Portal de Periódicos da CAPES

Pharmacological Characterization of RJR‐2403: A Nicotinic Agonist with Potential Therapeutic Benefit in the Treatment of Alzheimer's Disease

1997; Wiley; Volume: 3; Issue: 4 Linguagem: Inglês

10.1111/j.1527-3458.1997.tb00331.x

1527-3458

Merouane Bencherif, Gary D. Byrd, William S. Caldwell, Jane Hayes, P M Lippiello,

Medicinal Plants and Neuroprotection

CNS Drug ReviewsVolume 3, Issue 4 p. 325-345 Free Access Pharmacological Characterization of RJR-2403: A Nicotinic Agonist with Potential Therapeutic Benefit in the Treatment of Alzheimer's Disease M. Bencherif, Corresponding Author M. Bencherif R. J. Reynolds Research & Development, Winston-Salem, USA.Address correspondence and reprint-requests to Dr. M. Bencherif, R. J. Reynolds, Research & Development, Winston-Salem, NC 27102 USA.Search for more papers by this authorG. Byrd, G. Byrd R. J. Reynolds Research & Development, Winston-Salem, USA.Search for more papers by this authorW. S. Caldwell, W. S. Caldwell R. J. Reynolds Research & Development, Winston-Salem, USA.Search for more papers by this authorJ. R. Hayes, J. R. Hayes R. J. Reynolds Research & Development, Winston-Salem, USA.Search for more papers by this authorP. M. Lippiello, P. M. Lippiello R. J. Reynolds Research & Development, Winston-Salem, USA.Search for more papers by this author M. Bencherif, Corresponding Author M. Bencherif R. J. Reynolds Research & Development, Winston-Salem, USA.Address correspondence and reprint-requests to Dr. M. Bencherif, R. J. Reynolds, Research & Development, Winston-Salem, NC 27102 USA.Search for more papers by this authorG. Byrd, G. Byrd R. J. Reynolds Research & Development, Winston-Salem, USA.Search for more papers by this authorW. S. Caldwell, W. S. Caldwell R. J. Reynolds Research & Development, Winston-Salem, USA.Search for more papers by this authorJ. R. Hayes, J. R. Hayes R. J. Reynolds Research & Development, Winston-Salem, USA.Search for more papers by this authorP. M. Lippiello, P. M. Lippiello R. J. Reynolds Research & Development, Winston-Salem, USA.Search for more papers by this author First published: 29 September 2006 https://doi.org/10.1111/j.1527-3458.1997.tb00331.xCitations: 7AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onEmailFacebookTwitterLinkedInRedditWechat References 1 Acheson RM, Ferris MJ, Sinclair NM. Transformations involving the pyrrolidine ring of nicotine. J Chem Soc 1980; 2: 579–585. Google Scholar 2 Akaike A, Tamura U, Yokota T, Shimohama S, Kimura J. Nicotine-induced protection of cultured cortical neurons against N-methyl-D-aspartate receptor-mediated glutamate cytotoxicity. Brain Res 1994; 644: 181–187. 10.1016/0006-8993(94)91678-0 CASPubMedWeb of Science®Google Scholar 3 Arneric SP, Sullivan JP, Briggs CA, et al. (S)-3-Methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT-418): A novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization. J Pharmacol Exp Ther 1994; 270: 310–318. CASPubMedWeb of Science®Google Scholar 4 Arneric SP, Sullivan JP, Williams M. Neuronal nicotinic acetylcholine receptors — Novel targets for CNS therapeutics. In: FE Bloom, DJ Kupfer, eds. Psychopharmacology: The Fourth Generation of Progress. New York : Raven Press, 1995; 1–16. Google Scholar 5 Arneric SP, Holladay MW, Sullivan JP. Cholinergic channel modulators as a novel therapeutic strategy for Alzheimer's disease. Exp Opin Invest Drugs 1996; 5: 79–100. 10.1517/13543784.5.1.79 CASGoogle Scholar 6 Baron JA. The epidemiology of cigarette smoking and Parkinson's disease. In: PBS Clarke, M Quik, F Adlkofer, K Thurau, eds. Adv Pharmacol Sci. Basel : Birkhauser Verlag, 1994; 313–319. Google Scholar 7 Bencherif M, Lukas RJ. Ligand binding and functional characterization of muscarinic acetylcholine receptors on the TE671/RD cells. J Pharmacol Exp Ther 1991; 257: 946–953. CASPubMedWeb of Science®Google Scholar 8 Bencherif M, Lovette ME, Arrington S, et al. RJR-2403: A nicotinic agonist with CNS selectivity —in vitro characterization. Abstr Soc Neurosci 1995; 21: 605. Google Scholar 9 Bencherif M, Fowler K, Lukas RJ, Lippiello PM. Mechanisms of up-regulation of neuronal nicotinic acetylcholine receptors in clonal cell lines and primary cultures of fetal rat brain. J Pharmacol Exp Ther 1995; 275: 987–994. CASPubMedWeb of Science®Google Scholar 10 Bencherif M, Lovette ME, Fowler KW et al. RJR-2403: A nicotinic agonist with CNS selectivity. I. In vitro characterization. J Pharmacol Exp Ther 1996; 279: 1413–1421. CASPubMedWeb of Science®Google Scholar 11 Benwell MEM, Balfour DJK. Anderson JM. Evidence that tobacco smoking increases the density of (−)-[3H]nicotine binding sites in human brain. J Neurochem 1988; 50: 1243–1247. 10.1111/j.1471-4159.1988.tb10600.x CASPubMedWeb of Science®Google Scholar 12 Boulter J, Connolly J, Deneris ES, Goldman D, Heinemann S, Patrick J. Functional expression of two neuronal nicotinic acetylcholine receptors from cDNA clones identifies a gene family. Proc Nail Acad Sci USA 1987; 84: 7763–7767. 10.1073/pnas.84.21.7763 CASPubMedGoogle Scholar 13 Calderon-Gonzalez R. Attention deficit disorders spectrum: Neurological and neuropsychological basis. Int. Pediat 1993; 8: 176–188. Google Scholar 14 Calkins BM. A meta-analysis of the role of smoking in inflammatory bowel disease. Dig Dis Sci 1989; 34: 1841–1854. 10.1007/BF01536701 CASPubMedWeb of Science®Google Scholar 15 Clarke PBS, Reuben M. Release of [3H]noradrenaline from rat hippocampal synaptosomes by nicotine: Mediation by different nicotinic receptor subtypes from striatal [3H]dopamine release. Br J Pharmacol 1996; 117: 595–606. 10.1111/j.1476-5381.1996.tb15232.x CASPubMedWeb of Science®Google Scholar 16 Couturier S, Bertrand D, Matter J-M, et al. A neuronal nicotinic acetylcholine receptor subunit (α7) is developmentally regulated and forms a homo-oligomeric channel blocked by α-BTX. Neuron 1990; 5: 847–856. 10.1016/0896-6273(90)90344-F CASPubMedWeb of Science®Google Scholar 17 Davies P, Maloney AJF. Selective loss of central cholinergic neurons in Alzheimer's disease. Lancet 1976; 2: 1403. 10.1016/S0140-6736(76)91936-X CASPubMedWeb of Science®Google Scholar 18 Decker MW, Brioni JD, Sullivan JP, et al. (S)-3-Methyl-5-(l-methyl-2-pyrrolidinyl)isoxazole (ABT-418): A novel cholinergic ligand with cognition-enhancing and anxiolytic activities: II. In vivo characterization. J Pharmacol Exp Ther 1994; 270: 319–328. CASPubMedWeb of Science®Google Scholar 19 Deneris ES, Connolly JG, Boulter J, et al. Primary structure and expression of beta 2: A novel subunit of neuronal nicotinic acetylcholine receptors. Neuron 1988; 1: 45–54. 10.1016/0896-6273(88)90208-5 CASPubMedGoogle Scholar 20 Deneris ES, Connolly JG, Rogers SW, Duvoisin R. Pharmacological and functional diversity of neuronal nicotinic acetylcholine receptors. Trends Pharmacol Sci 1991; 12: 34–40. 10.1016/0165-6147(91)90486-C CASPubMedWeb of Science®Google Scholar 21 Elogoyhen AB, Johnson D, Boulter J, Vetter D, Heinemann SF. Alpha-9: An acetylcholine receptor with novel pharmacological properties expressed in rat cochlear hair cells. Cell 1994; 79: 705–715. 10.1016/0092-8674(94)90555-X CASPubMedWeb of Science®Google Scholar 22 Freedman R, Leonard S, Adler P. Nicotine receptors and the pathophysiology of schizophrenia. In: PBS Clarke, M Quik, F Adlkofer, K Thurau, eds. Adv Pharmacol Sci Basel : Birkhauser Verlag, 1994; 307–312. Google Scholar 23 Goldman D, Deneris E, Luyten W, Kochhar A, Patrick J, Heinemann S. Members of a nicotinic acetylcholine receptor gene family are expressed in different regions of the mammalian central nervous system. Cell 1987; 48: 965–973. 10.1016/0092-8674(87)90705-7 CASPubMedWeb of Science®Google Scholar 24 Graves AB, van Duijn CM, Chandra V, et al. Alcohol and tobacco consumption as risk factors for Alzheimer's disease: A collaborative re-analysis of case-control studies. Int J Epidemiol 1991; 20: S48–S57. 10.1093/ije/20.Supplement_2.S48 PubMedWeb of Science®Google Scholar 25 Hansch C, Steward AR, Anderson SM, Bentley D. The parabolic dependence of drug action upon lipo-philic character as revealed by a study of hypnotics. J Med Chem 1968; 11: 1–11. 10.1021/jm00307a001 CASPubMedWeb of Science®Google Scholar 26 Hopfinger AJ. Conformational Properties of Macromolecules. New York : Academic Press, 1973. Google Scholar 27 Hughes JR, McHugh P. Nicotine and neuropsychiatric disorders: Schizophrenia. In: PBS Clarke, M Quik, F Adlkofer, K Thurau, eds. Adv Pharmacol Sci. Basel : Birkhäuser Verlag, 1994; 301–305. Google Scholar 28 Jones GM, Sahakian BJ, Levy R. Warburton DM, Gray JA. Effects of acute subcutaneous nicotine on attention, information processing, and short-term memory in Alzheimer's disease. Psychopharmacology 1992; 108: 485–494. 10.1007/BF02247426 CASPubMedWeb of Science®Google Scholar 29 Joseph MH, Grigoryan G, Hodges H, Gray JA. Possible mechanisms underlying beneficial effects of nicotine on cognitive function, In: PBS Clarke, M Quik, F Adlkofer, K Thurau, eds. Adv Pharmacol Sci Basel : Birkhäuser Verlag, 1994; 337–344. Google Scholar 30 Kellar KJ, Whitehouse PJ, Martino-Barrows AM, Marcus K, Price DL. Muscarinic and nicotinic binding sites in Alzheimer's disease cerebral cortex. Brain Res 1987; 436: 62–68. 10.1016/0006-8993(87)91556-3 CASPubMedWeb of Science®Google Scholar 31 Levin ED, Lorry D. Nicotine effects on memory performance. In: PBS Clarke, M Quik, F Adlkofer, K Thurau, eds. Adv Pharmacol Sci Basel : Birkhauser Verlag, 1994; 329–335. Google Scholar 32 Lippiello PM, Caidwell WS, Marks MJ, Collins AC. Development of nicotinic agonists for Alzheimer disease treatment. In: E Giacobini, R Becker, eds. Alzheimer's Disease, Therapeutic Strategies. Boston : Birkhauser, 1994; 186–190. Google Scholar 33 Lippiello PM, Bencherif M, Gray JA, et al. RJR-2403: A nicotinic agonist with CNS selectivity. I. In vivo characterization. J Pharmacol Exp Ther 1996; 279: 1422–1429. CASPubMedWeb of Science®Google Scholar 34 Lukas RJ, Bencherif M. Heterogeneity and regulation of nicotinic acetylcholine receptors. Int Rev Neurobioi 1992; 34: 25–130. 10.1016/S0074-7742(08)60097-5 CASPubMedWeb of Science®Google Scholar 35 Luetje CW, Patrick J. Both a- and p-subunits contribute to the agonist sensitivity of neuronal nicotinic acetylcholine receptors. J Neurosci 1991; 55: 837–845. Google Scholar 36 Marks MJ, Romm E, Bealer S, Collins AC. A test battery for measuring nicotine effects in mice. Pharmacol Biochem Behav 1985; 23: 325–330. 10.1016/0091-3057(85)90577-5 CASPubMedWeb of Science®Google Scholar 37 McConville BJ, Sanberg PR, Fogelson HM, King J, Cirino P. The effects of nicotine plus haloperidol compared to nicotine only and placebo nicotine only in reducing tic severity and frequency in Tourette's disorder. Biol Psychiatry 1992; 31: 832–840. 10.1016/0006-3223(92)90315-Q CASPubMedWeb of Science®Google Scholar 38 McGehee DS, Heath MJS, Gelber S, Devay P, Role LW. Nicotine enhancement of fast excitatory synap-tic transmission in CNS by presynaptic receptors. Science 1995; 269: 1692–1696. 10.1126/science.7569895 CASPubMedWeb of Science®Google Scholar 39 Nef P, Oneyser C, Alliod C, Couturier S, Ballivet M. Genes expressed in the brain define three distinct neuronal nicotinic acetylcholine receptors. Embo J 1988; 7: 595–601. 10.1002/j.1460-2075.1988.tb02852.x CASPubMedWeb of Science®Google Scholar 40 Newhouse PA, Sunderland T, Tariot PN, et al. Intravenous nicotine in Alzheimer's disease. A pilot study. Psychopharmacology 1988; 95: 171–175. 10.1007/BF00174504 CASPubMedWeb of Science®Google Scholar 41 Newhouse PA, Potter A, Pisasecki M. Nicotinic modulation of cognitive functioning in humans. In: PBS Clarke, M Quik, F Adlkofer, K Thurau, eds. Adv Pharmacol Sci Basel : Birkhauser Verlag, 1994; 345–351. Google Scholar 42 Nordberg A, Winblad B. Reduced number of [3H]nicotine and [3H]acetylcholine binding sites in the frontal cortex of Alzheimer brains. Neurosci Lett 1986; 72: 275–285. 10.1016/0304-3940(86)90629-4 CASWeb of Science®Google Scholar 43 Peng X, Gerzanich V, Anand R, Whiting PJ, Lindstrom J. Nicotine-induced increase in neuronal nicotinic receptors results from a decrease in the rate of receptor turnover. Mol Pharmacol 1994; 46: 523–530. CASPubMedWeb of Science®Google Scholar 44 Pullan RD, Rhodes J, Ganesh S et al. Transdermal nicotine for ulcerative colitis. N Engl J Med 1994; 30: 811–815. 10.1056/NEJM199403243301202 Web of Science®Google Scholar 45 Rapier C, Lunt GO, Wonnacott S. Stereoselective nicotine-induced release of dopamine from striatal sy-naptosomes: concentration dependence and repetitive stimulation. J Neurochem 1988; 50: 1123–1130. 10.1111/j.1471-4159.1988.tb10582.x CASPubMedWeb of Science®Google Scholar 46 Sahakian B, Jones G, Levy R, Gray J, Warburton D. The effects of nicotine on attention, information processing, and short-term memory in patients with dementia of the Alzheimer type. Br J Psychiatry 1989; 154: 797–800. 10.1192/bjp.154.6.797 CASPubMedWeb of Science®Google Scholar 47 Sanberg PR, McConville BJ, Fogelson HM, et al. Nicotine potentiates the effects of haloperidol in animals and in patients with Tourette's syndrome. Biomed Pharmacother 1989; 43: 19–23. 10.1016/0753-3322(89)90186-8 CASPubMedWeb of Science®Google Scholar 48 Sargent PB. The diversity of neuronal nicotinic acetylcholine receptors. Ann Rev Neurosci 1993; 16: 403–443. 10.1146/annurev.ne.16.030193.002155 CASPubMedWeb of Science®Google Scholar 49 Schwartz RD, Kellar KJ. Nicotinic cholinergic receptor binding sites in brain: In vivo regulation. Science 1983; 220: 214–216. 10.1126/science.6828889 CASPubMedWeb of Science®Google Scholar 50 Shivananda S, Mayberry JF. Epidemiology of inflammatory bowel disease. Curr Opin Gastroenternl 1993; 9: 550–565. 10.1097/00001574-199307000-00006 Web of Science®Google Scholar 51 Silver AA, Shytlc RD, Philipp MK, Sanberg PR. Transdermal nicotine in Tourette's syndrome. In: PBS Clarke, M Quik, F Adlkofer, K Thurau, eds. Adv Pharmacol Sci Basel : Birkhauser Verlag, 1994; 293–299. Google Scholar 52 Sjak-Shie NN, Meyer EM. Effects of chronic nicotine and pilocarpine administration on neocortical neuronal density and [3H]GABA uptake in nucleus basalis lesioned rats. Brain Res 1993; 624: 295–298. 10.1016/0006-8993(93)90091-Z CASPubMedWeb of Science®Google Scholar 53 Smith CJ, Giacobini E. Nicotine, Parkinson's and Alzheimer's disease. Rev Neurosci 1992; 3: 25–43. 10.1515/REVNEURO.1992.3.1.25 CASPubMedWeb of Science®Google Scholar 54 Summers KL, Lippiello P, Verhulst S, Giacobini E. 5-Fluoronicotine, noranhydroecgonine, and pyridyl-methylpyrrolidine release acetylcholine and biogenic amines in rat cortex in vivo. Neurochem Res 1995; 20: 1089–1094. 10.1007/BF00995564 CASPubMedWeb of Science®Google Scholar 55 Thomas GAO, Rhodes J. Relationship between smoking, nicotine and ulcerative colitis. In: PBS Clarke, M Quik, F Adlkofer, K Thurau, eds. Adv Pharmacol Sci Basel : Birkhauser Verlag, 1994; 287–305. Google Scholar 56 van Duijn CM, Hofman A. Relation between nicotine intake and Alzheimer's disease. Br Med J 1991; 302: 1491–1494. 10.1136/bmj.302.6791.1491 CASPubMedWeb of Science®Google Scholar 57 Whitehouse PJ, Price DL, Struble G, Clark AW, Coyle JT, DeLong MR. Alzheimer's disease and senile dementia: Loss of neurons in the basal forebrain. Science 1982; 215: 1237–1239. 10.1126/science.7058341 CASPubMedWeb of Science®Google Scholar 58 Williams M, Sullivan JP, Arneric SP. Neuronal nicotinic acetylcholine receptors. Drug News Perspecl 1994; 7: 205–223. Google Scholar 59 Wilson AL, Langley LK, Monley J, et al. Nicotine patches in Alzheimer's disease: Pilot study on learning, memory, and safety. Pharmacol Biochem Behav 1995; 51: 509–514. 10.1016/0091-3057(95)00043-V CASPubMedWeb of Science®Google Scholar 60 Wonnacott S, Drasdo A, Sanderson E, Rowell P. Presynaptic nicotinic receptors and the modulation of transmitter release. In: G Bock, J Marsh, eds. The Biology of Nicotine Dependence. Chichester : John Wiley, 1990; 87–101. 10.1002/9780470513965.ch6 Google Scholar Citing Literature Volume3, Issue4December 1997Pages 325-345 ReferencesRelatedInformation