6-[18F]fluoro-A-85380: An in vivo tracer for the nicotinic acetylcholine receptor

Nuclear Medicine and Biology

Volumn 27, Issue 1, 2000, Pages 51-56

  Scheffel, Ursula ^a   Horti, Andrew G ^b   Koren, Andrei O ^b   Ravert, Hayden T ^a   Banta, Jeffrey P ^c   Finley, Paige A ^a   London, Edythe D ^b   Dannals, Robert F ^a  

^a DEPARTMENT OF PATHOLOGY   (United States)

^b NATIONAL INSTITUTE ON DRUG ABUSE   (United States)

^c CTI Inc   (United States)

Author keywords

6 18F FA; A 85380 derivative; Mouse brain distribution; Nicotinic acetylcholine receptor (nAChR); PET; Radiotracer

Indexed keywords

3 (2 AZETIDINYLMETHOXY)PYRIDINE; CYTISINE; FLUORINE 18; MECAMYLAMINE; NICOTINE; NICOTINIC RECEPTOR; SCOPOLAMINE; AZETIDINE DERIVATIVE; DIAGNOSTIC AGENT; FLUORINE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; COMPUTER ASSISTED EMISSION TOMOGRAPHY; CONTROLLED STUDY; DRUG DISTRIBUTION; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; FLUORINATION; IN VIVO STUDY; MALE; MOUSE; NONHUMAN; ANIMAL; BRAIN; INSTITUTE FOR CANCER RESEARCH MOUSE; METABOLISM; RADIOCHEMISTRY; SCINTISCANNING; SUBCUTANEOUS DRUG ADMINISTRATION; SYNTHESIS; TISSUE DISTRIBUTION;

ANIMALS; AZETIDINES; BRAIN; FLUORINE RADIOISOTOPES; INJECTIONS, SUBCUTANEOUS; MALE; MICE; MICE, INBRED ICR; RADIOCHEMISTRY; RECEPTORS, NICOTINIC; TISSUE DISTRIBUTION; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0033625016     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0969-8051(99)00082-7     Document Type: Article

References (32)

1. Abreo M.A., Lin N.-H., Garvey D.S., Gunn D.E., Hettinger A.-M., Wasicak J.T., Pavlik P.A., Martin Y.C., Donnelly-Roberts D.L., anderson D.J., Sullivan J.P., Williams M., Arneric S.P., Holladay M.W. Novel 3-pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors. J. Med. Chem. 39:1996;817-825.
2. Adler L.E., Olincy A., Waldo M., Harris J.G., Griffith J., Stevens K., Flach K., Nagamoto H., Bickford P., Leonard S., Freedman R. Schizophrenia, sensory gating, and nicotinic receptors. Schizophr. Bull. 24:1998;189-202.
3. 3H]l-nicotine in the mouse brain. Life Sci. 44:1989;1123-1132.
4. 123I]iodo-A-85380 using single photon emission computed tomography. Life Sci. 63:1998;355-360.
5. Decker M.W., Brioni J.D., Bannon A.W., Arneric S.P. Diversity of neuronal nicotinic acetylcholine receptor Lessons from behavior and implications for CNS therapeutics . Life Sci. 56:1995;545-570.
6. Ding Y.-S., Gatley S.J., Fowler J.S., Volkow N.D., Aggarwal D., Logan J., Dewey S.L., Liang F., Carroll F.I., Kuhar M.J. Mapping nicotinic acetylcholine receptors with PET. Synapse. 24:1996;403-407.
7. 18F]fluoro-3-[2(S)-2-azetidinylmethoxy] pyridine, a highly potent radioligand for in vivo imaging central nicotinic acetylcholine receptors. J. Labelled Compd. Radiopharm. 41:1998;451-463.
8. Flicker D.R.L., Watkins D.L., Fisher S.K., Bartus R.T. Behavioral and neurochemical effects following neurotoxic lesions of a major cholinergic input to cerebral cortex in rat. Pharmacol. Biochem. Behav. 18:1983;973-981.
9. Freedman R., Hall M., Adler L.E., Leonard S. Evidence in postmortem brain tissue for decreased numbers of hippocampal nicotinic receptors in schizophrenia. Biol. Psychiatry. 38:1995;22-33.
10. Giacobini E. Nicotinic cholinergic receptors in human brain Effects of aging and Alzheimer . Adv. Exp. Med. Biol. 296:1991;303-315.
11. Henningfield J.E., Woodson P.P. Dose-related actions of nicotine on behavior and physiology Review and implications for replacement therapy for nicotine dependence . J. Subst. Abuse. 1:1989;301-317.
12. Holladay M.W., Wasicak J.T., Lin N.-H., He Y., Ryther K.B., Kincaid J.F., Bannon A.W., Buckley M.J., Kim J.B., Decker M.W., anderson D.J., Campbell J.E., Kuntzweiler T.A., Donelly-Roberts D.L., Piattoni-Kaplan M., Briggs C.A., Williams M., Arneric S.P. Identification and initial structure-activity relationship of (R)-5-(2-azetinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, nonopioid analgesic agent acting via neuronal nicotinic acetylcholine receptors. J. Med. Chem. 41:1998;407-412.
13. 18F]Fluoro-5-pyridyl)-7-azabicyclo[2.2.1]heptane . J. Labelled Compd. Radiopharm. 38:1996;355-365.
14. 18F]FPH for PET imaging of nicotinic acetylcholine receptors. J. Nucl. Med. 38:1997;1260-1265.
15. 18F]A-85380) . J. Labelled Compd. Radiopharm. 41:1998;309-318.
16. 18F]Fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors. Nucl. Med. Biol. 25:1998;599-603.
17. 11C]-N-methylated analogs of epibatidine as tracers for PET studies of nicotinic acetylcholine receptors. J. Med. Chem. 41:1998;4199-4206.
18. 123/125I]iodo-3-(2(S)-azetidinylmethoxy)pyridine A radioligand for nicotinic acetylcholine receptors . Nucl. Med. Biol. 26:1999;175-182.
19. Irle E., Markowitsch H.J. Basal forebrain-lesioned monkeys are severely impaired in tasks of association and recognition memory. Ann. Neurol. 14:1985;1025-1032.
20. Koren A.O., Horti A.G., Mukhin A.G., Gundisch D., Kimes A.S., Dannals R.F., London E.D. 2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy) pyridines Synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling . J. Med. Chem. 41:1998;3690-3698.
21. Levin E.D., Rose J.E. Acute and chronic nicotinic interactions with dopamine systems and working memory performance. Ann. N.Y. Acad. Sci. 757:1995;245-252.
22. 3H]nicotine binding sites in the rat brain. Neurosci. Lett. 53:1985;179-184.
23. London E.D., Ball M.J., Waller S.B. Nicotinic binding sites in cerebral cortex and hippocampus in Alzheimer's dementia. Neurochem. Res. 14:1989;745-749.
24. 11C Synthesis and distribution kinetics in animals . Eur. J. Nucl. Med. 1:1976;255-258.
25. Molina P., Ding Y.S., Carroll F.I., Liang F., Volkow N., Kuhar M., Pappas N., Abumrad N., Gatley S.J., Fowler J.S. Fluoro-norchlorofluoroepibatidine (NFEP) Preclinical assessment of acute toxicity . Nucl. Med. Biol. 24:1997;743-747.
26. Musachio J. L., Scheffel U., Finley P. A., Zhan Y., Mochizuki T., Wagner H. N. and Dannals R. F. (1998) 5-[I-125/123]Iodo-3(2(S)-azetidydinylmethoxy) pyridine, a radioiodinated analog of A-85380 for in vivo studies of central nicotinic acetylcholine receptors. Life Sci. 62, PL 351-357.
27. Pert A. Cholinergic and catecholaminergic modulation of nociceptive reactions. Interactions with opiates. Akil H., Lewis J.W. Pain and Headache, Neurotransmitters and Pain Control. 1987;1-63 Karger, Basel, Switzerland.
28. Steinlein O.K., Mulley J.C., Propping P., Wallace R.H., Phillips H.A., Sutherland G.R., Scheffer I.E., Berkovic S.F. A missense mutation in the neuronal nicotinic acetylcholine receptor alpha 4 subunit is associated with autosomal nocturnal frontal lobe epilepsy. Nat. Genet. 11:1995;201-203.
29. Villemagne V.L., Horti A., Scheffel U., Ravert H.T., Finley P., Clough D.J., London E.D., Wagner H.N., Dannals R.F. Imaging nicotinic acetylcholine receptors with fluorine-18-FPH, an epibatidine analog. J. Nucl. Med. 38:1997;1737-1741.
30. 125I]5-I-A-85380, a nicotinic acetylcholine receptor radioligand. Neuroreport. 9:1998;2311-2317.
31. Whitehouse P.J., Martino A.M., Antuono P.G., Lowenstein P.R., Coyle J.T., Price D.L., Kellar K.J. Nicotinic acetylcholine binding sites in Alzheimer's disease. Brain Res. 371:1986;146-151.
32. Yokoi F., Komiyama T., Hayashi T., Lio M., Hara T. Application of carbon-11 labelled nicotine in the measurement of human cerebral blood flow and other physiological parameters. Eur. J. Nucl. Med. 20:1993;46-52.