Evaluation of the kappa-opioid receptor-selective tracer [11C] GR103545 in awake rhesus macaques

European Journal of Nuclear Medicine and Molecular Imaging

Volumn 37, Issue 6, 2010, Pages 1174-1180

  Schoultz, Bent W ^a   Hjornevik, Trine ^a,b   Willoch, Frode ^a,b   Marton, János ^c   Noda, Akihiro ^d   Murakami, Yoshihiro ^d   Miyoshi, Sosuke ^d   Nishimura, Shintaro ^d   Årstad, Erik ^e   Drzezga, Alexander ^f   Matsunari, Ichiro ^d   Henriksen, Gjermund ^a,f  

^a UNIVERSITY OF OSLO   (Norway)

^b AKERSHUS UNIVERSITY HOSPITAL   (Norway)

^c ABX Advanced Biochemical Compounds GmbH   (Germany)

^d Medical and Pharmacological   (Japan)

^e UNIVERSITY COLLEGE LONDON   (United Kingdom)

^f TECHNICAL UNIVERSITY OF MUNICH   (Germany)

Author keywords

11C; GR103545; Kappa; Opioid receptor; PET imaging

Indexed keywords

4 [(3,4 DICHLOROPHENYL)ACETYL] 3 (1 PYRROLIDINYLMETHYL) 1 PIPERAZINECARBOXYLIC ACID METHYL ESTER C 11; KAPPA OPIATE RECEPTOR; RADIOPHARMACEUTICAL AGENT; TRACER; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BINDING ASSAY; BRAIN REGION; CEREBELLUM; CINGULATE GYRUS; CLONE; CORPUS STRIATUM; DISTRIBUTION VOLUME; FRONTAL CORTEX; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; IN VITRO STUDY; KINETICS; MACACA; MALE; NEUROIMAGING; NONHUMAN; PARIETAL LOBE; POSITRON EMISSION TOMOGRAPHY; RADIOACTIVITY; TEMPORAL CORTEX; THALAMUS; WAKEFULNESS;

ANIMALS; CARBON RADIOISOTOPES; MACACA MULATTA; PIPERAZINES; POSITRON-EMISSION TOMOGRAPHY; PYRROLIDINES; RADIOACTIVE TRACERS; RECEPTORS, OPIOID, KAPPA; SUBSTRATE SPECIFICITY; WAKEFULNESS;

EID: 77954887345     PISSN: 16197070     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00259-010-1384-6     Document Type: Article

References (25)

1. Mansour A, Khachaturian H, Lewis ME, Akil H, Watson SJ. Anatomy of CNS opioid receptors. Trends Neurosci 1988;11:308-14.
2. Henriksen G, Willoch F. Imaging of opioid receptors in the central nervous system. Brain 2008;131:1171-96.
3. Glick SD, Maisonneuve IM, Raucci J, Archer S. Kappa opioid inhibition of morphine and cocaine self-administration in rats. Brain Res 1995;681:147-52.
4. Prisinzano TE. Natural products as tools for neuroscience: discovery and development of novel agents to treat drug abuse. J Nat Prod 2009;72:581-7.
5. Mathieu-Kia AM, Fan LQ, Kreek MJ, Simon EJ, Hiller JM. Mu-, delta-and kappa-opioid receptor populations are differentially altered in distinct areas of postmortem brains of Alzheimer's disease patients. Brain Res 2001;893:121-34.
6. Romualdi P, Bregola G, Donatini A, Capobianco A, Simonato M. Region-specific changes in prodynorphin mRNA and ir-dynorphin A levels after kindled seizures. J Mol Neurosci 1999;13:69-75.
7. Naylor A, Judd DB, Lloyd JE, Scopes DI, Hayes AG, Birch PJ. A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino) methyl]piperazines. J Med Chem 1993;36:2075-83.
8. Ravert HT, Mathews WB, Musachio JL, Scheffel U, Finley P, Dannals RF. [11C]-methyl 4-[(3, 4-dichlorophenyl) acetyl]-3-[(1-pyrrolidinyl)-methyl]-1- piperazinecarboxylate ([11C]GR89696): synthesis and in vivo binding to kappa opiate receptors. Nucl Med Biol 1999;26:737-41.
9. Ravert HT, Scheffel U, Mathews WB, Musachio JL, Dannals RF. [(11) C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers. Nucl Med Biol 2002;29:47-53.
10. Talbot PS, Narendran R, Butelman ER, Huang Y, Ngo K, Slifstein M, et al. 11C-GR103545, a radiotracer for imaging kappa-opioid receptors in vivo with PET: synthesis and evaluation in baboons. J Nucl Med 2005;46:484-94.
11. Schoultz BW, Arstad E, Marton J, Willoch F, Drzezga A, Wester HJ, et al. A new method for radiosynthesis of 11C-labeled carbamate groups and its application for a highly efficient synthesis of the kappa-opioid receptor tracer [11C]GR103545. Open Med Chem J 2008;2:72-4.
12. Noda A, Takamatsu H, Minoshima S, Tsukada H, Nishimura S. Determination of kinetic rate constants for 2-[18F]fluoro-2-deoxy-D-glucose and partition coefficient of water in conscious macaques and alterations in aging or anesthesia examined on parametric images with an anatomic standardization technique. J Cereb Blood Flow Metab 2003;23:1441-7.
13. Minoshima S, Berger KL, Lee KS, Mintun MA. An automated method for rotational correction and centering of three-dimensional functional brain images. J Nucl Med 1992;33:1579-85.
14. Minoshima S, Koeppe RA, Frey KA, Kuhl DE. Anatomic standardization: linear scaling and nonlinear warping of functional brain images. J Nucl Med 1994;35:1528-37.
15. Akaike H. A new look at the statistical model identification. IEEE Trans Automat Contr 1974; AC-19:716-23.
16. Simonin F, Befort K, Gavériaux-Ruff C, Matthes H, Nappey V, Lannes B, et al. The human delta-opioid receptor: genomic organization, cDNA cloning, functional expression, and distribution in human brain. Mol Pharmacol 1994;46:1015-21.
17. Simonin F, Gavériaux-Ruff C, Befort K, Matthes H, Lannes B, Micheletti G, et al. Kappa-opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology and expression pattern in the central nervous system. Proc Natl Acad Sci U S A 1995;92:7006-10.
18. Wang JB, Johnson PS, Persico AM, Hawkins AL, Griffin CA, Uhl GR. Human mu opiate receptor: cDNA and genomic clones, pharmacologic characterization and chromosomal assignment. FEBS Lett 1994;338:217-22.
19. Cohen RM, Andreason PJ, Doudet DJ, Carson RE, Sunderland T. Opiate receptor avidity and cerebral blood flow in Alzheimer's disease. J Neurol Sci 1997;148:171-80.
20. Hume SP, Lingford-Hughes AR, Nataf V, Hirani E, Ahmad R, Davies AN, et al. Low sensitivity of the positron emission tomography ligand [11C]diprenorphine to agonist opiates. J Pharmacol Exp Ther 2007;322:661-7.
21. 18F]fluoroethyl)-6-O-desmethyldiprenorphine ([18F]DPN): synthesis, biologic evaluation, and comparison with [11C]DPN in humans. J Nucl Med 2000;41:1279-86.
22. Butelman ER, Ko MCH, Traynor JR, Vivian JA, Kreek MJ, Woods JH. GR89, 696: a potent kappa-opioid agonist with subtype selectivity in rhesus monkeys. J Pharmacol Exp Ther 2001;298:1049-59.
23. Seeman P, Kapur S. Anesthetics inhibit high-affinity states of dopamine D2 and other G-linked receptors. Synapse 2003;50:35-40.
24. Schadrack J, Willoch F, Platzer S, Bartenstein P, Mahal B, Dworzak D, et al. Opioid receptors in the human cerebellum: evidence from [11C]diprenorphine PET, mRNA expression and autoradiography. Neuroreport 1999;10:619-24.
25. Pfeiffer A, Pasi A, Mehraein P, Herz A. Opiate receptor binding sites in human brain. Brain Res 1982;248:87-96.