Literature DB >> 25908514

Identification of lead compounds for (99m)Tc and (18)F GPR91 radiotracers.

Jeffrey Klenc1, Malgorzata Lipowska2, Andrew T Taylor2.   

Abstract

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 ((99m)Tc and (18)F) into the GPR91 pharmacophore as the final synthetic step. Pharmacological assays confirmed lead compounds for (99m)Tc and (18)F GPR91 radiotracers within the series.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Diabetes; GPR91; Hyperglycemia; Hypoxia; Lead identification; Radiotracer

Mesh：

Substances：

Year:  2015        PMID： 25908514      PMCID： PMC4433761          DOI： 10.1016/j.bmcl.2015.04.015

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  17 in total

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Journal:  Ann Nucl Med       Date:  2002-04       Impact factor: 2.668

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Review 3.  High glucose and renin release: the role of succinate and GPR91.

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5.  Preclinical evaluation of 99mTc(CO)3-aspartic-N-monoacetic acid, a renal radiotracer with pharmacokinetic properties comparable to 131I-o-iodohippurate.

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8.  99mTc(CO)3-nitrilotriacetic acid: a new renal radiopharmaceutical showing pharmacokinetic properties in rats comparable to those of 131I-OIH.

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9.  The succinate receptor GPR91 in neurons has a major role in retinal angiogenesis.

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Review 10.  Recent advances in tissue (pro)renin imaging.

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Journal:  Front Biosci (Elite Ed)       Date:  2010-06-01
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1.  Identification and pharmacological characterization of succinate receptor agonists.

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