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Journal of Nuclear Medicine

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Meeting ReportMolecular Targeting Probes - Radioactive and Nonradioactive

Single-step radiosynthesis and in vivo evaluation of a novel fluorine-18 labeled hippurate for use as a PET renal agent

Gopal Pathuri, Andria Hedrick, Vibhudutta Awasthi and Hariprasad Gali
Journal of Nuclear Medicine May 2012, 53 (supplement 1) 1566;
Gopal Pathuri
1Pharmaceutical Sciences, The University of Oklahoma College of Pharmacy, Oklahoma City, OK
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Andria Hedrick
1Pharmaceutical Sciences, The University of Oklahoma College of Pharmacy, Oklahoma City, OK
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Vibhudutta Awasthi
1Pharmaceutical Sciences, The University of Oklahoma College of Pharmacy, Oklahoma City, OK
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Hariprasad Gali
1Pharmaceutical Sciences, The University of Oklahoma College of Pharmacy, Oklahoma City, OK
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Abstract

1566

Objectives The objective of this study was to investigate a new fluorine-18 labeled hippurate, m-cyano-p-18F-fluorohippurate (18F-CNPFH), as a potential radiopharmaceutical for evaluating renal function by PET.

Methods 18F-CNPFH was synthesized by a direct one-step nucleophilic aromatic substitution of 18F-for-+N(CH3)3 reaction. In vivo stability was determined by HPLC analysis of urine collected from a healthy rat at 30 min p.i. of 18F-CNPFH. The plasma protein binding (PPB) and erythrocyte uptake of 18F-CNPFH were determined using blood collected from healthy rats at 5 min p.i. Biodistribution studies were conducted in healthy rats at 10 min and 1 hr p.i. of 18F-CNPFH. Dynamic PET/CT imaging data was acquired in normal rats. For comparison, the same rats underwent identical imaging study using previously reported p-18F-fluorohippurate (18F-PFH) renal agent.

Results 18F-CNPFH demonstrated high in vivo stability with no metabolic degradation. The in vivo PPB and erythrocyte uptake of 18F-CNPFH was found to be comparable to 18F-PFH. Biodistribution and dynamic PET/CT imaging studies revealed a rapid clearance of 18F-CNPFH primarily through renal-urinary pathway. However, unlike 18F-PFH, a minor (about 12%) fraction eliminated via hepatobiliary route. The PET-derived 18F-CNPFH renograms revealed an average time-to-peak (Tmax) of 3.2 ± 0.4 min which was similar to 18F-PFH, but the average time-to-half-maximal activity (11.4 ± 2.8 min) was found to be higher than 18F-PFH (7.1 ± 1.3 min).

Conclusions Our in vivo results indicate that 18F-CNPFH has renogram characteristics similar to that of 18F-PFH, however, the unexpected hepatobiliary elimination is adding undesirable background signal in the PET images.

Research Support This work was funded by the University of Oklahoma College of Pharmacy Startup Grant

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Journal of Nuclear Medicine
Vol. 53, Issue supplement 1
May 2012
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Single-step radiosynthesis and in vivo evaluation of a novel fluorine-18 labeled hippurate for use as a PET renal agent
Gopal Pathuri, Andria Hedrick, Vibhudutta Awasthi, Hariprasad Gali
Journal of Nuclear Medicine May 2012, 53 (supplement 1) 1566;

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Single-step radiosynthesis and in vivo evaluation of a novel fluorine-18 labeled hippurate for use as a PET renal agent
Gopal Pathuri, Andria Hedrick, Vibhudutta Awasthi, Hariprasad Gali
Journal of Nuclear Medicine May 2012, 53 (supplement 1) 1566;
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