Pharmacological characterization of RJR-2403: A nicotinic agonist with potential therapeutic benefit in the treatment of Alzheimer's disease

CNS Drug Reviews

Volumn 3, Issue 4, 1997, Pages 325-345

  Bencherif, M ^a   Byrd, G ^a   Caldwell, W S ^a   Hayes, J R ^a   Lippiello, P M ^a  

^a Winston Salem NC   (United States)

Author keywords

Alzheimer's disease NS; Choline receptor; Neuronal nicotinic acetyl; Nicotinic agonist; RJR 2403; Selectivity

Indexed keywords

N METHYL 4 (3 PYRIDINYL) 3 BUTENE 1 AMINE FUMARATE; NICOTINIC AGENT; NICOTINIC RECEPTOR; UNCLASSIFIED DRUG;

ALZHEIMER DISEASE; ANIMAL CELL; ANIMAL TISSUE; DRUG EFFECT; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; DRUG USE; GUINEA PIG; NEUROTRANSMISSION; NONHUMAN; REVIEW; XENOPUS;

EID: 0031402826     PISSN: 1080563X     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1527-3458.1997.tb00331.x     Document Type: Review

References (60)

1. Acheson RM, Ferris MJ, Sinclair NM. Transformations involving the pyrrolidine ring of nicotine. J Chem Soc 1980;2:579-585.
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.
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.
4. Arneric SP, Sullivan JP, Williams M. Neuronal nicotinic acetylcholine receptors - Novel targets for CNS therapeutics. In: Bloom FE, Kupfer DJ, eds. Psychopharmacology: The Fourth Generation of Progress. New York: Raven Press, 1995:1-16.
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.
6. Baron JA. The epidemiology of cigarette smoking and Parkinson's disease. In: Clarke PBS, Quik M, Adlkofer F, Thurau K, eds. Adv Pharmacol Sci. Basel: Birkhäuser Verlag, 1994:313-319.
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.
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.
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.
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.
11. 3H]nicotine binding sites in human brain. J Neurochem 1988;50:1243-1247.
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 Natl Acad Sci USA 1987;84:7763-7767.
13. Calderon-Gonzalez R. Attention deficit disorders spectrum: Neurological and neuropsychological basis. Int. Pediat 1993;8:176-188.
14. Calkins BM. A meta-analysis of the role of smoking in inflammatory bowel disease. Dig Dis Sci 1989;34:1841-1854.
15. 3H]dopamine release. Br J Pharmacol 1996;117:595-306.
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.
17. Davies P, Maloney AJF. Selective loss of central cholinergic neurons in Alzheimer's disease. Lancet 1976;2:1403.
18. Decker MW, Brioni JD, Sullivan JP, et al. (S)-3-Methyl-5-(1-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.
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.
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.
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.
22. Freedman R, Leonard S, Adler P. Nicotine receptors and the pathophysiology of schizophrenia. In: Clarke PBS, Quik M, Adlkofer F, Thurau K, eds. Adv Pharmacol Sci Basel: Birkhäuser Verlag, 1994:307-312.
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.
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.
25. Hansch C, Steward AR, Anderson SM, Bentley D. The parabolic dependence of drug action upon lipophilic character as revealed by a study of hypnotics. J Med Chem 1968;11:1-11.
26. Hopfinger A J. Conformational Properties of Macromolecules, New York: Academic Press, 1973.
27. Hughes JR, McHugh P. Nicotine and neuropsychiatric disorders: Schizophrenia. In: Clarke PBS, Quik M, Adlkofer F, Thurau K, eds. Adv Pharmacol Sci. Basel: Birkhäuser Verlag, 1994;301-305.
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.
29. Joseph MH, Grigoryan G, Hodges H, Gray JA. Possible mechanisms underlying beneficial effects of nicotine on cognitive function, In: Clarke PBS, Quik M, Adlkofer F, Thurau K, eds. Adv Pharmacol Sci Basel: Birkhäuser Verlag, 1994:337-344.
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.
31. Levin ED, Torry D. Nicotine effects on memory performance. In: Clarke PBS, Quik M, Adlkofer F, Thurau K, eds. Adv Pharmacol Sci Basel: Birkhäuser Verlag, 1994;329-335.
32. Lippiello PM, Caldwell WS, Marks MJ, Collins AC. Development of nicotinic agonists for Alzheimer disease treatment. In: Giacobini E, Becker R, eds. Alzheimer's Disease, Therapeutic Strategies. Boston: Birkhäuser, 1994:186-190.
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.
34. Lukas RJ, Bencherif M. Heterogeneity and regulation of nicotinic acetylcholine receptors. Int Rev Neurobiol 1992;34:25-130.
35. Luetje CW, Patrick J. Both α- and β-subunits contribute to the agonist sensitivity of neuronal nicotinic acetylcholine receptors. J Neurosci 1991;55:837-845.
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.
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.
38. McGehee DS, Heath MJS, Gelber S, Devay P, Role LW. Nicotine enhancement of fast excitatory synaptic transmission in CNS by presynaptic receptors. Science 1995;269:1692-1696.
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.
40. Newhouse PA, Sunderland T, Tariot PN, et al. Intravenous nicotine in Alzheimer's disease. A pilot study. Psychopharmacology 1988;95:171-175.
41. Newhouse PA, Potter A, Pisasecki M. Nicotinic modulation of cognitive functioning in humans. In: Clarke PBS, Quik M, Adlkofer F, Thurau K, eds. Adv Pharmacol Sci Basel: Birkhäuser Verlag, 1994;345-351.
42. 3H]acetylcholine binding sites in the frontal cortex of Alzheimer brains. Neurosci Lett 1986;72:275-285.
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.
44. Pullan RD, Rhodes J, Ganesh S et al. Transdermal nicotine for ulcerative colitis. N Engl J Med 1994;30:811-815.
45. Rapier C, Lunt GG, Wonnacott S. Stereoselective nicotine-induced release of dopamine from striatal synaptosomes: concentration dependence and repetitive stimulation. J Neurochem 1988;50:1123-1130.
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.
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.
48. Sargent PB. The diversity of neuronal nicotinic acetylcholine receptors. Ann Rev Neurosci 1993;16:403-443.
49. Schwartz RD, Kellar KJ. Nicotinic cholinergic receptor binding sites in brain: In vivo regulation. Science 1983;220:214-216.
50. Shivananda S, Mayberry JF. Epidemiology of inflammatory bowel disease. Curr Opin Gastroenterol 1993;9:550-565.
51. Silver AA, Shytle RD, Philipp MK, Sanberg PR. Transdermal nicotine in Tourette's syndrome. In: Clarke PBS, Quik M, Adlkofer F, Thurau K, eds. Adv Pharmacol Sci Basel: Birkhäuser Verlag, 1994;293-299.
52. 3H]GABA uptake in nucleus basalis lesioned rats. Brain Res 1993;624:295-298.
53. Smith CJ, Giacobini E. Nicotine, Parkinson's and Alzheimer's disease. Rev Neurosci 1992;3:25-43.
54. Summers KL, Lippiello P, Verhulst S, Giacobini E. 5-Fluoronicotine, noranhydroecgonine, and pyridylmethylpyrrolidine release acetylcholine and biogenic amines in rat cortex in vivo. Neurochem Res 1995;20:1089-1094.
55. Thomas GAO, Rhodes J. Relationship between smoking, nicotine and ulcerative colitis. In: Clarke PBS, Quik M, Adlkofer F, Thurau K, eds. Adv Pharmacol Sci Basel: Birkhäuser Verlag, 1994;287-305.
56. van Duijn CM, Hofman A. Relation between nicotine intake and Alzheimer's disease. Br Med J 1991;302:1491-1494.
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.
58. Williams M, Sullivan JP, Arneric SP. Neuronal nicotinic acetylcholine receptors. Drug News Perspect 1994;7:205-223.
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.
60. Wonnacott S, Drasdo A, Sanderson E, Rowell P. Presynaptic nicotinic receptors and the modulation of transmitter release. In: Bock G, Marsh J, eds. The Biology of Nicotine Dependence. Chichester: John Wiley, 1990:87-101.