An Approach for Assaying Benzodiazepine Receptor Binding with Radioiodinated Ligand: 125I-Labeled Diazepam Derivative.

Saji, Hideo; Iida, Yasuhiko; Ariyoshi, Kazuhiko; Nakatsuka, Iwao; Kataoka, Masaki; Yoshitake, Akira; Yokoyama, Akira

doi:10.1248/bpb.16.513

Cited by 7 publications

(8 citation statements)

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“…Among these radioisotopes, there are two groups. One is radioisotopes of essential elements constituting bioactive molecules and drugs, such as 11 C and 15 O. The other is radioisotopes of nonconstituent elements of bioactive molecules and drugs, which therefore cannot be used simply to replace one of the common constituent atoms in biologically interesting compounds, such as 18 F, 123 I, and 99m Tc.…”

Section: Development and Application Of Probes For Nuclear Medical Momentioning

confidence: 99%

“…These I-2′-iododiazepam (2′-IDZ), [15][16][17] and 123 I-5-iodo-A85830 (5IA) [18][19][20][21][22][23][24][25][26][27] for imaging the dopamine D2 receptor (D2R), central benzodiazepine receptor (BZR), and nicotinic acetylcholine receptor (nAChR) in the brain, respectively. Especially, neuroreceptor imaging of the human brain with 123 I-2′-ISP was a world first as a 123 I-labeled molecular probe of neuroreceptors, and was evaluated as a pioneer study in this field [9][10][11] (Fig.…”

Section: Molecular Imaging Of Neuroreceptorsmentioning

confidence: 99%

“…Therefore this therapeutic strategy using 90 Y-labeled POZ derivatives may be promising for brachytherapy, a typical radiotherapy using "seeds" containing therapeutic radioisotopes. 89) We also developed an injectable 15 O oxygen obtained after 15 O-O 2 gas circulation into artificial lung and estimated changes in oxygen metabolism after occluding the middle cerebral artery in hypertensive rats using it. Consequently, we found that hypertension intensifies metabolic disturbances after the onset of strokes.…”

Section: Tc or 186/188mentioning

confidence: 99%

“…Consequently, we found that hypertension intensifies metabolic disturbances after the onset of strokes. [90][91][92][93] Thus injectable 15 O-O 2 could be used reliably to estimate oxygen metabolism in an infarction rat model with PET. Furthermore, we developed molecular probes for nuclear medicinal imaging targeting β-secretase in the brain, acetylcholine esterase, cyclooxygenase-2 (COX-2), epidermal growth factor receptor (EGFR), and hepatic organic anion transporter (OATP1B1).…”

Section: Tc or 186/188mentioning

confidence: 99%

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<i>In Vivo</i> Molecular Imaging

Saji

2017

Biological & Pharmaceutical Bulletin

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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 methodologies used in in vivo molecular imaging, two methodologies are of great interest from the view of high sensitivity. One is nuclear medical imaging, and distribution and kinetics of a radiolabeled molecular probe are measured using positron emission tomography (PET) and single-photon emission computed tomography (SPECT). The other is optical molecular imaging, and distribution and kinetics of a fluorescent probe are measured using a fluorescent imaging instrument. In this review, the development of imaging probes for these two methodologies is briefly discussed. In nuclear medical molecular imaging, based on structure-activity-biodistribution relationship studies for small molecule and the concept of "functional unit-binding multifunctional molecular probe" containing 3 functional units (target recognition unit, signal-releasing unit, linker unit) for peptides and proteins, we developed radiolabeled probes with high and specific accumulation to the target for neuroreceptors, β-amyloid plaques, and tau aggregates in the brain, tumors, atherosclerotic plaques, pancreatic β-cell, myocardial sympathetic nerves, and so on. We also discuss the progression of molecular imaging toward therapy (radiotheranotics). In in vivo optical molecular imaging, taking into account the characteristics of optical imaging, we designed tumor-specific optical imaging probes with characteristic imaging mechanism, including near-infrared (NIR) fluorescent probes and activatable probes. Furthermore, we developed a photoacoustic imaging probe, which enables highly sensitive and high-resolution imaging in deep tissues.

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Section: Development and Application Of Probes For Nuclear Medical Momentioning

confidence: 99%

Section: Molecular Imaging Of Neuroreceptorsmentioning

confidence: 99%

Section: Tc or 186/188mentioning

confidence: 99%

Section: Tc or 186/188mentioning

confidence: 99%

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<i>In Vivo</i> Molecular Imaging

Saji

2017

Biological & Pharmaceutical Bulletin

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“…1). 21 •22 This compound was found to have a high affinity for cerebral benzodiazepine receptors, approximately 9 times greater than that of diazepam (K, = 0.66 nM). 21 z2 In addition, radioiodinated 2'-IDZ was synthesized and was found to bind to benzodiazepine receptors in vivo.…”

Section: Introductionmentioning

confidence: 99%

11C-labeled 2′-iododiazepam for PET studies of benzodiazepine receptors: Synthesis and comparison of biodistribution with its radioiodinated compound

et al. 1994

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For PET studies of benzodiazepine receptors, N-11C-methyl-2'-iododiazepam (2'-IDZ) was synthesized by N-methylation of its desmethyl derivative with 11C-methyl iodide, and was subsequently purified by HPLC. The labeling and purification procedures were completed within 45 min after 11C-methyl iodide trapping, and the radiochemical yield (corrected for decay) was approximately 40% based on the initial trapped radioactivity of 11C-methyl iodide. Biodistribution studies in mice demonstrated that 11C-2'-IDZ was rapidly and noticeably accumulated in the brain, and subsequently decreased with time. Accumulation was greater in the cortex than in other brain regions. When compared with 125I-2'-IDZ, the distribution was almost the same until 5 min after injection, but levels were low after 20 min. Metabolic studies indicated that the difference between these two compounds in the time course of brain radioactivity distribution may be due to N-demethylation in vivo.

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