Identification of lead compounds for 99mTc and 18F GPR91 radiotracers

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:25

Article

Klenc, Jeffrey¹  Lipowska, Malgorzata¹  Taylor, Andrew T.¹ 

[1] Emory Univ, Dept Radiol & Imaging Sci, Atlanta, GA 30322 USA

关键词: GPR91;    Radiotracer;    Hyperglycemia;    Hypoxia;    Diabetes;    Lead identification;   

DOI  :  10.1016/j.bmcl.2015.04.015

来源: Elsevier

【 摘 要 】

To develop the first radiotracer targeting GPR91, a cell membrane-bound receptor that modulates the cellular response to hyperglycemia and hypoxia, we designed and prepared a small series of compounds based on a published series of 1,8-naphthyridines with high affinity to GPR91. Our approach provides a mechanism to incorporate radioactive atoms (Tc-99m and F-18) into the GPR91 pharmacophore as the final synthetic step. Pharmacological assays confirmed lead compounds for Tc-99m and F-18 GPR91 radiotracers within the series. (C) 2015 Elsevier Ltd. All rights reserved.

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