Cited by 110Neurotransmitter Receptor Influence on BehaviorSchizophrenia research and treatmentParkinson's Disease Mechanisms and Treatments

Effect of amphetamine on dopamine D2 receptor binding in nonhuman primate brain: a comparison of the agonist radioligand [11C]MNPA and antagonist [11C]raclopride

Open access
Seneca, Nicholas, Finnema, Sjoerd J., Farde, Lars, Gulyás, Balázs, Wikström, Håkan V., Halldin, Christer, Innis, Robert B.·2006·Synapse

Abstract

PET measurements of stimulant-induced dopamine (DA) release are typically performed with antagonist radioligands that bind to both the high- and low-affinity state of the receptor. In contrast, an agonist radioligand binds preferentially to the high-affinity state and is expected to have greater sensitivity to DA, which is the endogenous agonist. [(11)C]MNPA, (R)-2-CH(3)O-N-n-propylnorapomorphine (MNPA), is a D(2) agonist radioligand with subnanomolar affinity to the D(2) receptor. The aim of the present study is to assess and compare the sensitivity of the agonist radioligand [(11)C]MNPA and antagonist radioligand [(11)C]raclopride to synaptic DA levels. Four cynomolgus monkeys were examined with [(11)C]MNPA and [(11)C]raclopride (16 PET measurements with each tracer) at baseline and after pretreatment with various doses of amphetamine. The effect of amphetamine was calculated by the change in binding potential (BP) analyzed with the multilinear reference tissue model (MRTM2). Amphetamine caused a reduction in [(11)C]MNPA BP of 4% at 0.1, 23% at 0.2, 25% at 0.5, and 46% at 1.0 mg/kg. [(11)C]Raclopride BP was reduced to a lesser extent by 2% at 0.1, 16% at 0.2, 15% at 0.5, and 23% at 1.0 mg/kg. The data were used to estimate the in vivo percentage of high-affinity state receptors to be approximately 60%. These results demonstrate that [(11)C]MNPA is more sensitive than [(11)C]raclopride to displacement by endogenous DA, and that it may provide additional information about the functional state of the D(2) receptor in illnesses such as schizophrenia and Parkinson's disease.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Integrity signals

Registry

Crossref · 10.1002/syn.20238

Cites

57 of 57 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

A few free checks a day · papers already verified open instantly · results are public

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Cites

Flagged first, then by citations

Research works printed but not linked: 1

  1. Langer O, Na ˚gren K, Dolle F, Lundkvist C, Sandell J, Swahn C, Vaufrey F, Crouzel C, Maziere B, Halldin C. 1999. Precursor syn- thesis and radiolabelling of the dopamine. J Labelled Comp Rad 42:1183-1193.

Cited by

Sorted by citations

Authors
Seneca, N., Finnema, S. J., Farde, L., Gulyás, B., Wikström, H. V., Halldin, C., & Innis, R. B.
Affiliations
  • National Institutes of Health (US)
  • Karolinska University Hospital (SE)
  • University of Groningen (NL)
Corresponding author
Seneca, Nicholas
Venue
Synapse
Publisher
Wiley
Published
2006
Volume
59
Issue
5
Pages
260-269
ISSN
  • 0887-4476 (ISSN-L)
  • 1098-2396
OpenAlex
W2053445747
Cited by
110
References
57
Citations by year
2025: 1 · 2021: 2 · 2020: 2 · 2019: 4 · 2018: 7 · 2017: 6 · 2016: 3 · 2015: 7 · 2014: 8 · 2013: 6 · 2012: 8
FWCI
4.53
Type
journal article
Language
en
Open access
Locations
  • Synapse (publishedVersion, public-domain)
  • PubMed (publishedVersion)
  • University of Groningen research database (University of Groningen / Centre for Information Technology) (submittedVersion)
Funders
  • Karolinska Institutet
  • National Institutes of Health
  • National Institute of Mental Health
Topics
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
  • Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
  • Health Sciences › Medicine › Neurology › Parkinson's Disease Mechanisms and Treatments
Keywords
amphetamine, dopamine D2 receptor, [11C]raclopride, high-affinity receptor state, synaptic dopamine, binding potential, Macaca fascicularis, dopamine release, schizophrenia, Parkinson's disease
MeSH terms
Amphetamine, Animals, Binding, Competitive, Brain, Brain Chemistry, Dose-Response Relationship, Drug, Macaca fascicularis, Naproxen, Protein Binding, Time Factors, Tissue Distribution, Receptors, Dopamine D2, Dopamine Agonists, Dopamine Antagonists, Dopamine Uptake Inhibitors, Radiopharmaceuticals, Raclopride, 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 ›

Are you an author, or do you see a problem with this page? Request a review