Characterization of r-[11C]rolipram for PET imaging of phosphodieterase-4: in vivo binding, metabolism, and dosimetry studies in rats.

@article{Lourenco2001CharacterizationOR,
  title={Characterization of r-[11C]rolipram for PET imaging of phosphodieterase-4: in vivo binding, metabolism, and dosimetry studies in rats.},
  author={Celia M. Lourenco and Sylvain Houle and Alan A. Wilson and Jean N DaSilva},
  journal={Nuclear medicine and biology},
  year={2001},
  volume={28 4},
  pages={347-58}
}
The high-affinity phosphodiesterase-4 (PDE4) inhibitor R-rolipram and the less potent S-enantiomer, both labeled with (11)C, were evaluated in vivo in rats. Regional brain uptake of R-[(11)C]rolipram was higher than R/S-[(11)C]rolipram, whereas S-[(11)C]rolipram retention subsided rapidly to levels below blood. Binding of R-[(11)C]rolipram was selective for PDE4 over PDE1, since treatment with PDE4 competitors Ro 20-1724, or R-, S- or R/S-rolipram, but not with the PDE1 inhibitor vinpocetine… CONTINUE READING

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