracers is presented. Clinical studies performed with different PET ligands are also reviewed and the compound-dependent findings are summarized. An outlook is given concluding with the tailoring of tracer properties, in order to facilitate for a selective addressment of dynamic changes to the availability of a single subclass, in combination with an optimization of the quantification framework are essentials for further progress in the field of in vivo opioid receptor imaging.

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Authors
Henriksen, G., & Willoch, F.
Affiliations
  • TUM Klinikum (DE)
  • University of Oslo (NO)
Corresponding author
Willoch, Frode
ORCID
Willoch, Frode
Venue
Brain
Publisher
Oxford University Press (OUP)
Published
2007-11-29
Volume
131
Issue
5
Pages
1171-1196
ISSN
  • 0006-8950 (ISSN-L)
  • 1460-2156
DOI
10.1093/brain/awm255
PMC
PMC2367693
OpenAlex
W2095336616
Cited by
214
References
7
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FWCI
0.87
Type
journal article
Language
en
Open access
Licence
other-oa
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  • Brain (publishedVersion, other-oa)
  • Europe PMC (PubMed Central) (publishedVersion, cc-by-nc)
  • PubMed Central (publishedVersion, cc-by-nc)
  • PubMed (publishedVersion)
  • mediaTUM – the media and publications repository of the Technical University Munich (Technical University Munich) (submittedVersion)
Topics
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Pharmacological Receptor Mechanisms and Effects
Keywords
opioid receptors, mu-opioid receptor, kappa opioid receptor, delta opioid receptor, positron emission tomography, PET radiotracer, receptor availability, central nervous system, chronic pain, epilepsy, stimulants, opioids
MeSH terms
Brain, Brain Mapping, Epilepsy, Humans, Ligands, Movement Disorders, Pain, Receptors, Opioid, Substance-Related Disorders, Positron-Emission Tomography

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

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