Radiofluorinated N-Octanoyl Dopamine ([18F]F-NOD) as a Tool To Study Tissue Distribution and Elimination of NOD in Vitro and in Vivo

Journal of Medicinal Chemistry
2016.0

Abstract

To mitigate pretransplantation injury in organs of potential donors, N-octanoyl dopamine (NOD) treatment might be considered as it does not affect hemodynamic parameters in braindead (BD) donors. To better assess optimal NOD concentrations for donor treatment, we report on the fast and facile radiofluorination of the NOD-derivative [F]F-NOD [F]5 for in vivo assessment of NOD's elimination kinetics by means of PET imaging. [F]5 was synthesized in reproducibly high radiochemical yields and purity (>98%) as well as high specific activities (>20 GBq/μmol). Stability tests showed no decomposition of [F]5 over a period of 120 min in rat plasma. In vitro, low cell association was found for [F]5, indicating no active transport mechanism into cells. In vivo, [F]5 exhibited a fast blood clearance and a predominant hepatobiliary elimination. As these data suggest that also NOD might be cleared fast, further pharmacokinetic evaluation is warranted.

Knowledge Graph

Similar Paper

Radiofluorinated N-Octanoyl Dopamine ([<sup>18</sup>F]F-NOD) as a Tool To Study Tissue Distribution and Elimination of NOD in Vitro and in Vivo
Journal of Medicinal Chemistry 2016.0
N-(3-[18F]Fluoropropyl)-N-nordiprenorphine: synthesis and characterization of a new agent for imaging opioid receptors with positron emission tomography
Journal of Medicinal Chemistry 1990.0
Synthesis and radiopharmacological investigation of 3-[4′-[18F]fluorobenzylidene]indolin-2-one as possible tyrosine kinase inhibitor
Bioorganic &amp; Medicinal Chemistry 2009.0
Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT
Journal of Medicinal Chemistry 1993.0
Synthesis and Evaluation of Two Positron-Labeled Nitric Oxide Synthase Inhibitors, S-[<sup>11</sup>C]Methylisothiourea and S-(2-[<sup>18</sup>F]Fluoroethyl)isothiourea, as Potential Positron Emission Tomography Tracers
Journal of Medicinal Chemistry 1996.0
Synthesis and biological evaluation of 18F labeled fluoro-oligo-ethoxylated 4-benzylpiperazine derivatives for sigma-1 receptor imaging
Bioorganic &amp; Medicinal Chemistry 2013.0
Radiofluorinated histamine H3 receptor antagonist as a potential probe for in vivo PET imaging: Radiosynthesis and pharmacological evaluation
Bioorganic &amp; Medicinal Chemistry 2012.0
Synthesis, evaluation and metabolic studies of radiotracers containing a 4-(4-[18F]-fluorobenzyl)piperidin-1-yl moiety for the PET imaging of NR2B NMDA receptors
European Journal of Medicinal Chemistry 2011.0
N-Fluoroalkylated and N-alkylated analogs of the dopaminergic D-2 receptor antagonist raclopride
Journal of Medicinal Chemistry 1990.0
Synthesis of Three Novel Fluorine-18 Labeled Analogues of <scp>l</scp>-Deprenyl for Positron Emission Tomography (PET) studies of Monoamine Oxidase B (MAO-B)
Journal of Medicinal Chemistry 2011.0