Evaluation of novel tropane analogues in comparison with the binding characteristics of [18F]FP-CIT and [131I]β-CIT

Sihver, Wiebke; Drewes, Birte; Schulze, Annette; Olsson, Ray A.; Coenen, Heinz H.

doi:10.1016/j.nucmedbio.2006.11.005

Cited by 10 publications

(4 citation statements)

References 46 publications

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“…The electrophilic radioiodination of β-CIT was performed using either Chloramine T or Iodo-Gen ® as an oxidizing agent followed by SPE purification according to previous methods [14,15,23,24,25], with some modifications. The precursor TMS-β-CIT was purchased from ABX Advanced Biochemical Compounds GmbH (Radeberg, Germany).…”

Section: Methodsmentioning

confidence: 99%

“…The radiolabeling of molecules, including β-CIT, with radioactive iodine ( 123 I, 124 I, 125 I or 131 I) is frequently based on electrophilic aromatic substitution using several oxidizing agents such as Chloramine T (N-chloro-p-toluenesulfonamide sodium salt), Iodo-Gen ® (1,3,4,6-tetrachloro-3α,6β-diphenylglycouril), lactoperoxidase, and the solid-state variants as pre-coated Iodo-Gen ® tubes, Iodo-Beads ® , or Enzymobeads ® . The most commonly used are Chloramine T and Iodo-Gen ® , at room temperature [13,14,15,16].…”

Section: Introductionmentioning

confidence: 99%

“…Chloramine T has been used since 1962 [17]. It is a strong oxidizing agent, demanding shorter reaction periods, and is soluble in aqueous solutions [15,18]. On the other hand, Iodo-Gen ® is a moderate oxidizing agent, requiring longer reaction times, and is insoluble under aqueous conditions [19,20].…”

Section: Introductionmentioning

confidence: 99%

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Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen®, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson’s Disease

et al. 2019

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Parkinson’s disease (PD) is a neurodegenerative disease characterized by the loss of dopaminergic neurons in the substantia nigra pars compacta, leading to alteration of the integrity of dopaminergic transporters (DATs). In recent years, some radiopharmaceuticals have been used in the clinic to evaluate the integrity of DATs. These include tropane derivatives such as radiolabeled β-CIT and FP-CIT with iodine-123 (123I), and TRODAT-1 with metastable technetium-99 (99mTc). Radiolabeling of β-CIT with radioactive iodine is based on electrophilic radioiodination using oxidizing agents, such as Chloramine T or Iodo-Gen®. For the first time, the present work performed a comparative study of the radiolabeling of β-CIT with iodine-131 (131I), using either Chloramine T or Iodo-Gen® as oxidizing agents, in order to improve the radiolabeling process of β-CIT and to choose the most advantageous oxidizing agent to be used in nuclear medicine. Both radiolabeling methods were similar and resulted in high radiochemical yield (> 95%), with suitable 131I-β-CIT stability up to 72 h. Although Chloramine T is a strong oxidizing agent, it was as effective as Iodo-Gen® for β-CIT radiolabeling with 131I, with the advantage of briefer reaction time and solubility in aqueous medium.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen®, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson’s Disease

et al. 2019

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“…[ [22]. Thus, we hypothesized that pretreatment with fluvoxamine could affect the results of [ 18 F]FP-CIT PET in small animals and also in humans.…”

Section: Introductionmentioning

confidence: 99%

Effect of Animal Condition and Fluvoxamine on the Result of [18F]N-3-Fluoropropyl-2β-carbomethoxy-3β-(4-iodophenyl) Nortropane ([18F]FP-CIT) PET Study in Mice

Shin

Park

Kim

et al. 2011

Nucl Med Mol Imaging

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Purpose PET (positron emission tomography) is a noninvasive imaging technique, visualizing biological aspects in vivo. In animal models, the result of PET study can be affected more prominently than in humans by the animal conditions or drug pretreatment. We assessed the effects of anesthesia, body temperature, and pretreatment with selective serotonin reuptake inhibitor on the results of18 F]FP-CIT PET of C57BL/6 mice was performed in three different conditions: (1) anesthesia (isoflurane) with active warming (38°C) as a reference; (2) no anesthesia or warming; (3) anesthesia without warming at room temperature. Additional groups of mice pretreated with escalating doses of fluvoxamine (5, 20, 40, 80 mg/kg) were imaged in condition (1). The time activity curve and standardized uptake value of the striatum, cerebral cortex, and bone were compared among these conditions. Results In all conditions, radioactivities of the striatum and cortex tended to form a plateau after rapid uptake and washout, but that of bone tended to increase gradually. When anesthetized without any warming, all the mice developed hypothermia and showed reduced bone uptake with slightly increased striatal and cortical uptakes compared to the reference condition. In conditions without anesthesia, striatal and cortical uptakes were reduced, whereas the bone uptake showed no change. Pretreatment with fluvoxamine increased the striatal uptake and striatal specific to cortical non-specific uptake ratio, whereas the bone uptake was reduced. Conclusion Anesthesia, body temperature, and fluvoxamine affect the result of [18 F]FP-CIT PET in mice by altering striatal and bone uptakes.

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Nuclear Medicine Imaging Tracers for Neurology

Elsinga

2020

PET and SPECT in Neurology

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Evaluation of novel tropane analogues in comparison with the binding characteristics of [18F]FP-CIT and [131I]β-CIT

Cited by 10 publications

References 46 publications

Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen®, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson’s Disease

Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen®, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson’s Disease

Effect of Animal Condition and Fluvoxamine on the Result of [18F]N-3-Fluoropropyl-2β-carbomethoxy-3β-(4-iodophenyl) Nortropane ([18F]FP-CIT) PET Study in Mice

Nuclear Medicine Imaging Tracers for Neurology

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