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Chemical Compound Review

AC1L9FXA     2,3-dihydroacridin-9-amine

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Disease relevance of Tacrine


Psychiatry related information on Tacrine

  • Tacrine in Alzheimer's disease [6].
  • Age, severity of dementia, and exposure to tacrine prior to randomization had no clear influence on the treatment effect [7].
  • The results indicate tha the meningoencephalitis induced by SIV in monkeys is similar to the lesions of the central nervous system in patients with AIDS and that SIV infection in the macaque is a useful animal model to study the pathogenesis of human immunodeficiency virus--related subacute encephalitis or AIDS encephalopathy [8].
  • A recent review suggests that tacrine is modestly effective in treating cognitive symptoms and that-neuroleptic drugs are modestly effective in treating agitation and aggression [9].
  • The two models appeared consistent, the main aspects they had in common being (a) the individuation of the strongly negative contribution of the substituents in position 7 of tacrine and (b) a tentative assignment of the hydrophobic character to the favorable effect exerted by the substituents in position 6 [10].

High impact information on Tacrine

  • It therefore seems likely tha differential alterations in the rate of histone synthesis do not occur to a significant degree as cells proceed through the cycle, but the association of newly synthesized histones with DNA takes place after the onset of DNA replication [11].
  • Moreover, atypical BuChE demonstrated 1/200th the affinity for tacrine of normal BuChE or the related enzyme acetylcholinesterase (AChE) [12].
  • Meta-analysis of tacrine for Alzheimer disease: the influence of industry sponsors [13].
  • Cholinesterase inhibition for Alzheimer disease: a meta-analysis of the tacrine trials. Dementia Trialists' Collaboration [7].
  • Among patients receiving 80 mg/d of tacrine, 51% achieved a four-point or greater improvement of the ADAS cognitive component after 12 weeks of treatment [14].

Chemical compound and disease context of Tacrine


Biological context of Tacrine


Anatomical context of Tacrine


Associations of Tacrine with other chemical compounds


Gene context of Tacrine

  • Cabp4(-/-) retinas also had ectopic synapses originating from rod bipolar and horizontal cells tha HJt extended into the outer nuclear layer [30].
  • Recent studies using human liver microsomes have suggested that a single liver enzyme, cytochrome P450 1A2 (CYP1A2), catalyzes the major route of metabolism and elimination of tacrine, and also catalyzes the pathway(s) involved in the generation of reactive metabolites capable of covalent protein binding and cytotoxicity [31].
  • This indicates tha different molecular mechanisms might be operational for low and high salt responses of the GPD1 promoter [32].
  • BuChE mutations that prevented tacrine interactions also hampered its ability to bind other drugs and inhibitors, which suggests a partial overlap of the binding sites [28].
  • The histamine receptor H1 antagonist diphenhydramine, the antimalarial drug amodiaquine, the antifolate drug metoprine, and the anticholinesterase drug tacrine (an early drug for Alzheimer's disease) are surprisingly all potent HNMT inhibitors, having inhibition constants in the range of 10-100nM [33].

Analytical, diagnostic and therapeutic context of Tacrine

  • A double-blind, placebo-controlled multicenter study of tacrine for Alzheimer's disease. The Tacrine Collaborative Study Group [15].
  • RESULTS--Among the 2446 patients who received tacrine in clinical trials, ALT levels greater than the upper limit of normal (ULN) occurred on at least one occasion in 1203 patients (49%), ALT levels greater than three times the ULN occurred in 621 patients (25%), and ALT levels greater than 20 times the ULN occurred in 40 patients (2%) [2].
  • Tacrine is a cholinesterase inhibitor with activity in the central nervous system originally marketed for the reversal of competitive neuromuscular blockade [5].
  • These results indicate that T4+ and T8+ T lymphocytes have receptors for different classes of MHC antigens and suggest tha cytotoxic T4+ subpopulations might be important in human transplantation and autoimmune disorders [34].
  • These results suggest tha MSA paces MEC theta rhythm and that the presumed cholinergic projection which mediates this function travels in the dorsal fornix [35].


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  3. Run-in periods in randomized trials: implications for the application of results in clinical practice. Pablos-Méndez, A., Barr, R.G., Shea, S. JAMA (1998) [Pubmed]
  4. Uncoupling of rat and human mitochondria: a possible explanation for tacrine-induced liver dysfunction. Berson, A., Renault, S., Lettéron, P., Robin, M.A., Fromenty, B., Fau, D., Le Bot, M.A., Riché, C., Durand-Schneider, A.M., Feldmann, G., Pessayre, D. Gastroenterology (1996) [Pubmed]
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  6. Tacrine in Alzheimer's disease. Lachs, M. N. Engl. J. Med. (1993) [Pubmed]
  7. Cholinesterase inhibition for Alzheimer disease: a meta-analysis of the tacrine trials. Dementia Trialists' Collaboration. Qizilbash, N., Whitehead, A., Higgins, J., Wilcock, G., Schneider, L., Farlow, M. JAMA (1998) [Pubmed]
  8. Simian immunodeficiency virus-induced meningoencephalitis: natural history and retrospective study. Ringler, D.J., Hunt, R.D., Desrosiers, R.C., Daniel, M.D., Chalifoux, L.V., King, N.W. Ann. Neurol. (1988) [Pubmed]
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  10. SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues. Recanatini, M., Cavalli, A., Belluti, F., Piazzi, L., Rampa, A., Bisi, A., Gobbi, S., Valenti, P., Andrisano, V., Bartolini, M., Cavrini, V. J. Med. Chem. (2000) [Pubmed]
  11. G1 and S phase mammalian cells synthesize histones at equivalent rates. Groppi, V.E., Coffino, P. Cell (1980) [Pubmed]
  12. Genetic predisposition to adverse consequences of anti-cholinesterases in 'atypical' BCHE carriers. Loewenstein-Lichtenstein, Y., Schwarz, M., Glick, D., Nørgaard-Pedersen, B., Zakut, H., Soreq, H. Nat. Med. (1995) [Pubmed]
  13. Meta-analysis of tacrine for Alzheimer disease: the influence of industry sponsors. Koepp, R., Miles, S.H. JAMA (1999) [Pubmed]
  14. A controlled trial of tacrine in Alzheimer's disease. The Tacrine Study Group. Farlow, M., Gracon, S.I., Hershey, L.A., Lewis, K.W., Sadowsky, C.H., Dolan-Ureno, J. JAMA (1992) [Pubmed]
  15. A double-blind, placebo-controlled multicenter study of tacrine for Alzheimer's disease. The Tacrine Collaborative Study Group. Davis, K.L., Thal, L.J., Gamzu, E.R., Davis, C.S., Woolson, R.F., Gracon, S.I., Drachman, D.A., Schneider, L.S., Whitehouse, P.J., Hoover, T.M. N. Engl. J. Med. (1992) [Pubmed]
  16. Influence of the CYP1A2 inhibitor fluvoxamine on tacrine pharmacokinetics in humans. Becquemont, L., Ragueneau, I., Le Bot, M.A., Riche, C., Funck-Brentano, C., Jaillon, P. Clin. Pharmacol. Ther. (1997) [Pubmed]
  17. Effects of estrogen replacement therapy on response to tacrine in patients with Alzheimer's disease. Schneider, L.S., Farlow, M.R., Henderson, V.W., Pogoda, J.M. Neurology (1996) [Pubmed]
  18. Role of the anteroventral third ventricle region and the renin angiotensin system in methylprednisolone hypertension. Marson, O., Ribeiro, A.B., Tufik, S., Filho, G.A., Saragoço, M.A., Ramos, O.L. Hypertension (1981) [Pubmed]
  19. T cell regulation of immunoglobulin class expression in the antibody response to trinitrophenyl-ficoll. Evidence for T cell enhancement of the immunoglobulin class switch. Mongini, P.K., Paul, W.E., Metcalf, E.S. J. Exp. Med. (1982) [Pubmed]
  20. Tacrine in Alzheimer's disease. Eagger, S.A., Levy, R., Sahakian, B.J. Lancet (1991) [Pubmed]
  21. An antibody Fab selected from a recombinant phage display library detects deesterified pectic polysaccharide rhamnogalacturonan II in plant cells. Williams, M.N., Freshour, G., Darvill, A.G., Albersheim, P., Hahn, M.G. Plant Cell (1996) [Pubmed]
  22. Characterization of the interaction of plant transcription factors using a bacterial repressor protein. Frohberg, C., Heins, L., Gatz, C. Proc. Natl. Acad. Sci. U.S.A. (1991) [Pubmed]
  23. Lewy bodies and response to tacrine in Alzheimer's disease. Levy, R., Eagger, S., Griffiths, M., Perry, E., Honavar, M., Dean, A., Lantos, P. Lancet (1994) [Pubmed]
  24. Effects of bombesin and bombesin-like peptides on gastrointestinal myoelectric activity. Caprilli, R., Melchiorri, P., Improta, G., Vernia, P., Frieri, G. Gastroenterology (1975) [Pubmed]
  25. Structure and function of rat liver polysome populations. I. Complexity, frequency distribution, and degree of uniqueness of free and membrane-bound polysomal polyadenylate-containing RNA populations. Mueckler, M.M., Pitot, H.C. J. Cell Biol. (1981) [Pubmed]
  26. Modification of practice-dependent plasticity in human motor cortex by neuromodulators. Meintzschel, F., Ziemann, U. Cereb. Cortex (2006) [Pubmed]
  27. Inhibition of tacrine oral clearance by cimetidine. Forgue, S.T., Reece, P.A., Sedman, A.J., deVries, T.M. Clin. Pharmacol. Ther. (1996) [Pubmed]
  28. Overlapping drug interaction sites of human butyrylcholinesterase dissected by site-directed mutagenesis. Loewenstein-Lichtenstein, Y., Glick, D., Gluzman, N., Sternfeld, M., Zakut, H., Soreq, H. Mol. Pharmacol. (1996) [Pubmed]
  29. Plasma tacrine concentrations are significantly increased by concomitant hormone replacement therapy. Laine, K., Palovaara, S., Tapanainen, P., Manninen, P. Clin. Pharmacol. Ther. (1999) [Pubmed]
  30. Essential role of Ca2+-binding protein 4, a Cav1.4 channel regulator, in photoreceptor synaptic function. Haeseleer, F., Imanishi, Y., Maeda, T., Possin, D.E., Maeda, A., Lee, A., Rieke, F., Palczewski, K. Nat. Neurosci. (2004) [Pubmed]
  31. The caffeine breath test does not identify patients susceptible to tacrine hepatotoxicity. Fontana, R.J., Turgeon, D.K., Woolf, T.F., Knapp, M.J., Foster, N.L., Watkins, P.B. Hepatology (1996) [Pubmed]
  32. Rap1p-binding sites in the saccharomyces cerevisiae GPD1 promoter are involved in its response to NaCl. Eriksson, P., Alipour, H., Adler, L., Blomberg, A. J. Biol. Chem. (2000) [Pubmed]
  33. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. Horton, J.R., Sawada, K., Nishibori, M., Cheng, X. J. Mol. Biol. (2005) [Pubmed]
  34. Clonal analysis of human cytotoxic T lymphocytes: T4+ and T8+ effector T cells recognize products of different major histocompatibility complex regions. Meuer, S.C., Schlossman, S.F., Reinherz, E.L. Proc. Natl. Acad. Sci. U.S.A. (1982) [Pubmed]
  35. Medial septal area lesions disrupt theta rhythm and cholinergic staining in medial entorhinal cortex and produce impaired radial arm maze behavior in rats. Mitchell, S.J., Rawlins, J.N., Steward, O., Olton, D.S. J. Neurosci. (1982) [Pubmed]
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