Comparative studies of epibatidine derivatives [18F]NFEP and [18F]n- methyl-NFEP: Kinetics, nicotine effect, and toxicity

Nuclear Medicine and Biology

Volumn 26, Issue 1, 1999, Pages 139-148

  Ding, Yu Shin ^a   Molina, Patricia E ^b   Fowler, Joanna S ^a   Logan, Jean ^a   Volkow, Nora D ^b   Kuhar, Michael J ^c   Carroll, F Ivy ^d  

^a BROOKHAVEN NATIONAL LABORATORY   (United States)

^b BROOKHAVEN NATIONAL LABORATORY   (United States)

^c EMORY UNIVERSITY   (United States)

^d RTI INTERNATIONAL   (United States)

Author keywords

Epibatidine; Fluorine 18; Nicotine; Nicotinic acetylcholine receptors; PET; Toxicity

Indexed keywords

EPIBATIDINE; N METHYLNORCHLOROFLUOROEPIBATIDINE F 18; NORCHLOROFLUOROEPIBATIDINE F 18; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BABOON; BRAIN; CONTROLLED STUDY; DRUG EFFECT; DRUG RECEPTOR BINDING; FEMALE; INTRAVENOUS DRUG ADMINISTRATION; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; THALAMUS; TOXICITY TESTING;

ANIMALS; BENZAMIDES; BICYCLO COMPOUNDS, HETEROCYCLIC; BRAIN; DOGS; FEMALE; FLUORINE RADIOISOTOPES; NICOTINE; PAPIO; PYRIDINES; RADIOPHARMACEUTICALS; RATS; RECEPTORS, NICOTINIC; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0032892066     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0969-8051(98)00070-5     Document Type: Article

References (38)

1. 3H]ABT-418 A novel cholinergic channel ligand . J. Pharmacol. Exp. Ther. 273:1995;1434-1441.
2. Arneric S.P., Anderson D.J., Campbell J.E., Kuntzweiller T., Wasicak J., Halladay M.W., Pauly J., Williams M., Donnelly-Roberts D. In vitro pharmacology of ABT-594 A novel non-opioid analgesic, neuronal nicotinic acetylcholine receptor (nAChR) ligand . Soc. Neurosci. 23:1997;1199.
3. Arneric S.P., Sullivan J.P., Williams M. Neuronal nicotinic acetylcholine receptors Novel targets for CNS therapeutics . Bloom E.F., Kupfer D.J. Psychopharmacology The Fourth Generation of Progress . 1995;95-110 Raven, New York.
4. Badio B., Daly J.W. Epibatidine, a potent analgetic and nicotinic agonist. Mol. Pharmacol. 45:1994;563-569.
5. Badio B., Shi D., Garraffo H.M., Daly J.W. Antionociceptive effects of the alkaloid epibatidine Further studies on involvement of nicotinic receptors . Drug Develop. Res. 36:1995;46-59.
6. Bannon A.W., Decker M.W., Holladay M.W., Curzon P., Donnelly-Roberts D., Puttfarcken P.S., Bitner R.S., Diaz A., Dickenson A.H., Porsolt R.D., Williams M., Arneric S.P. Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors. Science. 279:1998;77.
7. 3H]1-nicotine in the mouse brain. Life Sci. 44:1989;123-132.
8. Damaj M.I., Creasy K.R., Grove A.D., Rosecrans J.A., Martin B.R. Pharmacological effects of epibatidine optical enantiomers. Brain Res. 664:1994;34-40.
9. Dewey S.L., MacGregor R.R., Brodie J.D., Bendriem B., King P.T., Volkow N.D., Schlyer D.J., Fowler J.S., Wolf A.P., Gatley S.J., Hitzemann R. Mapping muscarinic receptors in human and baboon brain using [N-11C-methyl]benztropine. Synapse. 5:1990;213-223.
10. 11C-raclopride and positron emission tomography. J. Neurosci. 12:1992;3773-3780.
11. 18F]Norchlorofluoroepibatidine with autoradiography and a phosphor-imaging device. XIIth International Symposium on Radiopharmaceutical Chemistry. Uppsala, Sweden, J. Label. Cmpds. Radiopharm. XL, 157.
12. 18F]Norchloro-2-fluoroepibatidine studies of nicotinic acetylcholine receptors (nAChR) in living primate and postmortem human brain. Soc. Neurosci. 23:1997;382.
13. Ding Y.-S., Fowler J. S., Volkow N. D., Liang F., Carroll F. I. and Kuhar M. J. (1997) Comparative studies of F-18 labeled epibatidine derivatives in mapping nicotinic acetylcholine receptors. XIIth International Symposium on Radiopharmaceutical Chemistry. Uppsala, Sweden, J. Label. Cmpds. Radiopharm. XL, 546.
14. Ding Y.-S., Fowler J.S., Volkow N.D., Logan J., Gatley S.J., Sugano Y. Carbon-11-d-threo-methylphenidate binding to dopamine transporter in baboon brain. J. Nucl. Med. 36:1995;2298-2305.
15. 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 [abstract]. Soc. Neurosci. 22:1996;269.
16. 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.
17. 18F]Norchlorofluoroepibatidine and its N-methyl derivative New PET ligands for mapping nicotinic acetylcholine receptors . J. Label. Cmpds. Radiopharm. 34:1997;827-832.
18. Domino E.F. Brain Imaging of Nicotine and Tobacco Smoking. 1995;NPP Books, Ann Arbor, MI.
19. Fisher M., Huangfu D., Shen T.Y., Guyenet P.G. Epibatidine, an alkaloid from the poison frog Epipedobates tricolor, is a powerful ganglionic depolarizing agent. J. Pharm. Exp. Therap. 270:1994;702-707.
20. 18F]fluoro-nor-chloroepibatidine in rodent and human brain. Nucl. Med. Biol. 25:1998;449-454.
21. Halladay M.W., Dart M.J., Lynch J.K. Neuronal nicotinic acetylcholine receptors as targets for drug discovery. J. Med. Chem. 40:1997;4169-4194.
22. 18F]fluoro-5-pyridyl)-7-azabicyclo[2.2.1]heptane . J. Label. Cmpds. Radiopharm. 38:1996;355-365.
23. Jones G.M.M., Sahakian B.J., Levy R., Warburton D.M., Gray J.A. Effects of actue subcutaneous nicotine on attention, information processing and short-term memory in Alzheimer's disease. Psychopharmacology. 108:1992;485-494.
24. 11C-methyl]-(-)-cocaine PET studies in human subjects. J. Cereb. Blood Flow Metab. 10:1990;740-747.
25. Macallan D.R., Lunt G.G., Wannacott S., Swanson K.L., Rapoport H., Albuquerque E.X. Methyllycaconitine and (+)-anatoxin - A differentiate between nicotinic receptors in vertebrate and invertebrate nervous systems. FEBS Lett. 226:1988;357-363.
26. Marks M.J., Grady S.R., Collins A.C. Downregulation of nicotinic receptor function after nicotine infusion. J. Pharmacol. Exp. Ther. 266:1993;1268-1276.
27. Marks M.J., Stitzel J.A., Collins A.C. Time course study of the effects of chronic nicotinic infusion on drug response and brain receptors. J. Pharm. Exp. Ther. 235:1985;619-628.
28. Molina P.E., Ding Y.-S., Carroll F.I., Liang F., Volkow N.D., Pappas N., Kuhar M., Abumrad N., Gatley S.J., Fowler J.S. Fluoro-norchloroepibatidine Preclinical assessment of acute toxicity . Nucl. Med. Biol. 24:1997;743-747.
29. Molina P.E., Williams P., Abumrad N.N. Histaminergic contribution to the metabolic effects of neuroglucopenia. Am. J. Physiol. 272:1997;1918-1924.
30. 11C-nicotine in the brains of rhesus monkey - An attempt to study nicotinic receptors in vivo. J. Neural Transm. 1:1989;195-205.
31. 2 subunit are involved in the reinforcing properties of nicotine. Nature. 391:1998;173-177.
32. 3H](-)-nicotine to rat brain membranes and its inhibition by analogues of nicotine. Neuropharmacology. 27:1988;235-241.
33. Sullivan J.P., Briggs C.A., Donnelly-Roberts D., Brioni J.D., Radek R.G., McKenna D.J., Campbell J.E., Arneric S.P., Decker M.W., Bannon A.W. (±)-Epibatidine can differentially evoke responses mediated by putative subtypes of nicotinic acetylcholine receptors (nAChRs). Med. Chem. Res. 4:1994;502-516.
34. Sullivan J.P., Decker M.W., Brioni J.D., Donnelly-Roberts D., Anderson D.J., Bannon A.W., Kang C.-H., Adams P., Piattoni-Kaplan M., Buckley M.J., Gopalakrishnan M., Williams M., Arneric S.P. (+)-Epibatidine elicits a diversity of in vitro and in vivo effects mediated by nicotinic acetylcholine receptors. J. Pharm. Exp. Therap. 271:1994;624-631.
35. Taylor P. (1996) Agents acting at the neuromuscular junction and autonomic ganglia. In: Goodman & Gilman's: The Pharmacological Basis of Therapeutics (9th ed.) (Edited by Hardman J. G., Limbird L. E., Molinoff P. B., Ruddon R. W. and Gilman A. G.), p. 193. McGraw-Hill, New York.
36. Guide for the Care and Use of Laboratory Animals (NIH Publication No. 86-23). 1986;USDHHS, Washington DC.
37. Preparation and Maintenance of Higher Mammals During Neuroscience Experiments (NIH Publication No. 94-3207). 1994;USDHHS, Washington DC.
38. Vidal C. Nicotinic receptors in the brain. Molecular biology, function, and therapeutics. Mol. Chem. Neuropathol. 28:1996;3-11.