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Radiosynthesis and Preclinical Evaluation of 11C-VA426, a Cyclooxygenase-2 Selective Ligand
المؤلفون المشاركون
Carpinelli, Assunta
Rainone, Paolo
Belloli, Sara
Reale, Annalisa
Cappelli, Andrea
Germano, Giuliani
Murtaj, Valentina
Coliva, Angela
Di Grigoli, Giuseppe
Valeri, Angela
Gianolli, Luigi
Anzini, Maurizio
Moresco, Rosa Maria
Gilardi, Maria Carla
المصدر
Contrast Media & Molecular Imaging
العدد
المجلد 2019، العدد 2019 (31 ديسمبر/كانون الأول 2019)، ص ص. 1-12، 12ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2019-09-24
دولة النشر
مصر
عدد الصفحات
12
التخصصات الرئيسية
الملخص EN
Cyclooxygenase-2 (COX-2) is involved in the inflammatory response, and its recurrent overexpression in cancers as well as in neurodegenerative disorders has made it an important target for therapy.
For this reason, noninvasive imaging of COX-2 expression may represent an important diagnostic tool.
In this work, a COX-2 inhibitor analogue, VA426 [1-(4-fluorophenyl)-3-(2-methoxyethyl)-2-methyl-5-(4-(methylsulfonil)phenyl)-1H-pyrrole], was synthesized and radiolabelled with the 11C radioisotope.
The ex vivo biodistribution profile of 11C-VA426 was evaluated in the brain and periphery of healthy rats and mice and in brain and periphery of inflammation models, based on the administration of LPS.
11C-VA426 synthesis with the tBuOK base showed optimal radiochemical yield (15 ± 2%) based on triflate activity, molar activity (range 37–148 GBq/μmol), and radiochemical purity (>95%).
Ex vivo biodistribution studies showed a fast uptake of radioactivity but a rapid washout, except in regions expressing COX-2 (lungs, liver, and kidney) both in rats and in mice, with maximum values at 30 and 10 minutes p.i., respectively.
LPS administration did not show significant effect on radioactivity accumulation.
Celecoxib competition experiments performed in rats and mice treated with LPS produced a general target unrelated reduction of radioactivity concentration in all peripheral tissues and brain areas examined.
Finally, in agreement with the negative results obtained from biodistribution experiments, radiometabolites analysis revealed that 11C-VA426 is highly unstable in vivo.
This study indicates that the compound 11C-VA426 is not currently suitable to be used as radiopharmaceutical for PET imaging.
This family of compounds needs further implementation in order to improve in vivo stability.
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Carpinelli, Assunta& Rainone, Paolo& Belloli, Sara& Reale, Annalisa& Cappelli, Andrea& Germano, Giuliani…[et al.]. 2019. Radiosynthesis and Preclinical Evaluation of 11C-VA426, a Cyclooxygenase-2 Selective Ligand. Contrast Media & Molecular Imaging،Vol. 2019, no. 2019, pp.1-12.
https://search.emarefa.net/detail/BIM-1130297
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Carpinelli, Assunta…[et al.]. Radiosynthesis and Preclinical Evaluation of 11C-VA426, a Cyclooxygenase-2 Selective Ligand. Contrast Media & Molecular Imaging No. 2019 (2019), pp.1-12.
https://search.emarefa.net/detail/BIM-1130297
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Carpinelli, Assunta& Rainone, Paolo& Belloli, Sara& Reale, Annalisa& Cappelli, Andrea& Germano, Giuliani…[et al.]. Radiosynthesis and Preclinical Evaluation of 11C-VA426, a Cyclooxygenase-2 Selective Ligand. Contrast Media & Molecular Imaging. 2019. Vol. 2019, no. 2019, pp.1-12.
https://search.emarefa.net/detail/BIM-1130297
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-1130297
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
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