In vivo binding of [11C]nemonapride to sigma receptors in the cortex and cerebellum.

@article{Ishiwata1999InVB,
  title={In vivo binding of [11C]nemonapride to sigma receptors in the cortex and cerebellum.},
  author={Kiichi Ishiwata and Michio Senda},
  journal={Nuclear medicine and biology},
  year={1999},
  volume={26 6},
  pages={
          627-31
        }
}
Radiolabeled nemonapride (NEM, YM-09151-2) is widely used as a representative dopamine D2-like receptor ligand in pharmacological and neurological studies, and 11C-labeled analog ([11C]NEM) has been developed for positron emission tomography (PET) studies. The aim of this study was to evaluate whether [11C]NEM binds in vivo to sigma receptors. [11C]NEM and one of six dopamine D2-like receptor ligands or seven sigma receptor ligands were co-injected into mice, and the regional brain uptake of… 
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TLDR
Findings support that both [11C]raclopride and [ 11C]SA4503 are selective in vivo ligands for dopamine D(2)-like receptors and sigma(1) receptors, respectively, in spite of the partial blocking effect of SA4503 on the striatal uptake of [11 C]racLopride.
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The role of σ-receptors in levodopa-induced dyskinesia in patients with advanced Parkinson disease: a positron emission tomography study
Object. Levodopa-induced dyskinesia (LID) in patients with Parkinson disease (PD) mimics acute dystonic reactions induced by antipsychotic agents, possibly mediated by σ-receptors; however, there are
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References

SHOWING 1-10 OF 25 REFERENCES
Multiple [3H]-nemonapride binding sites in calf brain
TLDR
Three areas of calf brain were examined and [3H]-nemonapride has no selectivity for dopamine receptors unless stringent experimental conditions are met.
Differential labeling of dopamine and sigma sites by [3H]nemonapride and [3H]raclopride in postmortem human brains
TLDR
The nemonapride-raclopride subtraction method was applied to postmortem, non-schizophrenic human striatum to examine the variation in dopaminergic receptor binding labeled by these ligands and no significant nor consistent observation of striatal dopamine D4 receptors or D4-like binding sites was observed in the striatum.
[3H]YM‐09151–2 (nemonapride), a potent radioligand for both sigma1 and sigma2 receptor subtypes
TLDR
[3H]YM-09151–2 is a potent and useful radioligand for sigma1/sigma2 receptor subtypes and also showed a characteristic distribution of sigma receptors in rat brain.
In vivo binding of [3H]d-N-allylnormetazocine and [3H]haloperidol to sigma receptors in the mouse brain.
Specific binding to sigma sites has been demonstrated and characterized in vitro using [3H]d-N-allylnormetazocine ([3H]d-NANM) and [3H]haloperidol ([3H]HAL) as ligands. As an extension of these
Effects of reserpine treatment on the dopamine receptor binding of [3H/11C]nemonapride in the mouse and rat brain
TLDR
The results suggest that the receptor binding of NEM was not significantly influenced by reserpine-induced depletion of endogenous dopamine probably because of its high affinity for the receptors.
Brain σ receptors labelled by [3H]nemonapride
Binding of [3H]nemonapride and [3H]raclopride was examined in the brain areas of three species (rat, cow and human). The results indicated that [3H]nemonapride binding is inhibited by selective sigma
D2-dopamine receptor specific brain uptake of carbon-11-labeled YM-09151-2.
TLDR
The present results demonstrate that [11C]YM-09151-2 is a D2 receptor specific compound and is a potential in vivo tracer for measuring D2 receptors.
Synthesis and Preliminary Evaluation of [11C]NE-100 Labeled in Two Different Positions as a PET σ Receptor Ligand
N,N-Dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]ethylamine (NE-100) was labeled with 11C in two different positions by the alkylation of an N-despropyl precursor with [11C]propyl iodide and of an
Measurement of D2 dopamine receptor-specific carbon-11-YM-09151-2 binding in the canine brain by PET: importance of partial volume correction.
  • J. Hatazawa, K. Hatano, +6 authors S. Seo
  • Chemistry, Medicine
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine
  • 1991
TLDR
The present study demonstrates the importance of partial volume correction and the Bmax/Kd measurement in a single PET study with carbon-11-YM-09151-2 and the bound-to-free ligand ratio in the striatum at equilibrium was consistent with the Scatchard analysis.
Quantitative ex vivo and in vitro receptor autoradiography using 11C-labeled ligands and an imaging plate: a study with a dopamine D2-like receptor ligand [11C]nemonapride.
TLDR
The photo-stimulated luminescence (PSL) values of the rat brain section provided by the imaging plates showed an excellent linear relationship with the radioactivity in a wide range under constant slice-thickness, although the PSL values slightly decreased with increasing slice-Thickness both in ex vivo and in vitro ARG.
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