Synthesis and Preliminary Evaluation of <sup>18</sup>F-Labeled Pyridaben Analogues for Myocardial Perfusion Imaging with PET

Mou, Tiantian; Zhao, Zuoquan; Fang, Wei; Peng, Cheng; Guo, Feng; Liu, Boli; Ma, Yonggang; Zhang, Xianzhong

doi:10.2967/jnumed.111.088096

Cited by 24 publications

(40 citation statements)

References 21 publications

(30 reference statements)

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“…The biological properties of these probes, [ 18 F]FP1OP and [ 18 F]FP2OP (Figure ), exhibited improved properties in heart uptake and non‐target background. However, [ 18 F]FP1OP and [ 18 F]FP2OP exhibit poor stability in water, which limits their further application in the clinic . Therefore, it is necessary to modify the structure to improve the stability.…”

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confidence: 99%

Synthesis and Bio‐Evaluation of New ¹⁸F‐Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice

et al. 2015

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To improve the stability of (18) F-labeled pyridaben analogs for myocardial perfusion imaging, three new analogs of pyridaben ([(18) F]FPTP2, [(18) F]FPTP-P2, and [(18) F]FPTP-P3) were synthesized with 'side chain' modifications. The radiolabeled tracers and corresponding non-radioactive compounds were obtained by substituting tosyl group with (18/19) F. The effect of structure modification on myocardial targeting and physicochemical properties of new tracers were evaluated in vitro and in vivo. The total radiosynthesis time of these tracers was approximately 70-90 min with high decay-corrected radiochemical yields (36-65%) and good radiochemical purity (> 98%). These lipophilic tracers exhibited obvious improved stability in water. Studies of their biodistribution in normal Kunming mice demonstrated that [(18) F]FPTP2 exhibited very high initial heart uptake (39.70 ± 2.81 %ID/g at 2 min after injection) and low background in the liver, blood, and soft tissues. The heart-to-liver, heart-to-lung, and heart-to-blood ratios were 3.59, 19.34, and 67.34 at 15 min postinjection, respectively. Favorable myocardial targeting property and remarkable improvement of stability of [(18) F]FPTP2 suggest that the substitution of the phenyl 'sidechain' with other non-phenyl rings has no effect on the myocardial targeting property of (18) F-labeled pyridaben analogs.

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Synthesis and Bio‐Evaluation of New ¹⁸F‐Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice

et al. 2015

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“…Therefore, it is necessary to develop PET radiotracers for myocardial perfusion imaging (MPI) in order to improve diagnostic accuracy, reader confidence and ver- [39,40]. Among these, [ 18 F]FP1OP seems to be a potential MPI agent [40]. It showed high heart uptake and low background uptake in both the mouse model and the Chinese mini swine model.…”

Section: F-labeled Myocardial Perfusion Imaging Agentsmentioning

confidence: 98%

“…Nowadays obesity prevalence increases and poses a challenge for image quality of CAD. Therefore, it is necessary to develop PET radiotracers for myocardial perfusion imaging (MPI) in order to improve diagnostic accuracy, reader confidence and ver- [39,40]. Among these, [ 18 F]FP1OP seems to be a potential MPI agent [40].…”

Section: F-labeled Myocardial Perfusion Imaging Agentsmentioning

confidence: 99%

Radiopharmaceuticals in China: current status and prospects

Jia¹,

Liu

2014

Radiochimica Acta

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The review provides an overview of the current status of radiopharmaceuticals in China for in vivo clinical use and also describes some important advances in the past three decades. Development of the diagnostic and therapeutic radiopharmaceuticals as well as basic research on radiopharmaceutical chemistry are being introduced. The radiotracers developed in China include: (1) Brain perfusion imaging agents and CNS radiotracers for -amyloid plaques, 1 receptors, and dopamine D 2 or D 4 receptors;(2) 99m Tc-and 18 F-labeled myocardial perfusion imaging agents; (3) tumor imaging agents including integrin-targeting radiotracer, novel sentinel lymph node imaging agents, hypoxia imaging agents, 99m Tc-labeled glucose derivatives, 2 receptor imaging agents, folate receptor imaging agents, and potential radiotracers for imaging of human telomerase reverse transcriptase expression; (4) Potential infection imaging agents; (5) Potential asialoglycoprotein receptor imaging agents; (6) Other imaging agents. Moreover, some prospects of research and development of radiopharmaceuticals in the near future are discussed.

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“…Another study prompted that 2-tertbutyl-4-chloro-5-(4-(2-(2-(2- 18 F-fluoroethoxy) ethoxy) ethoxy)) benzyloxy-2H-pyridazin-3-one ( 18 F-FP3OP) had a better metabolic stability and faster clearance in myocardium compared with 18 F-FP2OP. However, 2-tertbutyl-4-chloro-5-(4-(2- 18 F-fluoro-ethoxy)) benzyloxy-2H-pyridazin-3-one ( 18 F-FP1OP) is worth developing as a new PET MPI tracer owing to its superiority over 18 F-FP3OP [65]. The instability of 18 F-FP2OP in water limits its range of applications.…”

Section: Mitochondrial-targeted Pet Agentsmentioning

confidence: 99%

Mitochondrial-Targeted Molecular Imaging in Cardiac Disease

Lu²,

Zhou

2017

BioMed Research International

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The present study aimed to discuss the role of mitochondrion in cardiac function and disease. The mitochondrion plays a fundamental role in cellular processes ranging from metabolism to apoptosis. The mitochondrial-targeted molecular imaging could potentially illustrate changes in global and regional cardiac dysfunction. The collective changes that occur in mitochondrial-targeted molecular imaging probes have been widely explored and developed. As probes currently used in the preclinical setting still have a lot of shortcomings, the development of myocardial metabolic activity, viability, perfusion, and blood flow molecular imaging probes holds great potential for accurately evaluating the myocardial viability and functional reserve. The advantages of molecular imaging provide a perspective on investigating the mitochondrial function of the myocardium in vivo noninvasively and quantitatively. The molecular imaging tracers of single-photon emission computed tomography and positron emission tomography could give more detailed information on myocardial metabolism and restoration. In this study, series mitochondrial-targeted 99mTc-, 123I-, and 18F-labeled tracers displayed broad applications because they could provide a direct link between mitochondrial dysfunction and cardiac disease.

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Synthesis and Preliminary Evaluation of ¹⁸F-Labeled Pyridaben Analogues for Myocardial Perfusion Imaging with PET

Cited by 24 publications

References 21 publications

Synthesis and Bio‐Evaluation of New ¹⁸F‐Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice

Synthesis and Bio‐Evaluation of New ¹⁸F‐Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice

Radiopharmaceuticals in China: current status and prospects

Mitochondrial-Targeted Molecular Imaging in Cardiac Disease

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Synthesis and Preliminary Evaluation of 18F-Labeled Pyridaben Analogues for Myocardial Perfusion Imaging with PET

Cited by 24 publications

References 21 publications

Synthesis and Bio‐Evaluation of New 18F‐Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice

Synthesis and Bio‐Evaluation of New 18F‐Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice

Radiopharmaceuticals in China: current status and prospects

Mitochondrial-Targeted Molecular Imaging in Cardiac Disease

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Synthesis and Preliminary Evaluation of ¹⁸F-Labeled Pyridaben Analogues for Myocardial Perfusion Imaging with PET

Synthesis and Bio‐Evaluation of New ¹⁸F‐Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice

Synthesis and Bio‐Evaluation of New ¹⁸F‐Labeled Pyridaben Analogs with Improved Stability for Myocardial Perfusion Imaging in Mice