Development of 125I-labeled probe for the detection of macrophage-like cells in inflammatory lesion

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K15459
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Radiation science
• Research Institution: Kyoto Pharmaceutical University
• Principal Investigator: Kawashima Hidekazu 京都薬科大学, 薬学部, 准教授 (70359438)
• Co-Investigator(Renkei-kenkyūsha): Ohkura Kazue 北海道医療大学, 薬学部, 教授 (60094827) ; Oshima Nobuhiro 北海道医療大学, 薬学部, 助教 (80508648)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: 炎症 / マクロファージ / 分子イメージング / 放射線 / プリン受容体

Outline of Final Research Achievements

Purinoceptor (P2Y6 subtype) is expressed on the surface of macrophage-like cells at inflamed tissue. The purpose of this study was to develop a novel radioligand targeting to P2Y6 receptor which can quantitatively detect the inflammatory lesion.
Uridine diphosphate is known as a selective endogenous ligand for P2Y6 receptor. Based on the consideration of structure-activity relationship, iodine-125 was introduced at C5 position on the uridine site of UDP and then [125I]5-I-UDP was synthesized. When [125I]5-I-UDP was intravenously injected to mice bearing inflammation induced by the subcutaneous treatment of turpentine, 1.6 times higher radioactivity was accumulated at the inflammatory lesion compared to the unaffected site. However, further investigations are needed to improve both yield and radiochemical purity.

Free Research Field

放射性医薬品