Systemic catechol-O-methyl transferase inhibition enables the D1 agonist radiotracer R-[11C]SKF 82957

Mikael Palner; Patrick McCormick; Jun Parkes; Gitte M Knudsen; Alan A Wilson

doi:10.1016/j.nucmedbio.2010.04.193

Systemic catechol-O-methyl transferase inhibition enables the D1 agonist radiotracer R-[11C]SKF 82957

Mikael Palner, Patrick McCormick, Jun Parkes, Gitte M Knudsen, Alan A Wilson

Department of Clinical Medicine

Research output: Contribution to journal › Journal article › Research › peer-review

15 Citations (Scopus)

Abstract

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	https://doi.org/10.1016/j.nucmedbio.2010.04.193 https://doi.org/10.1016/j.nucmedbio.2010.04.193
Publication status	Published - 1 Oct 2010

Keywords

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

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title = "Systemic catechol-O-methyl transferase inhibition enables the D1 agonist radiotracer R-[11C]SKF 82957",

abstract = "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.",

keywords = "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",

author = "Mikael Palner and Patrick McCormick and Jun Parkes and Knudsen, {Gitte M} and Wilson, {Alan A}",

year = "2010",

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doi = "10.1016/j.nucmedbio.2010.04.193",

language = "English",

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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

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

SN - 0969-8051

VL - 37

SP - 837

EP - 843

JO - Nuclear Medicine and Biology

JF - Nuclear Medicine and Biology

IS - 7

ER -