Quantification of human nicotinic acetylcholine receptors with 123I-5IA SPECT

Journal of Nuclear Medicine

Volumn 45, Issue 9, 2004, Pages 1458-1470

  Mamede, Marcelo ^a   Ishizu, Koichi ^a   Ueda, Masashi ^a   Mukai, Takahiro ^a   Iida, Yasuhiko ^a   Fukuyama, Hidenao ^a   Saga, Tsuneo ^a   Saji, Hideo ^a  

^a KYOTO UNIVERSITY   (Japan)

Author keywords

5 123I iodo 3 (2(S) azetidinylmethoxy)pyridine; Compartmental model analysis; Distribution volume; Human brain; Logan plot; Nicotinic acetylcholine receptors; Quantitative measurement; SPECT

Indexed keywords

5 IODO 3 (2 AZETIDINYLMETHOXY)PYRIDINE; IODINE 123; NICOTINIC RECEPTOR; RADIOLIGAND; UNCLASSIFIED DRUG; 5-IODO-3-(2-AZETIDINYLMETHOXY)PYRIDINE; AZETIDINE DERIVATIVE; DIAGNOSTIC AGENT; PYRIDINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT;

ADULT; ARTICLE; BLOOD BRAIN BARRIER; BRAIN CORTEX; BRAIN PERFUSION; BRAIN REGION; BRAIN STEM; CEREBELLUM; CHOLINERGIC SYSTEM; COGNITION; COMPARTMENT MODEL; CONTROLLED STUDY; DEGENERATIVE DISEASE; FEMALE; HUMAN; IMAGE ANALYSIS; ISOTOPE LABELING; KINETICS; LEARNING; MALE; MEMORY; NEUROIMAGING; NEUROPHYSIOLOGY; NORMAL HUMAN; PRIORITY JOURNAL; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY; THALAMUS; AGED; BIOLOGICAL MODEL; BLOOD; BRAIN; CLINICAL TRIAL; COMPARATIVE STUDY; COMPUTER ASSISTED DIAGNOSIS; COMPUTER SIMULATION; CONTROLLED CLINICAL TRIAL; ISOTOPE DILUTION ASSAY; METABOLIC CLEARANCE RATE; METABOLISM; METHODOLOGY; MIDDLE AGED; REPRODUCIBILITY; SCINTISCANNING; SENSITIVITY AND SPECIFICITY; TISSUE DISTRIBUTION; VALIDATION STUDY;

ADULT; AGED; AZETIDINES; BRAIN; COMPUTER SIMULATION; FEMALE; HUMANS; IMAGE INTERPRETATION, COMPUTER-ASSISTED; MALE; METABOLIC CLEARANCE RATE; MIDDLE AGED; MODELS, BIOLOGICAL; PYRIDINES; RADIOISOTOPE DILUTION TECHNIQUE; RADIOPHARMACEUTICALS; RECEPTORS, NICOTINIC; REPRODUCIBILITY OF RESULTS; SENSITIVITY AND SPECIFICITY; TISSUE DISTRIBUTION;

EID: 6944243782     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (32)

1. Lindstrom J, Anand R, Peng X, Gerzanich V, Wang F, Li Y. Neuronal nicotinic receptor subtypes. Ann NY Acad Sci. 1995;757:100-116.
2. Paterson D, Nordberg A. Neuronal nicotinic receptors in the human brain. Prog Neurobiol. 2000;61:75-111.
3. Whiting P, Esch F, Shimasaki S, Lindstrom J. Neuronal nicotinic acetylcholine receptor beta-subunit is coded for by the cDNA clone alpha 4. FEBS Lett. 1987;219:459-463.
4. Flores CM, Rogers SW, Pabreza LA, Wolfe BB, Kellar KJ. A subtype of nicotinic cholinergic receptor in rat brain is composed of alpha 4 and beta 2 subunits and is up-regulated by chronic nicotine treatment. Mol Pharmacol. 1992;41:31-37.
5. Zoli M, Lena C, Picciotto MR, Changeux JP. Identification of four classes of brain nicotinic receptors using beta2 mutant mice. J Neurosci. 1998;18:4461-4472.
6. Changeux JP, Bertrand D, Corringer PJ, et al. Brain nicotinic receptors: structure and regulation, role in learning and reinforcement. Brain Res Brain Res Rev. 1998;26:198-216.
7. Whitehouse PJ, Au KS. Cholinergic receptors in aging and Alzheimer's disease. Prog Neuropsychopharmacol Biol Psychiatry. 1986;10:665-676.
8. Perry EK, Morris CM, Court JA, et al. Alteration in nicotine binding sites in Parkinson's disease, Lewy body dementia and Alzheimer's disease: possible index of early neuropathology. Neuroscience. 1995;64:385-395.
9. 3H]epibatidine binding in relation to vesicular acetylcholine transport sites in the temporal cortex in Alzheimer's disease. Neuroscience. 1999;94:685-696.
10. Shimohama S, Taniguchi T, Fujiwara M, Kameyama M. Changes in nicotinic and muscarinic cholinergic receptors in Alzheimer-type dementia. J Neurochem. 1986;46:288-293.
11. Marks MJ, Romm E, Gaffney DK, Collins AC. Nicotine-induced tolerance and receptor changes in four mouse strains. J Pharmacol Exp Ther. 1986;237:809-819.
12. 3H]nicotine binding sites in human brain. J Neurochem. 1988;50:1243-1247.
13. Perry DC, Davila-Garcia MI, Stockmeier CA, Kellar KJ. Increased nicotinic receptors in brains from smokers: membrane binding and autoradiography studies. J Pharmacol Exp Ther. 1999;289:1545-1552.
14. 3H]nicotine binding in human postmortem brain. J Pharmacol Exp Ther. 1997;282:7-13.
15. Sullivan JP, Donnelly-Roberts D, Briggs CA, et al. A-85380 [3-(2(S)-azetidinylmethoxy)pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand. Neuropharmacology. 1996;35:725-734.
16. Koren AO, Horti AG, Mukhin AG, et al. 2-, 5-, and 6-Halo-3-(2(S)- azetidinylmethoxy) pyridines: synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling. J Med Chem. 1998;41:3690-3698.
17. Mukhin AG, Gundisch D, Horti AG, et al. 5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors. Mol Pharmacol. 2000;57:642-649.
18. Saji H, Ogawa M, Ueda M, et al. Evaluation of radioiodinated 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine as a ligand for SPECT investigations of brain nicotinic acetylcholine receptors. Ann Nucl Med. 2002;16:189-200.
19. 123I]iodo-A-85380 using single photon emission computed tomography. Life Sci. 1998;63:PL355-PL360.
20. Musachio JL, Scheffel U, Finley PA, et al. 5-[I-125/123]iodo-3(2(S)- azetidinylmethoxy) pyridine, a radioiodinated analog of A-85380 for in vivo studies of central nicotinic acetylcholine receptors. Life Sci. 1998;62:PL351-PL357.
21. Musachio JL, Villemagne VL, Scheffel UA, et al. Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon. Nucl Med Biol. 1999;26:201-207.
22. 123I]5-I-A-85380 SPECT. J Nucl Med. 2000;41:1552-1560.
23. 123I]5-I-A- 85380 in healthy human subjects. Eur J Nucl Med. 2002;29:183-190.
24. Vaupel DB, Tella SR, Huso DL, et al. Pharmacology, toxicology, and radiation dosimetry evaluation of [I-123]5-I-a-85380, a radioligand for in vivo imaging of cerebral neuronal nicotinic acetylcholine receptors in humans. Drug Dev Res. 2003;58:149-168.
25. Mintum MA, Raichle ME, Kilbourn MR, Wooten GF, Welch MJ. A quantitative model for the in vivo assessment of drug binding sites with positron emission tomography. Ann Neurol. 1984;15:217-227.
26. 11C-methyl]-(-)-cocaine PET studies in human subjects. J Cereb Blood Flow Metab. 1990;10:740-747.
27. 18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine as a PET tracer for nicotinic acetylcholine receptors. Nucl Med Biol. 2000;27:381-389.
28. 18F]F-A-85380: PET imaging of brain nicotinic acetylcholine receptors and whole body distribution in humans. FASEB J. 2003;17:1331-1333.
29. 3H]epibatidine. Brain Res. 1998;801:143-149.
30. Xiao Y, Meyer EL, Thompson JM, Surin A, Wroblewski J, Kellar KJ. Rat alpha3/beta4 subtype of neuronal nicotinic acetylcholine receptor stably expressed in a transfected cell line: pharmacology of ligand binding and function. Mol Pharmacol. 1998;54:322-333.
31. Kulak JM, Sum J, Musachio JL, McIntosh JM, Quik M. 5-Iodo-A-85380 binds to α-conotoxin MII-sensitive nicotinic acetylcholine receptors (nAChRs) as well as α4β2* subtypes. J Neurochem. 2002;81:403-406.
32. Carson RE. Mathematical modeling and compartmental analysis. In: Harbert J, Eckelman WC, Neumann R, eds. Nuclear Medicine: Diagnosis and Therapy. New York, NY: Thieme Medical; 1996:167-194.