Assessment of a7 nicotinic acetylcholine receptor availability in juvenile pig brain with [18F]NS10743

European Journal of Nuclear Medicine and Molecular Imaging

Volumn 38, Issue 8, 2011, Pages 1541-1549

  Deuther Conrad, Winnie ^a   Fischer, Steffen ^a   Hiller, Achim ^a   Becker, Georg ^b   Cumming, Paul ^c   Xiong, Guoming ^c   Funke, Uta ^a   Sabri, Osama ^b   Peters, Dan ^d   Brust, Peter ^a  

^a INSTITUTE OF ION BEAM PHYSICS AND MATERIALS RESEARCH   (Germany)

^b UNIVERSITY OF LEIPZIG   (Germany)

^c UNIVERSITY OF MUNICH   (Germany)

^d NEUROSEARCH A S   (Denmark)

Author keywords

7 nAChR; Neurology . Metabolism; Nicotinic acetylcholine receptors; PET

Indexed keywords

BUNGAROTOXIN RECEPTOR; ISOFLURANE; NS 10743; NS 10743 F 18; TRACER; UNCLASSIFIED DRUG; AZABICYCLO DERIVATIVE; DIAGNOSTIC AGENT; HETEROCYCLIC COMPOUND; NICOTINIC AGENT; NICOTINIC RECEPTOR; OXADIAZOLE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTERIAL BLOOD; ARTICLE; BINDING KINETICS; BLOOD SAMPLING; BRAIN REGION; CEREBELLUM; CONTINUOUS INFUSION; CONTROLLED STUDY; DRUG BINDING SITE; DRUG TUMOR LEVEL; DRUG UPTAKE; FEMALE; HIPPOCAMPUS; JUVENILE ANIMAL; MESENCEPHALON; MOLECULAR IMAGING; NONHUMAN; OLFACTORY BULB; PARAMETRIC TEST; POSITRON EMISSION TOMOGRAPHY; QUANTITATIVE ANALYSIS; RADIOACTIVITY; RECEPTOR BLOCKING; RECEPTOR OCCUPANCY; SWINE; TECTUM; TEMPORAL LOBE; THALAMUS; ANIMAL; BRAIN; KINETICS; METABOLISM; METHODOLOGY; SCINTISCANNING;

ANIMALS; AZA COMPOUNDS; AZABICYCLO COMPOUNDS; BRAIN; FEMALE; KINETICS; NICOTINIC AGONISTS; OXADIAZOLES; POSITRON-EMISSION TOMOGRAPHY; RECEPTORS, NICOTINIC; SWINE;

EID: 80052574182     PISSN: 16197070     EISSN: 16197089     Source Type: Journal    
DOI: 10.1007/s00259-011-1808-y     Document Type: Article

References (35)

1. Lindstrom J, Anand R, Gerzanich V, Peng X, Wang F, Wells G. Structure and function of neuronal nicotinic acetylcholine receptors. Prog Brain Res. 1996;109:125-37. (Pubitemid 27047080)
2. Gotti C, Clementi F. Neuronal nicotinic receptors: From structure to pathology. Prog Neurobiol. 2004;74(6):363-96. (Pubitemid 40092737)
3. Fucile S, Renzi M, Lax P, Eusebi F. Fractional Ca(2+) current through human neuronal alpha7 nicotinic acetylcholine receptors. Cell Calcium. 2003;34(2):205-9. (Pubitemid 36798404)
4. Breese CR, Adams C, Logel J, Drebing C, Rollins Y, Barnhart M, et al. Comparison of the regional expression of nicotinic acetylcholine receptor a7 mRNA and [125I]-a-bungarotoxin binding in human postmortem brain. J Comp Neurol. 1997;387(3):385-98. (Pubitemid 27430337)
5. Freedman R, HallM, Adler LE, Leonard S. Evidence in postmortem brain tissue for decreased numbers of hippocampal nicotinic receptors in schizophrenia. Biol Psychiatry. 1995;38(1):22-33.
6. Stephens SH, Logel J, Barton A, Franks A, Schultz J, Short M, et al. Association of the 5'-upstream regulatory region of the a7 nicotinic acetylcholine receptor subunit gene (CHRNA7) with schizophrenia. Schizophr Res. 2009;109(1-3):102-12.
7. Bencherif M, Lippiello PM. Alpha7 neuronal nicotinic receptors: The missing link to understanding Alzheimer's etiopathology? Med Hypotheses. 2010;74(2):281-5.
8. Dunlop J, Peri R, Terstappen GC, Bowlby M. Functional screening of a7 nicotinic ligands. Expert Opin Drug Discov. 2008;3(6):623-8.
9. Bunnelle WH, Dart MJ, Schrimpf MR. Design of ligands for the nicotinic acetylcholine receptors: The quest for selectivity. Curr Top Med Chem. 2004;4(3):299-334. (Pubitemid 38849362)
10. Gotti C, Balestra B,Moretti M, Rovati GE,Maggi L, Rossoni G, et al. 4-Oxystilbene compounds are selective ligands for neuronal nicotinic alphaBungarotoxin receptors. Br J Pharmacol. 1998;124(6):1197-206. (Pubitemid 28333943)
11. Maggi L, Palma E, Eusebi F, Moretti M, Balestra B, Clementi F, et al. Selective effects of a 4-oxystilbene derivative on wild and mutant neuronal chick a7 nicotinic receptor. Br J Pharmacol. 1999;126(1):285-95. (Pubitemid 29041769)
12. Meyer EM, Tay ET, Papke RL, Meyers C, Huang GL, de Fiebre CM. 3-[2,4-Dimethoxybenzylidene]anabaseine (DMXB) selectively activates rat a7 receptors and improves memory-related behaviors in a mecamylamine-sensitive manner. Brain Res. 1997;768(1-2):49-56. (Pubitemid 27433476)
13. Balestra M, Gordon JC, Griffith RC, Murray RJ. Spiro-azabicyclic compounds useful in therapy. Patent WO9606098. 1996.
14. Toyohara J, Ishiwata K, Sakata M, Wu J, Nishiyama S, Tsukada H, et al. In vivo evaluation of a7 nicotinic acetylcholine receptor agonists [11C]A-582941 and [11C]A-844606 in mice and conscious monkeys. PLoS ONE. 2010;5(2):e8961.
15. Toyohara J, Sakata M, Wu J, Ishikawa M, Oda K, Ishii K, et al. Preclinical and the first clinical studies on [11C]CHIBA-1001 for mapping a7 nicotinic receptors by positron emission tomography. Ann Nucl Med. 2009;23(3):301-9.
16. Hashimoto K, Nishiyama S, Ohba H, Matsuo M, Kobashi T, Takahagi M, et al. [11C]CHIBA-1001 as a novel PET ligand for a7 nicotinic receptors in the brain: A PET study in conscious monkeys. PLoS ONE. 2008;3(9):e3231.
17. Whiteaker P, Davies AR, Marks MJ, Blagbrough IS, Potter BV, Wolstenholme AJ, et al. An autoradiographic study of the distribution of binding sites for the novel a7-selective nicotinic radioligand [3H]-methyllycaconitine in the mouse brain. Eur J Neurosci. 1999;11(8):2689-96. (Pubitemid 29365411)
18. Davies AR, Hardick DJ, Blagbrough IS, Potter BV, Wolstenholme AJ, Wonnacott S. Characterisation of the binding of [3H] methyllycaconitine: A new radioligand for labelling a7-type neuronal nicotinic acetylcholine receptors. Neuropharmacology. 1999;38(5):679-90. (Pubitemid 29150322)
19. Mathew SV, Law AJ, Lipska BK, Davila-Garcia MI, Zamora ED, Mitkus SN, et al. a7 nicotinic acetylcholine receptor mRNA expression and binding in postmortem human brain are associated with genetic variation in neuregulin 1. Hum Mol Genet. 2007;16 (23):2921-32. (Pubitemid 350048389)
20. Tanibuchi Y, Wu J, Toyohara J, Fujita Y, Iyo M, Hashimoto K. Characterization of [3H]CHIBA-1001 binding to a7 nicotinic acetylcholine receptors in the brain from rat, monkey, and human. Brain Res. 2010;1348:200-8.
21. Deuther-Conrad W, Fischer S, Hiller A, Nielsen EO, Timmermann DB, Steinbach J, et al. Molecular imaging of a7 nicotinic acetylcholine receptors: Design and evaluation of the potent radioligand [18F]NS10743. Eur J Nucl Med Mol Imaging. 2009;36 (5):791-800.
22. Briggs CA, Gronlien JH, Curzon P, Timmermann DB, Ween H, Thorin-Hagene K, et al. Role of channel activation in cognitive enhancement mediated by a7 nicotinic acetylcholine receptors. Br J Pharmacol. 2009;158(6):1486-94.
23. Brust P, Patt JT, Deuther-Conrad W, Becker G, Patt M, Schildan A, et al. In vivo measurement of nicotinic acetylcholine receptors with [18F]norchloro-fluoro-homoepibatidine. Synapse. 2008;62 (3):205-18. (Pubitemid 351186401)
24. Gillings NM, Bender D, Falborg L, Marthi K, Munk OL, Cumming P. Kinetics of the metabolism of four PET radioligands in living minipigs. Nucl Med Biol. 2001;28(1):97-104. (Pubitemid 32155970)
25. Brust P, Zessin J, Kuwabara H, Pawelke B, Kretzschmar M, Hinz R, et al. Positron emission tomography imaging of the serotonin transporter in the pig brain using [11C](+)-McN5652 and S-[18F] fluoromethyl-(+)-McN5652. Synapse. 2003;47(2):143-51. (Pubitemid 36020286)
26. Brust P, Hinz R, Kuwabara H, Hesse S, Zessin J, Pawelke B, et al. In vivo measurement of the serotonin transporter with (S)-[18F] fluoromethyl-(+)- McN5652. Neuropsychopharmacology. 2003;28 (11):2010-9. (Pubitemid 37412110)
27. Innis RB, Cunningham VJ, Delforge J, Fujita M, Gjedde A, Gunn RN et al. Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J Cereb Blood Flow Metab. 2007:27(9):1533-9. (Pubitemid 47301451)
28. Logan J, Fowler JS, Volkow ND, Wolf AP, Dewey SL, Schlyer DJ, et al. Graphical analysis of reversible radioligand binding from time-activity measurements applied to [N-11C-methyl]-(-)- cocaine PET studies in human subjects. J Cereb Blood Flow Metab. 1990;10(5):740-7. (Pubitemid 20260955)
29. Jensen SB, Smith DF, Bender D, Jakobsen S, Peters D, Nielsen EØ, et al. [11C]-NS 4194 versus [11C]-DASB for PET imaging of serotonin transporters in living porcine brain. Synapse. 2003;49(3):170-7. (Pubitemid 36870554)
30. Hoffmeister PG, Donat CK, Schuhmann MU, Voigt C, Walter B, Nieber K et al. Traumatic brain injury elicits similar alterations in a7 nicotinic receptor density in two different experimental models. Neuromolecular Med. 2010;13(1):44-53.
31. Cumming P, Rosa-Neto P, Watanabe H, Smith D, Bender D, Clarke PB, et al. Effects of acute nicotine on hemodynamics and binding of [11C]raclopride to dopamine D2,3 receptors in pig brain. Neuroimage. 2003;19(3):1127-36. (Pubitemid 36918250)
32. Court JA, Martin-Ruiz C, Graham A, Perry E. Nicotinic receptors in human brain: Topography and pathology. J Chem Neuroanat. 2000;20(3-4):281-98. (Pubitemid 32162887)
33. Uchida S, Hotta H. Cerebral cortical vasodilatation mediated by nicotinic cholinergic receptors: Effects of old age and of chronic nicotine exposure. Biol Pharm Bull. 2009;32(3):341-4.
34. Si ML, Lee TJ. a7-nicotinic acetylcholine receptors on cerebral perivascular sympathetic nerves mediate choline-induced nitrergic neurogenic vasodilation. Circ Res. 2002;91(1):62-9. (Pubitemid 34778943)
35. Andersen F, Watanabe H, Bjarkam C, Danielsen EH, Cumming P. Pig brain stereotaxic standard space: Mapping of cerebral blood flow normative values and effect of MPTP-lesioning. Brain Res Bull. 2005;66(1):17-29. (Pubitemid 40733108)