التفاصيل البيبلوغرافية
| العنوان: |
Novel [ 18 F]-Labeled Meta-Bromobenzylguanidine Derivatives: Potential Positron Emission Tomography Imaging Probes for the Norepinephrine Transporter |
| المؤلفون: |
Xiaoyan Li (117291), Shuyu Shi (9357888), Hang Zhou (230977), Zuoquan Zhao (1728325), Jie Lu (139953) |
| سنة النشر: |
2021 |
| المجموعة: |
Smithsonian Institution: Digital Repository |
| مصطلحات موضوعية: |
Biophysics, Biochemistry, Medicine, Cell Biology, Genetics, Physiology, Biotechnology, Environmental Sciences not elsewhere classified, Chemical Sciences not elsewhere classified, Physical Sciences not elsewhere classified, optimal pharmacokinetic properties, ] mibg ), 5 min p, 45 ± 0, 44 ± 0, 120 min p, 04 μm ), 00 ± 0, iodobenzylguanidine ([< sup, 18 , 123 , ]- labeled meta, novel [< sup, b >< sup, 12 , 50 , promising pet radiotracer, >- bromobenzylguanidine derivatives, 1 mechanism specific, [< sup |
| الوصف: |
To develop novel norepinephrine transporter (NET)-targeting positron emission tomography (PET) probes with optimal pharmacokinetic properties, a series of meta -bromobenzylguanidine derivatives was synthesized. 4-Fluorodiethoxyethane-3-bromobenzylguanidine (compound 12 ) showed relatively good affinity for the NET (IC 50 = 1.00 ± 0.04 μM). The corresponding radiotracer 18 F-12 was prepared in high radiochemical purity (>98%) via a three-step method. The in vitro cellular uptake results demonstrated that 18 F-12 was specifically taken up by NET-expressing SK-N-SH cells by the uptake-1 mechanism. Biodistribution studies in mice showed that 18 F-12 exhibited high cardiac uptake (10.45 ± 0.66 %ID/g at 5 min p.i. and 6.44 ± 0.40 %ID/g at 120 min p.i.), faster liver clearance, and a lower dose of absorbed radiation than [ 123 I]-labeled meta-iodobenzylguanidine ([ 123 I]MIBG). Small animal PET imaging confirmed the high heart-to-background ratio of 18 F-12 and the uptake-1 mechanism specific for the NET in rats, indicating its potential as a promising PET radiotracer for cardiac sympathetic nerve imaging. |
| نوع الوثيقة: |
article in journal/newspaper |
| اللغة: |
unknown |
| العلاقة: |
https://figshare.com/articles/journal_contribution/Novel_sup_18_sup_F_-Labeled_Meta-Bromobenzylguanidine_Derivatives_Potential_Positron_Emission_Tomography_Imaging_Probes_for_the_Norepinephrine_Transporter/16616587Test |
| DOI: |
10.1021/acs.molpharmaceut.1c00429.s001 |
| الإتاحة: |
https://doi.org/10.1021/acs.molpharmaceut.1c00429.s001Test |
| حقوق: |
CC BY-NC 4.0 |
| رقم الانضمام: |
edsbas.51E4FF4D |
| قاعدة البيانات: |
BASE |
