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Ex vivo and in vivo Evaluation of [18F]PR04.MZ in Rodents: A Selective Dopamine Transporter Imaging Agent
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Titel: |
Ex vivo and in vivo Evaluation of [18F]PR04.MZ in Rodents: A Selective Dopamine Transporter Imaging Agent |
In: | ChemMedChem, 4, 2009, 9, S. 1480-1487 |
veröffentlicht: |
Wiley
|
Umfang: | 1480-1487 |
ISSN: |
1860-7179 1860-7187 |
DOI: | 10.1002/cmdc.200900177 |
Zusammenfassung: | <jats:title>Abstract</jats:title><jats:p>N<jats:italic>‐4‐Fluorobut‐2‐yn‐1‐yl‐2β‐carbomethoxy‐3β‐phenyltropane (PR04.MZ) has been developed as dopamine transporter (DAT) ligand for molecular imaging. It contains a terminally fluorinated, conformationally constrained nitrogen substituent that is well suited for the introduction of fluorine‐18. The present report describes the pharmacological characterisation of [<jats:sup>18</jats:sup>F]PR04.MZ. The ligand shows an IC<jats:sub>50</jats:sub> value of 2 n<jats:sc>M</jats:sc> against human DAT, whereas the IC<jats:sub>50</jats:sub> value against human serotonin transporter and human noradrenalin transporter are lower (110 n<jats:sc>M</jats:sc> and 22 n<jats:sc>M</jats:sc>, respectively). Furthermore, its ex vivo organ distribution, its binding profile in the rat brain and reversibility of binding were examined. A μPET study illuminates a fast kinetic profile and specific binding to rat DAT.</jats:italic></jats:p> |
Format: | E-Article |
Quelle: | Wiley (CrossRef) |
Sprache: | Englisch |