Systemic catechol-O-methyl transferase inhibition enables the D1 agonist radiotracer R-[11C]SKF 82957
Research output: Contribution to journal › Journal article › Research › peer-review
R-[(11)C]-SKF 82957 is a high-affinity and potent dopamine D(1) receptor agonist radioligand, which gives rise to a brain-penetrant lipophilic metabolite. In this study, we demonstrate that systemic administration of catechol-O-methyl transferase (COMT) inhibitors blocks this metabolic pathway, facilitating the use of R-[(11)C]-SKF 82957 to image the high-affinity state of the dopamine D(1) receptor with PET.
| Original language | English |
|---|---|
| Journal | Nuclear Medicine and Biology |
| Volume | 37 |
| Issue number | 7 |
| Pages (from-to) | 837-43 |
| Number of pages | 7 |
| ISSN | 0969-8051 |
| DOIs | |
| Publication status | Published - 1 Oct 2010 |
- Animals, Benzazepines, Benzophenones, Brain, Carbon Radioisotopes, Catechol O-Methyltransferase, Catechols, Dopamine Agonists, Enzyme Inhibitors, Nitriles, Nitrophenols, Positron-Emission Tomography, Radiopharmaceuticals, Rats, Receptors, Dopamine D1, Tissue Distribution
Research areas
ID: 34142977