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Synthesis and Labeling of P-Nh2-Bn-Dtpa-(Dabcyl-Lys6,Phe7)-Phbsp With 99Mtc As a Radiopeptide Scintigraphic Agent to Detect Cardiac Ischemia Publisher



Mohtavinejad N1 ; Bitarafanrajabi A2 ; Shafiee Ardestani M1 ; Darbandiazar A3 ; Khalaj A4 ; Ghodrati A4 ; Asadi M4 ; Amanlou M4
Authors
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Authors Affiliations
  1. 1. Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, 16 Azar Ave., Tehran, Iran
  2. 2. Department of Nuclear Medicine, Rajaie Cardiovascular Medical and Research Center, University of Medical Sciences, Tehran, Iran
  3. 3. Rajaie Cardiovascular Research Center, Iran University of Medical Sciences, Tehran, Iran
  4. 4. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

Source: Journal of Radioanalytical and Nuclear Chemistry Published:2020


Abstract

Myocardial ischemia and infarction represent a major health burden worldwide, but their immediate diagnosis can reduce mortality and healthcare costs. Pyroglutamate helix B surface peptide (pHBSP) derived from erythropoietin have shown tissue-protective effects in the ischemic situation by binding to erythropoietin receptor–Beta common receptors)EPOR–βcR(. This research aimed to synthesize and biologically evaluate p-NH2-Bn-DTPA-(Lys-Dabcyl6,Phe7)-pHBSP for cardiac ischemia imaging. Radiolabeling yielded more than 97%, and radiolabeled peptide showed significant binding affinity to H9c2 hypoxic cells (p < 0.001). A considerable accumulation of 99mTc-p-NH2-Bn-DTPA-(Lys-Dabcyl6,Phe7)-pHBSP was detected in the ischemic region by biodistribution study and SPECT/CT scintigraphy (3.84 ID/g% at 30 min). © 2020, Akademiai Kiado, Budapest, Hungary.