Academic Journal
F-Desbromo-DuP-697 as a PET Tracer for Cyclooxygenase-2 Expression
| العنوان: | F-Desbromo-DuP-697 as a PET Tracer for Cyclooxygenase-2 Expression |
|---|---|
| المؤلفون: | Erik F. J. De Vries, Phd Aren Van Waarde, Phd Anne, Rixt Buursma, Willem Vaalburg |
| المساهمون: | The Pennsylvania State University CiteSeerX Archives |
| المصدر: | http://jnm.snmjournals.org/content/44/10/1700.full.pdf. |
| المجموعة: | CiteSeerX |
| الوصف: | Cyclooxygenase-2 (COX-2) overexpression has been observed in various pathologies, such as inflammation, cancer, ischemia, and Alzheimer’s disease. As an initial step toward a noninvasive PET technique to assay COX-2 expression, this study describes the synthesis and preliminary evaluation of the radiolabeled COX-2 inhibitor 18F-desbromo-DuP-697. Methods: Desbromo-DuP-697 was radiolabeled by a nucleophilic aromatic substitution reaction of the nitro precursor with 18F-fluoride. Biodistribution studies of the tracer were performed in a carrageenaninduced hyperalgesia rat model. Brain uptake was investigated with autoradiography. To confirm the results of the biodistribution, COX activity was determined by a peroxidase assay. Results: Biodistribution studies showed specific binding of the tracer to COX-2 in heart, kidney, brain, and blood cells, but not in the inflamed paw, which was probably due to low COX-2 expression. In the brain, regional differences in tracer uptake were observed, with high uptake in cortical regions. 18F-Des bromo-DuP-697 did not show any binding to COX-1. Nonspecific uptake was high in fat and intestines. Conclusion: Because of its ability to cross the blood–brain barrier, 18F-desbromo-DuP-697 appears to be suitable for COX-2 imaging in the brain. Its high nonspecific uptake in the intestines may limit its use for imaging in the abdominal region. Key Words: PET; desbromo-DuP-697; cyclooxygenase-2; inflammation; carrageenan |
| نوع الوثيقة: | text |
| وصف الملف: | application/pdf |
| اللغة: | English |
| Relation: | http://citeseerx.ist.psu.edu/viewdoc/summary?doi=10.1.1.317.9691; http://jnm.snmjournals.org/content/44/10/1700.full.pdf |
| الاتاحة: | http://citeseerx.ist.psu.edu/viewdoc/summary?doi=10.1.1.317.9691 http://jnm.snmjournals.org/content/44/10/1700.full.pdf |
| Rights: | Metadata may be used without restrictions as long as the oai identifier remains attached to it. |
| رقم الانضمام: | edsbas.45F96CEE |
| قاعدة البيانات: | BASE |
| الوصف غير متاح. |