Human PET studies of metabotropic glutamate receptor subtype 5 with 11C-ABP688

Journal of Nuclear Medicine

Volumn 48, Issue 2, 2007, Pages 247-252

  Ametamey, Simon M ^a,d   Treyer, Valerie ^b   Streffer, Johannes ^b   Wyss, Matthias T ^b   Schmidt, Mark ^c   Blagoev, Milen ^a   Hintermann, Samuel ^c   Auberson, Yves ^c   Gasparini, Fabrizio ^c   Fischer, Uta C ^b   Buck, Alfred ^b  

^a ETH ZURICH   (Switzerland)

^b UNIVERSITY OF ZURICH   (Switzerland)

^c NOVARTIS PHARMA AG   (Switzerland)

^d ETH Zurich   (Switzerland)

Author keywords

11C ABP688; Metabotropic glutamate receptor subtype 5; Positron emission tomography; Specific distribution volume

Indexed keywords

3 (6 METHYLPYRIDIN 2 YLETHYNYL)CYCLOHEX 2 ENONE O METHYLOXIME C 11; ABP 688; LIGAND; METABOTROPIC RECEPTOR 5; OXYGEN 15; RADIOISOTOPE; UNCLASSIFIED DRUG; 3 (6 METHYLPYRIDIN 2 YLETHYNYL)CYCLOHEX 2 ENONE O METHYLOXIME; 3-(6-METHYLPYRIDIN-2-YLETHYNYL)CYCLOHEX-2-ENONE-O-METHYLOXIME; DIAGNOSTIC AGENT; METABOTROPIC RECEPTOR; OXIME; PYRIDINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT;

ADULT; AMYGDALOID NUCLEUS; ARTERIAL BLOOD; ARTICLE; BLOOD SAMPLING; BRAIN PERFUSION; BRAIN REGION; CAUDATE NUCLEUS; CEREBELLUM; CINGULATE GYRUS; CLEARANCE; COMPARTMENT MODEL; DISTRIBUTION VOLUME; DRUG METABOLISM; DRUG SELECTIVITY; DRUG UPTAKE; FRONTAL CORTEX; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; NUCLEAR MAGNETIC RESONANCE IMAGING; OCCIPITAL CORTEX; OUTCOME ASSESSMENT; PARIETAL LOBE; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PUTAMEN; QUANTITATIVE ANALYSIS; RADIOACTIVITY; RECEPTOR DENSITY; TEMPORAL LOBE; WHITE MATTER; ANIMAL; BRAIN; ISOTOPE LABELING; METABOLISM; MOUSE; MOUSE MUTANT; STATISTICAL ANALYSIS; SYNTHESIS;

ADULT; ANIMALS; BRAIN; DATA INTERPRETATION, STATISTICAL; HUMANS; ISOTOPE LABELING; MAGNETIC RESONANCE IMAGING; MALE; MICE; MICE, KNOCKOUT; OXIMES; POSITRON-EMISSION TOMOGRAPHY; PYRIDINES; RADIOPHARMACEUTICALS; RECEPTORS, METABOTROPIC GLUTAMATE;

EID: 34047226403     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (28)

1. Pin JP, Duvoisin R. The metabotropic glutamate receptors: structure and functions. Neuropharmacology. 1995;34:1-26.
2. Spooren WP, Gasparini F, Salt TE, Kuhn R. Novel allosteric antagonists shed light on mGluR5 and CNS disorders. Trends Pharmacol Sci. 2001;22:331-337.
3. Gereau RW, Conn PJ. Roles of specific metabotropic glutamate receptor subtypes in regulation of hippocampal CA1 pyramidal cell excitability. J Neurophysiol. 1995;74:122-129.
4. Spooren WP, Vassout A, Neijt HC, et al. Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6- (phenylethynyl)-pyridine in rodents. J Pharmacol Exp Ther. 2000;295:1267-1275.
5. Tatarczynska E, Klodzinska A, Chojnacka-Wojcik E, et al. Potential anxiolyticand antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist. Br J Pharmacol. 2001;132:1423-1430.
6. Ohnuma T, Augood SJ, Arai H, McKenna PJ, Emson PC. Expression of the human excitatory amino acid transporter 2 and metabotropic glutamate receptors 3 and 5 in the prefrontal cortex from normal individuals and patients with schizophrenia. Brain Res Mol Brain Res. 1998;56:207-217.
7. Rouse ST, Marino MJ, Bradley SR, Awad H, Wittmann M, Conn PJ. Distribution and roles of metabotropic glutamate receptors in the basal ganglia motor circuit: implications for treatment of Parkinson's disease and related disorders. Pharmacol Ther. 2000;88:427-435.
8. Chiamulera C, Epping-Jordan MP, Zocchi A, et al. Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice. Nat Neurosci. 2001;4:873-874.
9. Walker K, Bowes M, Panesar M, et al. Metabotropic glutamate receptor subtype 5 (mGluR5) and nociceptive function. I. Selective blockade of mGluR5 in models of acute, persistent and chronic pain. Neuropharmacology. 2001a;40:1-9.
10. Walker K, Reeve A, Bowes M, et al. MGluR5 and nociceptive function II. MGluR5 functionally expressed on peripheral sensory neurones mediate inflammatory hyperalgesia. Neuropharmacology. 2001b;40:10-19.
11. Sotgiu ML, Bellomi P, Biella GE. The mGluR5 selective antagonist 6-methyl-2-(phenylethynyl)-pyridine reduces the spinal neuron pain-related activity in mononeuropathic rats. Neurosci Lett. 2003;342:85-88.
12. 3H-M-MPEP, a potent subtype selective radioligand for the metabotropic glutamate receptor subtype 5. Bioorg Med Chem Lett. 2002;12:407-409.
13. 3H-methoxyPEPy, an mGluR5 selective radioligand. Life Sci. 2003;73:371-379.
14. Gasparini F, Lingenhohl K, Stoehr N, et al. 2-Methyl-6-(phenylethynyl)- pyridine (MPEP), a potent, selective and systemically active mGluR5 antagonist. Neuropharmacology. 1999;38:1493-1503.
15. Ametamey SM, Kessler L, Honer M, et al. Radiosynthesis and preclinical evaluation of 11C-ABP688 as a probe for imaging metabotropic glutamate receptor subtype 5 (mGluR5). J Nucl Med. 2006;47:698-705.
16. 11C-M-MPEP as a PET ligand for imaging the metabotropic glutamate receptor 5 (mGluR5). J Labelled Compds Radiopharm. 2001;44:231.
17. Hamill TG, Krause S, Ryan C, et al. Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers. Synapse. 2005;56:205-216.
18. 11C-ABP688 as a probe for imaging the metabotropic glutamate receptor subtype 5. J Nucl Med. 2006;47:698-705.
19. 11C-radiolabelling of a tropane derivative lacking the 2β-ester group: a potential tracer for the dopamine transporter. J Labelled Compds Radiopharm. 1999;42:447-456.
20. Mikolajczyk K, Szabatin M, Rudnicki P, Grodzki M, Burger CA. JAVA environment for medical image data analysis: initial application for brain PET quantitation. Med Inform (Lond). 1998;23:207-214.
21. Alpert NM, Eriksson L, Chang JY, et al. Strategies for the measurement of regional cerebral flow using short-lived tracers and emission tomography. J Cereb Blood Flow Metab. 1984;4:28-34.
22. Buck A, Westera G, vonSchulthess G, Burger C. Modeling alternatives for cerebral carbon-11 iomazenil kinetics. J Nucl Med. 1996;37:699-705.
23. 11C]methylpiperidin-4-yl propionate: alternatives for analysis of an irreversible positron emission tomography trace for measurement of acetylcholinesterase activity in human brain. J Cereb Blood Flow Metab. 1999;19:1150-1163.
24. Akaike H. A new look at the statistical model identification. IEEE Trans Automat Contr. 1974;AC19:716-723.
25. Wilson AA, Houle S. Radiosynthesis of carbon-11 labeled N-methyl 2-(arylthio)benzylamines: potential tracers for the serotonin reuptake receptor. J Labelled Compds Radiopharm. 1999;42:1277-1288.
26. Romano C, Sesma MA, McDonald MT, O'Malley K, Van den Pol AN, Olney JW. Distribution of metabotropic glutamate receptor 5 (mGluR5) immunoreactivity in rat brain. J Comp Neurol. 1995;355:455-469.
27. Daggett LP, Sacaan AI, Akong M, et al. Molecular cloning and characterization of recombinant human metabotropic glutamate receptor subtype 5. Neuropharmacology. 1995;34:871-886.
28. Blumcke I, Behle K, Malitschek B, et al. Immunohistochemical distribution of metabotropic glutamate receptor subtypes mGluR1b, mGluR2/3, mGluR4a and mGluR5 in human hippocampus. Brain Res. 1996;736:217-226.