Details

Autor(en) / Beteiligte

• Sanad, M.H.
• Sallam, Kh.M.
• Marzook, F.A.
• Abd-Elhaliem, S.M.

Titel

Radioiodination and biological evaluation of candesartan as a tracer for cardiovascular disorder detection

Ist Teil von

• Journal of labelled compounds & radiopharmaceuticals, 2016-10, Vol.59 (12), p.484-491

Ort / Verlag

England: Blackwell Publishing Ltd

Erscheinungsjahr

2016

Link zum Volltext

Quelle

Wiley Online Library All Journals

Beschreibungen/Notizen

• The goal of the study aims to evaluate newly radioiodinated candesartan (CAN) as a potential cardiovascular tracer. CAN was labeled using 125I with chloramine‐T (Ch‐T) and N‐bromosuccinimide (NBS) with full characterization of cold Iodo‐candesartan. Factors such as pH, reaction temperature, reaction time, substrate, and oxidizing agent amounts were studied to optimize the radioiodination of CAN. The optimum radiochemical yield of 125I‐CAN was 98%. The labeled compound was separated and purified using high‐pressure liquid chromatography. The biological distribution indicates the suitability of 125I‐CAN as a novel tracer to detect cardiovascular disorders. Candesartan is angiotensin II receptor blocker (ARB) was labeled with iodine (125) in the presence of 75 μg of candesartan, 50 μg of Ch‐T, at pH 8, at room temperature and 15 minutes reaction time. With high radiochemical yield, high purity and in vivo / in vitro stability. That accumulated in heart with high ratio, make it a tracer for cardiovascular disorder detection.