Linoperdine: Pharmacology of a neurotransmitter release enhancer

CNS Drug Reviews

Volumn 3, Issue 2, 1997, Pages 103-119

  Zaczek, Robert ^a   Chorvat, Robert J ^a   Brown, Barry S ^a  

^a DUPONT COMPANY   (United States)

Author keywords

Alzheimer's disease; DuP 996; Linopirdine; Neurotransmitter release; Potassium channels

Indexed keywords

LINOPIRDINE;

ACETYLCHOLINE BRAIN LEVEL; ALZHEIMER DISEASE; CHOLINERGIC NERVE; DOPAMINE BRAIN LEVEL; HUMAN; HUMAN TISSUE; NEUROTRANSMITTER RELEASE; REVIEW; SEROTONIN BRAIN LEVEL;

EID: 0030691841     PISSN: 1080563X     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1527-3458.1997.tb00319.x     Document Type: Review

References (62)

1. Aiken SP, Lampe BJ, Murphy PA, Brown BS. Reduction of spike frequency adaptation and blockade of M-current in rat CA1 pyramidal neurons by linopirdine (DuP 996), a neurotransmitter release enhancer. Br J Pharmacol 1995;115:1163-1168.
2. Aiken SP, Zaczek R, Brown BS. Pharmacology of the neurotransmitter release enhancer linopirdine (DuP 996), and insights into its mechanism of action. Adv Pharmacol 1996;35:349-384.
3. Bartus RT, Dean RL, Beer B, Lippa AS. The cholinergic hypothesis of geriatric memory dysfunction. Science 1982;217:408-417.
4. Baumgarten M, Becker R, Gauthier, S. The validity and reliability of the dementia behavior disturbance scale. J Am Geriatr Soc 1990;38:221-226.
5. Baxter MG, Rohrbach KW, Tam SW, et al. Effects of linopirdine (DuP 996) and X9121 on age-related memory impairments and on the cholinergic system. Drug Devel Res 1993;31:186-196.
6. Benedek IH, Davidson AF, Fiske WD, Stull SG, Kornhauser DM. Pharmacokinetics of linopirdine in patients with chronic liver disease. J Clin Pharmacol 1994;34:1017.
7. Bondi MW, Salmon DP, Butters NM. Neuropsychological features of memory disorders. In: Terry RD, Katzman R, Bick KL, eds. Alzheimer Disease. New York: Raven Press, 1994:41-64.
8. Brioni JD, Curzon P, Buckley MJ, Arneric SP, Decker MW. Linopirdine (DuP 996) facilitates the retention of avoidance training and improves performance of septal-lesioned rats in the water maze. Pharmacol Biochem Behav 1993;44:37-43.
9. Buxton A, Callan OA, Blatt EJ, Wong EHF, Fontana DJ. Cholinergic agents and delay-dependent performance in the rat. Pharmacol Biochem Behav 1994;49:1067-1073.
10. Chorvat RJ, Earl RA, Zaczek R. Acetylcholine release enhancing agents: Potential therapeutics for Alzheimer's disease. Drugs Future 1995;20:1145-1162.
11. Cochran FR, Vitek MP. Neuroinflammatory mechanisms in Alzheimer's disease: Opportunities for drug discoveries. Exp Opin Invest Drugs 1996;5:449-455.
12. Cook L, Steinfels GF, Rohrbach RW, DeNoble VJ. Cognition enhancement by the acetylcholine releaser DuP 996. Drug Devel Res 1990;19:301-314.
13. D'Amato RJ, Zweig RM, Whitehouse PJ, et al. Aminergic systems in Alzheimer's disease and Parkinson's disease. Ann Neurol 1987;22:229-236.
14. 3H]Linopirdine (DuP 996) labels a novel binding site in rat brain involved in the enhancement of stimulus-induced neurotransmitter release: Autoradiographic localization studies. Brain Res 1992;582:335-341.
15. DeNoble VJ, DeNoble KF, Spencer KR, et al. Comparison of DuP 996, with physostigmine, THA, and 3,4-DAP on hypoxia-induced amnesia in rats. Pharmacol Biochem Behav 1990;36:957-961.
16. Dent G, Tam SW, Grzanna, R. The memory enhancer linopirdine increases c-fos expression in cerebral cortex of aged rats. Soc Neurosci Abstr 1993;23:423.6.
17. Farlow M, Gracon SI, Hershey LA, et al. A controlled trial of tacrine in Alzheimer's disease. JAMA 1992;268:2523-2529.
18. Fiske W, Saxton T, Martz R, Nibbelink D. Pharmacokinetics of DuP 996, a (potential) cognitive enhancer, in young and elderly healthy volunteers after multiple oral doses. Pharmaceut Res 1989;6: S-34.
19. Flagmeyer I, van der Staay FJ. Linopirdine (DuP 996;AVIVA): Its effects in the Morris water escape task and on retention of an incompletely acquired bar-press response in rodents. Pharmacol Biochem Behav 1995;51:111-117.
20. Francis PT, Cross AJ, Bowen DM. Neurotransmitters and neuropeptides: In: Terry RD, Katzman R, Bick KL, eds. Alzheimer Disease. New York: Raven Press, 1994:247-262.
21. Garner DM, Pieniaszek HJ, Connell JM, Fiske WD. Determination of linopirdine and its mono-N-oxide metabolite in human plasma and urine by high-performance liquid chromatography. J Liquid Chromatogr 1994;35:22-30.
22. Goedert M. Tau protein and the neurofibrillary pathology of Alzheimer's disease. Trends Neurosci 1993;16:460-465.
23. Gouliaev AH, Senning A. Piracetam and other structurally related nootropics. Brain Res 1994;19:180-222.
24. 3H]linopirdine (DuP 996) binding to brain membranes. Eur J Pharmacol 1996;289:307-312.
25. Holman BL, Johnson KA, Gerada B, et al. The scintographic appearance of Alzheimer's disease: A prospective study using technetium-99m-HMPAO SPECT. J Nucl Med 1992;33:181-185.
26. Hussain MA, Rakestraw D, Rowe S, Aungst BJ. Nasal administration of a cognition enhancer provides improved bioavailability but not enhanced brain delivery. J Pharmaceut Sci 1990;79:771-772.
27. Jaen JC, Moos WH, Johnson, G. Cholinomimetics and Alzheimer's disease. Bioorg Med Chem Lett 1992;2:777-780.
28. 123I single photon emission computed tomography is accurate in the diagnosis of Alzheimer's disease. Arch Intern Med 1990;150:752-756.
29. K(M) in rat sympathetic neurones by linopirdine (DuP 996). Br J Pharmacol 1995;116:123P.
30. Lampe BJ, Gaskill JL, Keim SC, Brown BS. Linopirdine reduces stimulus intensity threshold for induction of long-term potentiation in the Schaffer collateral/CA1 pathway in rat hippocampal slices. Neurosci Lett 1997;222:135-137.
31. + ion permeabilities in the acetylcholine release enhancing effects of linopirdine (DuP 996) in rat cerebral cortical slices. J Pharmacol Exp Ther 1994;271:891-897.
32. Marynowski M, Maciag C, Rominger CM, Tam SW, Zaczek R. Effects of linopirdine (DuP 996) on hippocampal extracellular levels of acetylcholine in freely moving animals. Soc Neurosci Abstr 1993;23:423.8.
33. McGeer PL, McGeer EG. Immune mechanisms in neurodegenerative disorders. Drugs Today 1996;32:149-158.
34. Nickolson VJ, Tam SW, Meyers MJ, Cook L. DuP 996 (3,3[4-pyridinylmethyl]-1-phenylindolin-2-one) enhances the stimulus evoked release of acetylcholine from rat brain in vitro and in vivo. Drug Dev Res 1990;19:285-300.
35. Nordholm AF, Moore E, Wenger GR. Linopirdine does not improve matching performance in the titrating matching to sample paradigm. Pharmacol Biochem Behav 1995;52:205-210.
36. 1 muscarinic receptors to G-proteins in Alzheimer's disease. Alz Dis Assoc Discord 1991;5:163-172.
37. Pieniaszek HJ, Jr, Fiske WD, Saxton TD, et al. Single dose pharmacokinetic, safety, and tolerance of linopirdine (DuP 996) in healthy young adults and elderly volunteers. J Clin Pharmacol 1995;35:22-30.
38. Provan SD, Miyamoto MD. Effect of the putative cognitive enhancer, linopirdine (DuP 996), on quantal parameters of acetylcholine release at the frog neuromuscular junction. Br J Pharmacol 1994;111:1103-1110.
39. Rakestraw DC, De Souza EB, Bilski DA, Brown FP. The penetration of DuP 996 across the blood brain barrier. Pharmaceut Res 1991;8:S-283.
40. Rakestraw DC, Bilski DA, Lam GN. Determination of linopirdine and its N-oxide metabolites in rat plasma by liquid chromatography. J Pharmaceut Biomed Anal 1994;12:1055-1061.
41. Rogers J, Cooper NR, Webster S, et al. Complement activation by β-amyloid in Alzheimer disease. Proc Natl Acad Sci USA 1992;89:10016-10020.
42. Rosen WG, Mohs RC, Davis KL. A new rating scale for Alzheimer's disease. Am J Psychiatry 1984;141:1356-1364.
43. Saletu B, Darragh A, Breuel HP, et al. EEG mapping central effects of multiple doses of linopirdine - a cognitive enhancer - in healthy elderly male subjects. Human Psychopharmacol 1991;6:267-275.
44. Saletu B, Darragh A, Salmon P, Coen R. EEG brain mapping in evaluating the time: course of the central action of DuP 996 - a new acetylcholine releasing drug. Br J Clin Pharmacol 1989;28:1-16.
45. Saydoff JA, Zaczek R. Linopirdine enhances KCl-evoked release, but not basal release, of endogenous dopamine in superfused rat striatum. FASEB Abstr 1993:1521.
46. 2+ stores on KCl-evoked acetylcholine release and linopirdine (DuP 996) release enhancement in rat hippocampal slices. Soc Neurosci Abstr 1993;23:423.9.
47. Schnee ME, Brown BS. Linopirdine, a neurotransmitter release enhancer, blocks voltage-activated potassium currents in hippocampal neurons. Soc Neurosci Abstr 1995;21:1832.
48. Selkoe DJ. The molecular pathology of Alzheimer's disease. Neuron 1991;6:487-489.
49. Smith CP, Broughm LR, Vargus HM. Linopirdine (DuP 996) selectively enhances acetylcholine release induced by high potassium but not electrical stimulation in rat brain slices and guinea pig ileum. Drug Devel Res 1993;29:262-270.
50. Smith TM, Ramirez AD, Heck SD, et al. In vivo microdialysis and pharmacokinetic studies with DuP 996. Soc Neurosci Abstr 1993;19:423.11.
51. Storm JF. Potassium currents in hippocampal pyramidal cells. In: Storm-Mathisen J, Zimmer J, Ottersen OP, eds. Progress in Brain Research. Elsevier: Amsterdam, 1990;83:161-187.
52. Struble RG, Powers RE, Casanova MF, Kitt CA, Brown EC, Price DL. Neuropeptidergic systems in plaques of Alzheimer's Disease. J Neuropathol Exp Neurol 1987;46:567-584.
53. Tam SW, Rominger D, Nickolson VJ. Novel receptor site involved in enhancement of stimulus-induced acetylcholine, dopamine, and serotonin release. Mol Pharmacol 1991;40:16-21.
54. 3H]acetylcholine from superfused hippocampal slices. Soc Neurosci Abstr 1992;22:518.12.
55. Tsai M-C, Su J-L, Chen M-L, Fan S-Z, Cheng C-Y. The effect of 3,3-dipyridylmethyl-1-phenyl-2-indolinone on the neuromuscular transmission in the rodent skeletal muscles. Neuropharmacology 1992;31:89-94.
56. Tsai M-C, Su J-L, Chen M-L, Fan S-Z, Cheng C-Y. The effect of 3,3-di-pyridyl-methyl-1-phenyl-2-indolinone on the nerve terminal currents of mouse skeletal muscles. Neuropharmacology 1992;31:943-947.
57. Van-Dyck CH, Lin CH, Robinson R, et al. Effects of the acetylcholine releaser linopirdine on SPECT rCBF and cognitive function in Alzheimer's disease. J Nucl Med (Suppl 5) 1995;36:238.
58. Vickroy TW. Presynaptic cholinergic actions by the putative cognitive enhancing agent DuP 996. J Pharmacol Exp Ther 1993;264:910-917.
59. Yankner BA, Mesulam M-M. β-Amyloid and the pathogenesis of Alzheimer's Disease. New Eng J Med 1991;325:1849-1857.
60. Zaczek R, Tinker WJ, Logue AR, Cain GA, Teleha CA, Tam SW. Effects of linopirdine, HP-749, and glycyl-prolyl-glutamate on transmitter release and uptake. Drug Develop Res 1993;29:203-208.
61. Zaczek R, Tinker WJ, Tam SW. Unique properties of norepinephrine release from terminals arising from the locus coeruleus: High potassium sensitivity and lack of linopirdine (DuP 996) enhancement. Neurosci Lett 1993;155:107-111.
62. Zaczek R, Rohrbach KW, Tam SW, Cook L. Preclinical evaluation of linopirdine: Neurochemical and behavioral effects. Advances in behavioral biology. In: Hanin I, Yoshida M, Fisher A, eds. Alzheimer's and Parkinson's Diseases: Recent Developments. 1995;44:491-498.