Systemic catechol-O-methyl transferase inhibition enables the D1 agonist radiotracer R-[11C]SKF 82957
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Systemic catechol-O-methyl transferase inhibition enables the D1 agonist radiotracer R-[11C]SKF 82957. / Palner, Mikael; McCormick, Patrick; Parkes, Jun; Knudsen, Gitte M; Wilson, Alan A.
In: Nuclear Medicine and Biology, Vol. 37, No. 7, 01.10.2010, p. 837-43.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Systemic catechol-O-methyl transferase inhibition enables the D1 agonist radiotracer R-[11C]SKF 82957
AU - Palner, Mikael
AU - McCormick, Patrick
AU - Parkes, Jun
AU - Knudsen, Gitte M
AU - Wilson, Alan A
N1 - Copyright © 2010 Elsevier Inc. All rights reserved.
PY - 2010/10/1
Y1 - 2010/10/1
N2 - 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.
AB - 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.
KW - Animals
KW - Benzazepines
KW - Benzophenones
KW - Brain
KW - Carbon Radioisotopes
KW - Catechol O-Methyltransferase
KW - Catechols
KW - Dopamine Agonists
KW - Enzyme Inhibitors
KW - Nitriles
KW - Nitrophenols
KW - Positron-Emission Tomography
KW - Radiopharmaceuticals
KW - Rats
KW - Receptors, Dopamine D1
KW - Tissue Distribution
U2 - 10.1016/j.nucmedbio.2010.04.193
DO - 10.1016/j.nucmedbio.2010.04.193
M3 - Journal article
C2 - 20870159
VL - 37
SP - 837
EP - 843
JO - Nuclear Medicine and Biology
JF - Nuclear Medicine and Biology
SN - 0969-8051
IS - 7
ER -
ID: 34142977