PMID: 22571785May 11, 2012Paper

Recent advances in positron emission tomography (PET) radiotracers for imaging phosphodiesterases

Current Topics in Medicinal Chemistry
José Ignacio AndrésGuy Bormans

Abstract

Phosphodiesterases (PDEs) are a family of enzymes that metabolically inactivate the second messengers 3',5'- cyclic adenosine monophosphate (cAMP) and/or 3',5'-cyclic guanosine monophosphate (cGMP). These two messengers regulate the extracellular signal from the plasma membrane G protein-coupled receptors (GPCRs) to the intracellular effector proteins, hence modulating a wide variety of biological processes both in the central nervous system (CNS) and peripheral tissues. Although there are many radiotracers available for positron emission tomography (PET) studies of different receptors, there are just a few tracers available for imaging studies of second messenger systems. The first reported PDE PET ligands were the 11C-labeled versions of the PDE4 inhibitors rolipram and Ro 20-1724, and, to date, PET imaging studies in human subjects have only been reported with [11C]rolipram. As a consequence of the growing interest in identifying selective PDE inhibitors as potential new therapeutic agents, new PET radiotracers for imaging specific PDEs have been described in literature as well. This article highlights these efforts on the design and evaluation of novel PET radioligands for in vivo imaging of PDEs.

Citations

Dec 3, 2013·Nuclear Medicine and Biology·Rufael ChekolGuy Bormans
May 24, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Susann SchröderPeter Brust
Sep 21, 2017·Molecular Imaging·Brian P RempelChristopher P Phenix
Sep 22, 2019·European Journal of Nuclear Medicine and Molecular Imaging·Stuart P McCluskeyOliver Howes
Jun 6, 2020·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Zhidong XuQi-Huang Zheng
May 28, 2021·Journal of Medicinal Chemistry·Jiyun SunSteven H Liang
Sep 18, 2021·Journal of Neurochemistry·Natasha S R BidesiMatthias M Herth

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