Evaluation of radioiodinated (2S,alphaS)-2-(alpha-(2-iodophenoxy)benzyl)morpholine as a radioligand for imaging of norepinephrine transporter in the heart.

  title={Evaluation of radioiodinated (2S,alphaS)-2-(alpha-(2-iodophenoxy)benzyl)morpholine as a radioligand for imaging of norepinephrine transporter in the heart.},
  author={Yasushi Kiyono and Taku Sugita and Masashi Ueda and Hidekazu Kawashima and Naoki Kanegawa and Yuji Kuge and Yasuhisa Fujibayashi and Hideo Saji},
  journal={Nuclear medicine and biology},
  volume={35 2},
INTRODUCTION The norepinephrine transporter (NET) is located presynaptically on noradrenergic nerve terminals and plays a critical role in the regulation of the synaptic norepinephrine (NE) concentration via the reuptake of NE. Changes in NET have been recently reported in several cardiac failures. Therefore, a NET-specific radioligand is useful for in vivo assessment of changes in NET density in various cardiac disorders. Recently, we developed a radioiodinated reboxetine analogue, (2S,alphaS… 
Critical analysis of radioiodination techniques for micro and macro organic molecules
A variety of radioiodination methods is available in the literature depending upon the nature of organic compound to be labeled, however only few can completely fulfill manufacturing
Inhibition of G-Protein-Activated Inwardly Rectifying K+ Channels by the Selective Norepinephrine Reuptake Inhibitors Atomoxetine and Reboxetine
GIRK channel inhibition may contribute to some of the therapeutic effects of NRIs and adverse side effects related to nervous system and heart function and be revealed in a novel characteristic of clinically used NRIs.
Review In Vivo Molecular Imaging
In vivo molecular imaging is the visualization, characterization, and measurement of biological processes at the molecular and cellular levels in humans and other living systems. Among the
In Vivo Molecular Imaging.
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    Biological & pharmaceutical bulletin
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In in vivo optical molecular imaging, taking into account the characteristics of optical imaging, the development of tumor-specific optical imaging probes with characteristic imaging mechanism are designed, including near-infrared (NIR) fluorescent probes and activatable probes.
Neurotoxic catecholamine metabolite in nociceptors contributes to painful peripheral neuropathy
Observations suggest that catecholamines in nociceptors are metabolized to neurotoxic products by MAO‐A, which can cause neuronal dysfunction underlying neuropathic pain.
The role of central catecholamines in performance during prolonged exercise in warm conditions
Performance during prolonged exercise capacity diminishes with increasing temperatures. The onset of fatigue under these conditions is not adequately explained by peripheral mechanisms. Recently,


Synthesis and evaluation of radioiodinated (S,S)-2-(α-(2-iodophenoxy)benzyl)morpholine for imaging brain norepinephrine transporter
The synthesis of (S,S)-123I-IPBM is a potential SPECT radiopharmaceutical for imaging brain NET and shows high affinity and selectivity for NET in the binding assay experiments.
Evaluation of radioiodinated (R)-N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine as a ligand for brain norepinephrine transporter imaging.
Results suggested that (R-N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine)MIPP is a potential radiopharmaceutical for imaging brain NET.
A new norepinephrine transporter imaging agent for cardiac sympathetic nervous function imaging: radioiodinated (R)-N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine.
Results suggested that (R)-[(123)I]MIPP may be an useful radiopharmaceutical for imaging cardiac sympathetic nervous functions.
Reduced 125I-meta-iodobenzylguanidine uptake and norepinephrine transporter density in the hearts of mice with MPTP-induced parkinsonism.
This study clearly shows that reduced cardiac I-MIBG uptake in mice with MPTP-induced parkinsonism is closely related to the reduced NET density in postganglionic cardiac sympathetic nerve terminals.
Synthesis of 11C-labeled imipramine and its biodistribution in mice: A potential tracer for positron emission tomography.
A tricyclic antidepressant, 11C-labeled imipramine was synthesized by N-methylation of desipramine with 11CH3I to assist in the imaging of the human imipramine receptor by positron emission
High-affinity [3H]desipramine binding in the peripheral and central nervous system: a specific site associated with the neuronal uptake of noradrenaline.
High-affinity [3H]desipramine binding sites thus appear to be localised on Noradrenergic nerve endings and are probably closely associated with the neuronal uptake system for noradrenaline.
Interactions of phenylalkylamines with human lung membrane and microsome preparation
The results showed that the compounds can be classified in order of their decreasing affinity: Iodoamphetamine, iodoisopropylamphetamine, dimethyliodophentermine, hydroxyiodobenzyl propane diamine (HIPDM), isoproylamphetamine and amphetamine.
Synthesis and regional mouse brain distribution of [11C]nisoxetine, a norepinephrine uptake inhibitor.
  • M. Haka, M. Kilbourn
  • Chemistry, Medicine
    International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
  • 1989
Nisoxetine, a selective and high affinity inhibitor of NE reuptake, has been radiolabeled in high specific activity by the alkylation of the nor-methyl precursor with [11C]CH3I.
PET and SPET tracers for mapping the cardiac nervous system
  • O. Langer, C. Halldin
  • Chemistry, Medicine
    European Journal of Nuclear Medicine and Molecular Imaging
  • 2002
Mapping of cardiac parasympathetic neurones is limited by a low density and focal distribution pattern of these neurones in myocardium, and derivatives of vesamicol, a molecule that binds to a receptor associated with the vesicular acetylcholine transporter, restrict their utility for cardiac neuronal imaging.
Carbon-11 labeled aliphatic amines in lung uptake and metabolism studies: potential for dynamic measurements in vivo.
A comparison of a series of compounds all having a carbon chain length of eight but with different functional groups showed that the amino group as well as the relatively lipophilic alkyl group were required for lung specificity.