Validation of an extracerebral reference region approach for the quantification of brain nicotinic acetylcholine receptors in squirrel monkeys with PET and 2-18F-fluoro-A-85380

Journal of Nuclear Medicine

Volumn 48, Issue 9, 2007, Pages 1492-1500

  Le Foll, Bernard ^a,b   Chefer, Svetlana I ^a   Kimes, Alane S ^a   Shumway, Dean ^a   Goldberg, Steven R ^a   Stein, Elliot A ^a   Mukhin, Alexey G ^a,c  

^a NATIONAL INSTITUTE ON DRUG ABUSE   (United States)

^b UNIVERSITY OF TORONTO   (Canada)

^c DUKE UNIVERSITY MEDICAL CENTER   (United States)

Author keywords

In vivo binding; Nicotinic acetylcholine receptors; Nonhuman primates; PET; Radioligand

Indexed keywords

2 FLUORO 3 (2 AZETIDINYLMETHOXY)PYRIDINE FLUORODEOXYGLUCOSE F 18; 3 (2 AZETIDINYLMETHOXY)PYRIDINE; BRAIN RECEPTOR; FLUORODEOXYGLUCOSE F 18; NICOTINE; NICOTINIC RECEPTOR; RADIOLIGAND; RECEPTOR SUBUNIT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BRAIN CORTEX; BRAIN REGION; CEREBELLUM; CORRELATION ANALYSIS; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; MALE; MUSCLE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RADIOISOTOPE DISTRIBUTION; REPRODUCIBILITY; SQUIRREL MONKEY; THALAMUS; VALIDATION PROCESS;

ANIMALS; AZETIDINES; BRAIN; CEREBELLUM; FLUORINE RADIOISOTOPES; MALE; MODELS, BIOLOGICAL; MUSCLE, SKELETAL; NICOTINE; NICOTINIC AGONISTS; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RECEPTORS, NICOTINIC; REFERENCE VALUES; SAIMIRI;

EID: 34548595377     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.107.039776     Document Type: Article

References (35)

1. Lammertsma AA, Hume SP. Simplified reference tissue model for PET receptor studies. Neuroimage. 1996;4:153-158.
2. Ding YS, Gatley SJ, Fowler JS, et al. Mapping nicotinic acetylcholine receptors with PET. Synapse. 1996;24;403-407.
3. 18F]F-A-85380: a PET radioligand for alpha4beta2 nicotinic acetylcholine receptors. Neuroreport. 1999;10:2715-2721.
4. 18F-fluoro-A-85380. J Nucl Med. 1999;40:1374-1380.
5. 18F]F-A-85380: PET imaging of brain nicotinic acetylcholine receptors and whole body distribution in humans. FASEB J. 2003;17:1331-1333.
6. 18F-fluoro-A-85380 in healthy volunteers. J Nucl Med. 2003;44:596-601.
7. Vaupel DB, Tella SR, Huso DL, et al. Pharmacological and toxicological evaluation of 2-fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-F-A-85380), a ligand for imaging cerebral nicotinic acetylcholine receptors with positron emission tomography. J Pharmacol Exp Ther. 2005;312:355-365.
8. Ichise M, Meyer JH, Yonekura Y. An introduction to PET and SPECT neuroreceptor quantification models. J Nucl Med. 2001;42:755-763.
9. 18F]Fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors. Nucl Med Biol. 1998;25:599-603.
10. National Research Council. Guidelines for the Care and Use of Mammals in Neuroscience and Behavioral Research. Washington, DC: The National Academy Press; 2003.
11. Gergen GA, MacLean PD. A Stereotaxic Atlas of the Brain of the Squirrel Monkey (Saimiri sciureus). Bethesda, MD: National Institutes of Health, Public Health Service, U.S. Department of Health, Education, and Welfare; 1962.
12. 18F]F-A-85380 in blood plasma using solid-phase extraction. Nucl Med Biol. 2007;34:221-228.
13. Bergstrom M, Awad R, Estrada S, et al. Autoradiography with positron emitting isotopes in positron emission tomography tracer discovery. Mol Imaging Biol. 2003;5:390-396.
14. Marquardt DW. An algorithm for least squares estimation of nonlinear parameters. J Soc Ind Appl Math. 1963;11:431-441.
15. Phelps ME, Huang SC, Hoffman EJ, Kuhl DE. Validation of tomographic measurement of cerebral blood volume with C-11-labeled carboxyhemoglobin. J Nucl Med. 1979;20:328-334.
16. 15O[CO and positron emission tomography. Am J Physiol. 1995;269:E1000-E1005.
17. 11C-methyl]-(-)-cocaine PET studies in human subjects. J Cereb Blood Flow Metab. 1990;10:740-747.
18. Cunningham VJ, Hume SP, Price GR, Ahier RG, Cremer JE, Jones AK. Compartmental analysis of diprenorphine binding to opiate receptors in the rat in vivo and its comparison with equilibrium data in vitro. J Cereb Blood Flow Metab. 1991;11:1-9.
19. Hume SP, Myers R, Bloomfield PM, et al. Quantitation of carbon-11-labeled raclopride in rat striatum using positron emission tomography. Synapse. 1992;12:47-54.
20. Gunn RN, Lammertsma AA, Hume SP, Cunningham VJ. Parametric imaging of ligand-receptor binding in PET using a simplified reference region model. Neuroimage. 1997;6:279-287.
21. 18F]FA binding to nicotinic acetylcholine receptors in rhesus monkey brain. Synapse. 2003;48:25-34.
22. 18F]fluoro-A-85380: a PET study in monkeys. Synapse. 2002;44:58-59.
23. 123I]5-I-A-85380 SPECT. J Nucl Med. 2000;41:1552-1560.
24. 123I]5-I-A-85380 SPET. Eur J Nucl Med Mol Imaging. 2003;30:1620-1629.
25. Ginovart N, Willeit M, Rusjan P, et al. Positron emission tomography quantification of [(11)C]-(+)-PHNO binding in the human brain. J Cereb Blood Flow Metab. 2007;27:857-871.
26. 18F-fluoro-A-85380 and PET. J Nucl Med. 2005;46:240-247.
27. Dolle F, Dolci L, Valette H, et al. Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy] pyridine: a new positron emission tomography ligand for nicotinic receptors. J Med Chem. 1999;42:2251-2259.
28. Turner JR, Kellar KJ. Nicotinic cholinergic receptors in the rat cerebellum: multiple heteromeric subtypes. J Neurosci. 2005;25:9258-9265.
29. Villemagne VL, Horti A, Scheffel U, et al. Imaging nicotinic acetylcholine receptors with fluorine-18-FPH, an epibatidine analog. J Nucl Med. 1997;38:1737-1741.
30. Paterson D, Nordberg A. Neuronal nicotinic receptors in the human brain. Prog Neurobiol. 2000;61:75-111.
31. Buisson B, Bertrand D. Nicotine addiction: the possible role of functional upregulation. Trends Pharmacol Sci. 2002;23:130-136.
32. Clozel M, Clozel JP. Effects of endothelin on regional blood flows in squirrel monkeys. J Pharmacol Exp Ther. 1989;250:1125-1131.
33. Crone C. The permeability of capillaries in various organs as determined by use of the 'indicator diffusion' method. Acta Physiol Scand. 1963;58:292-305.
34. 14C]urea pharmacokinetics. Am J Physiol. 1982;242:R339-R348.
35. Gjedde A, Wong DF, Wagner HN Jr. Transient analysis of irreversible and reversible tracer binding in human brain in vivo. In: Battistin L, Gerstenbrand F, eds. PET and NMR: New Perspectives in Neuroimaging and in Clinical Neurochemistry. New York, NY: A.R. Liss; 1986:223-235.