tacrine

Summary

Summary: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.

Top Publications

  1. ncbi The physicochemical properties and the in vivo AChE inhibition of two potential anti-Alzheimer agents, bis(12)-hupyridone and bis(7)-tacrine
    Hua Yu
    Institute of Chinese Medical Sciences, University of Macau, Macau SAR, PR China
    J Pharm Biomed Anal 46:75-81. 2008
  2. ncbi Molecular and genetic association of interleukin-6 in tacrine-induced hepatotoxicity
    Daniel F Carr
    Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool, UK
    Pharmacogenet Genomics 17:961-72. 2007
  3. ncbi Effect of tacrine on EEG slowing in the rat: enhancement by concurrent monoamine therapy
    H C Dringenberg
    Department of Psychology, Queen s University, Kingston, Ontario, Canada
    Neurobiol Aging 21:135-43. 2000
  4. ncbi Effects of a tacrine-8-hydroxyquinoline hybrid (IQM-622) on Aβ accumulation and cell death: involvement in hippocampal neuronal loss in Alzheimer's disease
    Desiree Antequera
    Neuroscience Group, Instituto de Investigación Hospital 12 de Octubre I 12, Madrid, Spain
    Neurobiol Dis 46:682-91. 2012
  5. ncbi Comparative effect of Prunus persica L. BATSCH-water extract and tacrine (9-amino-1,2,3,4-tetrahydroacridine hydrochloride) on concentration of extracellular acetylcholine in the rat hippocampus
    Yeon Kye Kim
    National Research Laboratory for Glycobiology NRLG, Korean Ministry of Science and Technology, Kyungju City, 780 714, Kyungbuk, South Korea
    J Ethnopharmacol 87:149-54. 2003
  6. ncbi Tacrine-based dual binding site acetylcholinesterase inhibitors as potential disease-modifying anti-Alzheimer drug candidates
    Pelayo Camps
    Laboratori de Química Farmacèutica Unitat Associada al CSIC, Facultat de Farmacia, and Institut de Biomedicina IBUB, Universitat de Barcelona, Av Diagonal 643, E 08028 Barcelona, Spain
    Chem Biol Interact 187:411-5. 2010
  7. ncbi Isolation and identification of phlorotannins from Ecklonia stolonifera with antioxidant and hepatoprotective properties in tacrine-treated HepG2 cells
    Min Sup Lee
    Department of Food Science and Nutrition, Pukyong National University, Busan 608 737, South Korea
    J Agric Food Chem 60:5340-9. 2012
  8. ncbi Diabetes-induced central cholinergic neuronal loss and cognitive deficit are attenuated by tacrine and a Chinese herbal prescription, kangen-karyu: elucidation in type 2 diabetes db/db mice
    Qi Zhao
    Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930 0194, Japan
    J Pharmacol Sci 117:230-42. 2011
  9. ncbi Production and on-line acetylcholinesterase bioactivity profiling of chemical and biological degradation products of tacrine
    Lygia Azevedo Marques
    VU University Amsterdam, Faculty of Sciences, Section of Biomolecular Analysis, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
    J Pharm Biomed Anal 53:609-16. 2010
  10. ncbi Effect of donepezil and tacrine on oxidative stress in intracerebral streptozotocin-induced model of dementia in mice
    Gunjan Saxena
    Division of Pharmacology, Central Drug Research Institute, PO Box 173, Lucknow UP 226001, India
    Eur J Pharmacol 581:283-9. 2008

Research Grants

Detail Information

Publications243 found, 100 shown here

  1. ncbi The physicochemical properties and the in vivo AChE inhibition of two potential anti-Alzheimer agents, bis(12)-hupyridone and bis(7)-tacrine
    Hua Yu
    Institute of Chinese Medical Sciences, University of Macau, Macau SAR, PR China
    J Pharm Biomed Anal 46:75-81. 2008
    The lipophilicity and solubility profiles of bis(12)-hupyridone (B12H) and bis(7)-tacrine (B7T), two novel acetylcholinesterase inhibitors dimerized from huperzine A fragments and tacrine, respectively, were investigated over a broad pH ..
  2. ncbi Molecular and genetic association of interleukin-6 in tacrine-induced hepatotoxicity
    Daniel F Carr
    Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool, UK
    Pharmacogenet Genomics 17:961-72. 2007
    b>Tacrine, an anticholinesterase used to treat Alzheimer's disease (AD), leads to an increase in serum alanine aminotransferase (ALT) levels. The factors determining individual susceptibility are largely unknown...
  3. ncbi Effect of tacrine on EEG slowing in the rat: enhancement by concurrent monoamine therapy
    H C Dringenberg
    Department of Psychology, Queen s University, Kingston, Ontario, Canada
    Neurobiol Aging 21:135-43. 2000
    ..5-4 Hz) and theta (4-8 Hz) bands affected most severely. The acetylcholinesterase inhibitor tacrine, at doses between 10 and 20 mg/kg, reversed these EEG changes; co-administration of tacrine and the noradrenaline-..
  4. ncbi Effects of a tacrine-8-hydroxyquinoline hybrid (IQM-622) on Aβ accumulation and cell death: involvement in hippocampal neuronal loss in Alzheimer's disease
    Desiree Antequera
    Neuroscience Group, Instituto de Investigación Hospital 12 de Octubre I 12, Madrid, Spain
    Neurobiol Dis 46:682-91. 2012
    ..A multifunctional molecule, the hybrid tacrine-8-hydroxyquinoline (named IQM-622), displays cholinergic, antioxidant, copper-complexing and neuroprotective ..
  5. ncbi Comparative effect of Prunus persica L. BATSCH-water extract and tacrine (9-amino-1,2,3,4-tetrahydroacridine hydrochloride) on concentration of extracellular acetylcholine in the rat hippocampus
    Yeon Kye Kim
    National Research Laboratory for Glycobiology NRLG, Korean Ministry of Science and Technology, Kyungju City, 780 714, Kyungbuk, South Korea
    J Ethnopharmacol 87:149-54. 2003
    ..the extracellular acetylcholine concentration in the hippocampus of rats were evaluated, and compared to that of tacrine (9-amino-1,2,3,4-tetrahydroacridine hydrochloride), a well-known and centrally acting acetylcholinesterase (AChE) ..
  6. ncbi Tacrine-based dual binding site acetylcholinesterase inhibitors as potential disease-modifying anti-Alzheimer drug candidates
    Pelayo Camps
    Laboratori de Química Farmacèutica Unitat Associada al CSIC, Facultat de Farmacia, and Institut de Biomedicina IBUB, Universitat de Barcelona, Av Diagonal 643, E 08028 Barcelona, Spain
    Chem Biol Interact 187:411-5. 2010
    ..Two novel families of dual binding site acetylcholinesterase (AChE) inhibitors have been developed, consisting of a tacrine or 6-chlorotacrine unit as the active site interacting moiety, either the 5,6-dimethoxy-2-[(4-piperidinyl)methyl]-..
  7. ncbi Isolation and identification of phlorotannins from Ecklonia stolonifera with antioxidant and hepatoprotective properties in tacrine-treated HepG2 cells
    Min Sup Lee
    Department of Food Science and Nutrition, Pukyong National University, Busan 608 737, South Korea
    J Agric Food Chem 60:5340-9. 2012
    ..activities against 2,2-diphenyl-1-picrylhydrazyl and suppressed the intracellular reactive oxygen species in tacrine-treated HepG2 cells...
  8. ncbi Diabetes-induced central cholinergic neuronal loss and cognitive deficit are attenuated by tacrine and a Chinese herbal prescription, kangen-karyu: elucidation in type 2 diabetes db/db mice
    Qi Zhao
    Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930 0194, Japan
    J Pharmacol Sci 117:230-42. 2011
    ..KK (100 - 200 mg/kg per day) and the reference drug tacrine (THA: 2.5 mg/kg per day) ameliorated the performance of O-db/db mice without affecting their serum glucose level...
  9. ncbi Production and on-line acetylcholinesterase bioactivity profiling of chemical and biological degradation products of tacrine
    Lygia Azevedo Marques
    VU University Amsterdam, Faculty of Sciences, Section of Biomolecular Analysis, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
    J Pharm Biomed Anal 53:609-16. 2010
    The present paper describes a methodology for rapid assessment of chemical and biological degradation products of tacrine and their bioactivity for acetylcholinesterase (AChE)...
  10. ncbi Effect of donepezil and tacrine on oxidative stress in intracerebral streptozotocin-induced model of dementia in mice
    Gunjan Saxena
    Division of Pharmacology, Central Drug Research Institute, PO Box 173, Lucknow UP 226001, India
    Eur J Pharmacol 581:283-9. 2008
    ..Therefore, the present study was designed to investigate the influence of antidementia drugs, tacrine and donepezil, on biochemical markers of oxidative stress, glutathione (GSH) and malondialdehyde (MDA), and ..
  11. ncbi Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition
    Sompop Bencharit
    Department of Chemistry, School of Dentistry, University of North Carolina, Chapel Hill, 27599, USA
    Chem Biol 10:341-9. 2003
    ..We determined the 2.4 A crystal structure of hCE1 in complex with tacrine, the first drug approved for treating Alzheimer's disease, and compare this structure to the Torpedo californica ..
  12. ncbi New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties
    Rafael Leon
    Laboratorio de Radicales Libres IQOG, CSIC, C Juan de la Cierva 3, 28006 Madrid, Spain
    Bioorg Med Chem 16:7759-69. 2008
    ..In this communication, we describe the synthesis and biological evaluation of tacripyrimedones 1-5, a series of new tacrine-1,4-dihydropyridine hybrids bearing the general structure of 11-amino-12-aryl-3,3-dimethyl-3,4,5,7,8,9,10,12-..
  13. ncbi Intranasal mucoadhesive microemulsion of tacrine to improve brain targeting
    Viral V Jogani
    Technology Information Forecasting and Assessment Council TIFAC, Centre of Relevance and Excellence CORE in New Drug Delivery Systems NDDS, The Maharaja Sayajirao University of Baroda, Fatehganj, India
    Alzheimer Dis Assoc Disord 22:116-24. 2008
    The aim of the investigation was to prepare and characterize microemulsion/mucoadhesive microemulsion of tacrine (TME/TMME), assess its pharmacokinetic and pharmacodynamic performances for brain targeting and for improvement in memory in ..
  14. ncbi Targeted delivery of tacrine into the brain with polysorbate 80-coated poly(n-butylcyanoacrylate) nanoparticles
    Barnabas Wilson
    Department of Pharmaceutics, J S S College of Pharmacy, Ootacamund, Tamil Nadu, India
    Eur J Pharm Biopharm 70:75-84. 2008
    The purpose of the present study was to investigate the possibility of targeting an anti-Alzheimer's drug tacrine in the brain using polymeric nanoparticles...
  15. ncbi Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase
    L Savini
    Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Via Aldo Moro, 53100, Siena, Italy
    Bioorg Med Chem Lett 11:1779-82. 2001
    Based upon synthetic and biochemical results, a novel and potent tacrine analogue and heterobivalent analogues of tacrine, were designed...
  16. ncbi Highly selective inhibition of butyrylcholinesterase by a novel melatonin-tacrine heterodimers
    Anna Zawadzka
    Faculty of Chemistry, University of Warsaw, Warsaw, Poland
    J Pineal Res 54:435-41. 2013
    Novel inhibitors of cholinesterases, especially butyrylcholinesterase (BuChE), were obtained by coupling melatonin-tacrine heterodimers via the carbamate bond...
  17. ncbi Effects of huperzine A on acetylcholinesterase isoforms in vitro: comparison with tacrine, donepezil, rivastigmine and physostigmine
    Qin Zhao
    State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, People s Republic of China
    Eur J Pharmacol 455:101-7. 2002
    Five inhibitors of acetylcholinesterase, huperzine A, donepezil, tacrine, rivastigmine and physostigmine, were compared with regard to their effects on different molecular forms of acetylcholinesterase in cerebral cortex, hippocampus, ..
  18. ncbi Effects of bis(7)-tacrine on spontaneous synaptic activity and on the nicotinic ACh receptor of Torpedo electric organ
    E Ros
    Laboratori de Neurobiologia Cellular i Molecular, , Facultat de Medicina, Hospital de Bellvitge, Universitat de Barcelona, E-08907 L'Hospitalet de Llobregat, Spain
    J Neurophysiol 86:183-9. 2001
    Bis(7)-tacrine is a potent acetylcholinesterase inhibitor in which two tacrine molecules are linked by a heptylene chain. We tested the effects of bis(7)-tacrine on the spontaneous synaptic activity...
  19. ncbi Bakuchiol: a hepatoprotective compound of Psoralea corylifolia on tacrine-induced cytotoxicity in Hep G2 cells
    H Cho
    MRRC and College of Pharmacy, Wonkwang University, Iksan, Korea
    Planta Med 67:750-1. 2001
    ..compound, bakuchiol (1), together with two moderately active compounds, bakuchicin (2) and psoralen (3), on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells. The EC(50) values of compounds 1 - 3 are 1.0, 47.0, 50...
  20. ncbi Neuroprotective effects of galanthamine and tacrine against glutamate neurotoxicity
    Yuki Takada-Takatori
    Department of Pharmacology, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto 606 8501, Japan
    Eur J Pharmacol 549:19-26. 2006
    ..mechanisms of the neuroprotective effects of two central-type acetylcholinesterase inhibitors, galanthamine and tacrine, on nitric oxide-mediated glutamate neurotoxicity using primary cultures from the cerebral cortex of fetal rats...
  21. ncbi Characterisation of the anticholinesterase activity of two new tacrine-huperzine A hybrids
    Maria del Mar Alcalá
    Dpt de Farmacologia, de Terapeutica i de Toxicologia, Facultat de Medicina, Universitat Autonoma de Barcelona, 08193 Bellaterra Barcelona, Spain
    Neuropharmacology 44:749-55. 2003
    The effects of two tacrine-huperzine A hybrids, (+/-)-huprine Y and (+/-)-huprine Z, have been evaluated. Bovine and human acetylcholinesterase (AChE) and human butyrylcholinesterase (BChE) inhibition were assayed by Ellman's method...
  22. ncbi Hepatoprotective compounds of the roots of Cudrania tricuspidata on tacrine-induced cytotoxicity in Hep G2 cells
    Ren Bo An
    College of Pharmacy, Wonkwang University, Iksan, Korea
    Biol Pharm Bull 29:838-40. 2006
    ..9+/-1.5 microM, against tacrine-induced cytotoxicity in Hep G2 cells. Silybin as positive control showed an EC50 value of 84.76+/-0.5 microM...
  23. ncbi Electroencephalographic activation by tacrine, deprenyl, and quipazine: cholinergic vs. non-cholinergic contributions
    Hans C Dringenberg
    Department of Psychology, Queen s University, K7L 3N6, Kingston, Ontario, Canada
    Eur J Pharmacol 447:43-50. 2002
    ..The acetylcholinesterase inhibitor tacrine (5-20 mg/kg) restored EEG activation in the low dose scopolamine group, but was less effective against the high ..
  24. ncbi Donepezil-tacrine hybrid related derivatives as new dual binding site inhibitors of AChE
    D Alonso
    NeuroPharma, S A, Avda de la Industria 52, 28760 Tres Cantos Madrid, Spain
    Bioorg Med Chem 13:6588-97. 2005
    A new series of donepezil-tacrine hybrid related derivatives have been synthesised as dual acetylcholinesterase inhibitors that could bind simultaneously to the peripheral and catalytic sites of the enzyme...
  25. ncbi Sesquiterpenes with hepatoprotective activity from Cnidium monnieri on tacrine-induced cytotoxicity in Hep G2 cells
    Hyuncheol Oh
    Professional Graduate School of Oriental Medicine, Wonkwang University, Iksan, Korea
    Planta Med 68:748-9. 2002
    ..Compounds 1 and 2 showed hepatoprotective effects on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells. The EC50 values of compounds 1 and 2 were 20.6 +/- 1...
  26. ncbi Tacrine attenuates hydrogen peroxide-induced apoptosis by regulating expression of apoptosis-related genes in rat PC12 cells
    Rui Wang
    State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 294 Tai Yuan Road, Shanghai 200031, PR China
    Brain Res Mol Brain Res 107:1-8. 2002
    The present studies investigated the effects of tacrine, a selective acetylcholinesterase (AChE) inhibitor and promising anti-dementia agent, on hydrogen peroxide (H(2)O(2))-induced apoptosis and the expression of apoptosis-related genes ..
  27. ncbi Nose-to-brain delivery of tacrine
    Viral V Jogani
    Department of Pharmacy, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Post Box No 51, Kalabhavan, Vadodara 390001, India
    J Pharm Pharmacol 59:1199-205. 2007
    In the treatment of Alzheimer's disease tacrine, a cholinesterase inhibitor, is not the drug of choice due to its low oral bioavailability, extensive hepatic first-pass effect, rapid clearance from the systemic circulation, pronounced ..
  28. ncbi Tacrine-melatonin hybrids as multifunctional agents for Alzheimer's disease, with cholinergic, antioxidant, and neuroprotective properties
    María Isabel Fernández-Bachiller
    Instituto de Química Médica, Consejo Superior de Investigaciones Cientificas CSIC, C Juan de la Cierva 3, 28006 Madrid, Spain
    ChemMedChem 4:828-41. 2009
    b>Tacrine-melatonin hybrids were designed and synthesized as new multifunctional drug candidates for Alzheimer's disease...
  29. ncbi Tribuli fructus constituents protect against tacrine-induced cytotoxicity in HepG2 cells
    Erisa Byun
    Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University, Iksan 570 749, Korea
    Arch Pharm Res 33:67-70. 2010
    ..Compounds 1 and 3 showed significant hepatoprotective activities, with EC50 values of 13.46 +/- 0.2 and 7.06 +/- 0.7 microM, respectively, against tacrine-induced cytotoxicity in HepG2 cells.
  30. ncbi Longitudinal changes in quantitative EEG during long-term tacrine treatment of patients with Alzheimer's disease
    V Jelic
    Karolinska Institute, Department of Clinical Neuroscience and Family Medicine, Huddinge University Hospital, Sweden
    Neurosci Lett 254:85-8. 1998
    ..In order to define the profile of EEG changes during tacrine long-term treatment, for 12 months we followed 15 AD patients receiving an optimal individually tolerable dose...
  31. ncbi Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers
    Stefano Rizzo
    Max Planck Institut fur molekulare Physiologie, Abteilung Chemische Biologie, Otto Hahn Str 11, 44227 Dortmund, Germany
    Eur J Med Chem 46:4336-43. 2011
    ..This is the case of tacrine and its dimeric derivative bis(7)-tacrine which, for instance, paved the way for the development of a broad ..
  32. ncbi Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors
    Huang Tang
    State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Chemical Engineering of Guangxi Normal University, Guilin 541004, PR China
    Eur J Med Chem 46:4970-9. 2011
    ..The new hybrids consist of a unit of 1-azabenzanthrone and a tacrine or its congener, connected through an oligomethylene linker containing an amine group at variable position...
  33. ncbi Synthesis and acetylcholinesterase/butyrylcholinesterase inhibition activity of new tacrine-like analogues
    J L Marco
    Laboratorio de Radicales Libres CSIC, Madrid, Spain
    Bioorg Med Chem 9:727-32. 2001
    ..These molecules are tacrine-like analogues which have been prepared from readily available polyfunctionalized ethyl [6-amino-5-cyano-4H-..
  34. ncbi Alaternin and emodin with hydroxyl radical inhibitory and/or scavenging activities and hepatoprotective activity on tacrine-induced cytotoxicity in HepG2 cells
    Hyun Ah Jung
    Research Institute of Marine Science and Technology, Korea Maritime University, Busan, 606 791, Korea
    Arch Pharm Res 27:947-53. 2004
    ..and emodin, to scavenge and/or inhibit hydroxyl radicals generated by the Fenton reaction and to protect tacrine-induced cytotoxicity in human liver derived HepG2 cells were evaluated, respectively...
  35. ncbi Tacrine derivatives-acetylcholinesterase interaction: 1H NMR relaxation study
    Maurizio Delfini
    Dipartimento di Chimica, Universita degli Studi La Sapienza, Piazzale Aldo Moro, 5 00185 Roma, Italy
    Bioorg Chem 35:243-57. 2007
    Two acetylcholinesterase (AChE) inhibitors structurally related to Tacrine, 6-methoxytacrine (1a) and 9-heptylamino-6-methoxytacrine (1b), and their interaction with Electrophorus Electricus AChE were investigated...
  36. ncbi Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge
    Edwin H Rydberg
    Department of Structural Biology, Weizmann Institute of Science, Rehovot 76100, Israel
    J Med Chem 49:5491-500. 2006
    ..X-ray crystal structures were solved for complexes with Torpedo californica acetylcholinesterase of two bivalent tacrine derivative compounds in which the two tacrine rings were separated by 5- and 7-carbon spacers...
  37. ncbi Homodimeric tacrine congeners as acetylcholinesterase inhibitors
    Ming Kuan Hu
    School of Pharmacy and Department of Pharmacology, National Defense Medical Center, 161 Section 6, Minchuan East Road Taipei, Taiwan 114, Republic of China
    J Med Chem 45:2277-82. 2002
    In the search for highly selective and potent derivatives of tacrine (1a), a number of homodimeric tacrine congeners were synthesized and conducted for their effects on rat acetylcholinesterase (AChE) and human butyrylcholinesterase (..
  38. ncbi Tacrine therapy is associated with reduced mortality in nursing home residents with dementia
    Brian R Ott
    Department of Clinical Neurosciences, Center for Gerontology and Health Care Research, and Department of Community Health, Brown University, Providence, Rhode Island
    J Am Geriatr Soc 50:35-40. 2002
    To investigate the extent to which treatment with tacrine is associated with a reduction in mortality in nursing home residents with dementia.
  39. ncbi Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as dual inhibitors for cholinesterases and amyloid beta aggregation
    Wen Luo
    Sun Yat Sen University, Guangzhou, People s Republic of China
    Bioorg Med Chem 19:763-70. 2011
    A new series of tacrine-multialkoxybenzene hybrids (9a-9n) were designed, synthesized and evaluated as dual inhibitors of cholinesterases (ChEs) and self-induced β-amyloid (Aβ) aggregation...
  40. ncbi Phenolic constituents of galla Rhois with hepatoprotective effects on tacrine- and nitrofurantoin-induced cytotoxicity in Hep G2 cells
    Ren Bo An
    College of Pharmacy, Wonkwang University, Korea
    Biol Pharm Bull 28:2155-7. 2005
    ..39+/-5.4 and 29.51+/-0.7 microM, respectively, against tacrine-induced cytotoxicity, and 150.9+/-6.4 and 23.81+/-0...
  41. ncbi New tacrine-hydrazinonicotinamide hybrids as acetylcholinesterase inhibitors of potential interest for the early diagnostics of Alzheimer's disease
    P Szymanski
    Department of Pharmaceutical Chemistry and Drug Analysis, Medical University, Lodz, Poland
    Pharmazie 61:269-73. 2006
    ..results of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition by an affinity series of tacrine-hydrazinonicotinamide hybrids are described...
  42. ncbi NO-donating tacrine hybrid compounds improve scopolamine-induced cognition impairment and show less hepatotoxicity
    Lei Fang
    Institute of Pharmacy, Friedrich Schiller University Jena, D 07743 Jena, Germany
    J Med Chem 51:7666-9. 2008
    A series of tacrine-NO donor hybrid compounds are synthesized and evaluated for cholinesterase inhibitory activity, cognition improving activity, and hepatotoxicity...
  43. ncbi Hybrid molecules from xanomeline and tacrine: enhanced tacrine actions on cholinesterases and muscarinic M1 receptors
    Lei Fang
    Center of Drug Discovery, China Pharmaceutical University, 210009 Nanjing, PR China
    J Med Chem 53:2094-103. 2010
    ..M(1) muscarinic receptor agonist xanomeline and the cholinesterase inhibitor and allosteric receptor modulator tacrine were prepared with varying spacer length of 10-17 atoms...
  44. ncbi Cholinergic and neuroprotective drugs for the treatment of Alzheimer and neuronal vascular diseases. II. Synthesis, biological assessment, and molecular modelling of new tacrine analogues from highly substituted 2-aminopyridine-3-carbonitriles
    Abdelouahid Samadi
    Laboratorio de Radicales Libres y Química Computacional IQOG, CSIC, C Juan de la Cierva 3, 28006 Madrid, Spain
    Bioorg Med Chem 19:122-33. 2011
    The synthesis, biological assessment, and molecular modelling of new tacrine analogues 11-22 is described...
  45. ncbi A new tacrine-melatonin hybrid reduces amyloid burden and behavioral deficits in a mouse model of Alzheimer's disease
    Carlos Spuch
    Neuroscience Laboratory, University Hospital, 12 de Octubre Research Center, 28041 Madrid, Spain
    Neurotox Res 17:421-31. 2010
    ..Emerging evidence indicates that antioxidants could be useful either for the prevention or treatment of AD. Tacrine and melatonin are well-known drugs which act as an acetylcholinesterase inhibitor and a free radical scavenger, ..
  46. ncbi Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions
    P R Carlier
    Department of Chemistry, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong
    J Med Chem 42:4225-31. 1999
    Dimeric acetylcholinesterase (AChE) inhibitors containing a single 9-amino-1,2,3,4-tetrahydroacridine (tacrine) unit were constructed in an effort to further delineate structural requirements for optimal binding to the AChE peripheral ..
  47. ncbi Cystamine-tacrine dimer: a new multi-target-directed ligand as potential therapeutic agent for Alzheimer's disease treatment
    A Minarini
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Neuropharmacology 62:997-1003. 2012
    ..The structure of tacrine, an acetylcholinesterase (AChE) inhibitor (AChEI), has been widely used as scaffold to provide new MTDLs...
  48. pmc Neuroprotective effects of bis(7)-tacrine against glutamate-induced retinal ganglion cells damage
    Jia Hua Fang
    Department of Ophthalmology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China
    BMC Neurosci 11:31. 2010
    ..Bis(7)-tacrine is a noncompetitive NMDA receptors antagonist that can prevent glutamate-induced hippocampal neurons damage...
  49. ncbi Synthesis and biological assessment of diversely substituted furo[2,3-b]quinolin-4-amine and pyrrolo[2,3-b]quinolin-4-amine derivatives, as novel tacrine analogues
    Carla Martins
    Research Institute for Medicines and Pharmaceutical Sciences, Faculty of Pharmacy, University of Lisbon, Av Prof Gama Pinto, 1649 003 Lisbon, Portugal
    Eur J Med Chem 46:6119-30. 2011
    ..Thus, we synthesized diversely substituted tacrine analogues 1-11 and 12-16 by Friedländer-type reaction of readily available o-amino(furano/pyrrolo)nitriles with ..
  50. ncbi Shuttle-box avoidance learning in mice: improvement by combined glucose and tacrine
    F Pavone
    Istituto di Psicobiologia e Psicofarmacologia, CNR, Roma, Italy
    Neurobiol Learn Mem 69:204-10. 1998
    Glucose and the acetylcholinesterase inhibitor tacrine were tested, alone and in combination, in mice of the CD-1 strain subjected to five daily shuttle-box training sessions...
  51. ncbi The secretion of amyloid beta-peptides is inhibited in the tacrine-treated human neuroblastoma cells
    D K Lahiri
    Institute of Psychiatric Research, Departments of Psychiatry and Neurology, 791 Union Drive, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Brain Res Mol Brain Res 62:131-40. 1998
    ..b>Tacrine, a cholinesterase inhibitor, has been shown to improve memory and cognitive functions in some patients with AD, ..
  52. ncbi Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates
    Lei Fang
    Lehrstuhl fur Pharmazeutische Medizinische Chemie, Institut fur Pharmazie, Friedrich Schiller Universitat Jena, Philosophenweg 14, D 07743 Jena, Germany
    Bioorg Med Chem Lett 18:2905-9. 2008
    Five tacrine-ferulic acid hybrids (6a-e) were designed and synthesized as multi-potent anti-Alzheimer drug candidates...
  53. ncbi Tacrine-NO donor and tacrine-ferulic acid hybrid molecules as new anti-Alzheimer agents: hepatotoxicity and influence on the cytochrome P450 system in comparison to tacrine
    Amelie Lupp
    Institute of Pharmacology and Toxicology, Friedrich Schiller University, Jena, Germany
    Arzneimittelforschung 60:229-37. 2010
    b>Tacrine (CAS 321-64-2) is a reversible acetylcholine esterase inhibitor that, despite exerting beneficial effects on Alzheimer's disease (AD), displays marked hepatotoxicity...
  54. ncbi Furocoumarins from Angelica dahurica with hepatoprotective activity on tacrine-induced cytotoxicity in Hep G2 cells
    Hyuncheol Oh
    Planta Med 68:463-4. 2002
    ..0 +/- 3.4 microM. Comparison of hepatoprotective activities for six furocoumarins 1 - 6 suggested that oxy-substitution at the C-9 position increased the hepatoprotective activity...
  55. ncbi Mitochondrial proteomic analysis and characterization of the intracellular mechanisms of bis(7)-tacrine in protecting against glutamate-induced excitotoxicity in primary cultured neurons
    Hongjun Fu
    Department of Biochemistry, Hong Kong University of Science and Technology, Hong Kong, China
    J Proteome Res 6:2435-46. 2007
    ..In this study, post-treatment of cerebellar granule neurons with bis(7)-tacrine significantly reversed declines in mitochondrial membrane potential, ATP production, and neuronal cell death ..
  56. ncbi Delayed evacuatory function due to specific smooth muscle reactivity in the gastrointestinal tracts of tacrine-treated rats
    A Krustev
    Department of Biophysics, Medical University, Plovdiv, Bulgaria
    Pharmacology 81:50-6. 2008
    Most of the side effects induced by tacrine are associated with the gastrointestinal (GI) tract...
  57. ncbi Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties
    María Isabel Fernández-Bachiller
    Instituto de Química Médica, Consejo Superior de Investigaciones Cientificas CSIC, Juan de la Cierva 3, 28006 Madrid, Spain
    J Med Chem 53:4927-37. 2010
    b>Tacrine and PBT2 (an 8-hydroxyquinoline derivative) are well-known drugs that inhibit cholinesterases and decrease beta-amyloid (Abeta) levels by complexation of redox-active metals, respectively...
  58. ncbi Tacrine derivatives and Alzheimer's disease
    V Tumiatti
    Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Curr Med Chem 17:1825-38. 2010
    ..b>Tacrine was the first AChEI introduced in therapy...
  59. ncbi Study of PMS777, a new type of acetylcholinesterase inhibitor, in human HepG2 cells. Comparison with tacrine and galanthamine on oxidative stress and mitochondrial impairment
    M J M Ezoulin
    Unité de Pharmacochimie Moléculaire et Systèmes Membranaires EA2381, Universite Paris 7 Denis Diderot, Case 7066, 2, place Jussieu, 75251 Paris Cedex 05, France
    Toxicol In Vitro 20:824-31. 2006
    Acetylcholinesterase inhibitors are commonly used as cognitive enhancers for dementia in aged people. Among them, tacrine (THA) but not galanthamine, was shown to exhibit hepatotoxicity which reduces its clinical use...
  60. ncbi Novel dimeric acetylcholinesterase inhibitor bis7-tacrine, but not donepezil, prevents glutamate-induced neuronal apoptosis by blocking N-methyl-D-aspartate receptors
    Wenming Li
    Department of Biochemistry and Biology, Hong Kong University of Science and Technology, Kowloon, Hong Kong
    J Biol Chem 280:18179-88. 2005
    The neuroprotective properties of bis(7)-tacrine, a novel dimeric acetylcholinesterase (AChE) inhibitor, on glutamate-induced excitotoxicity were investigated in primary cultured cerebellar granule neurons (CGNs)...
  61. ncbi Novel anti-Alzheimer's dimer Bis(7)-cognitin: cellular and molecular mechanisms of neuroprotection through multiple targets
    Wenming Li
    Department of Applied Biology and Chemical Technology, Institute of Modern Chinese Medicine, The Hong Kong Polytechnic University, Hong Kong SAR, China
    Neurotherapeutics 6:187-201. 2009
    ..decade, our group has developed several series of dimeric acetylcholinesterase (AChE) inhibitors derived from tacrine and huperzine A, a unique anti-Alzheimer's drug originally discovered from a traditional Chinese medicinal plant...
  62. ncbi The apolipoprotein E epsilon4 allele and the response to tacrine therapy in Alzheimer's disease
    A S Rigaud
    Hopital Broca, 54 56 Rue Pascal, 75013, Paris, France
    Eur J Neurol 7:255-8. 2000
    ..of our study was to evaluate the effects of the apolipoprotein E (ApoE) phenotype and gender on the response to tacrine treatment in Alzheimer's disease (AD). ApoE phenotyping was performed on 76 patients treated with tacrine for AD...
  63. ncbi Dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block L-type Ca(2+) channels
    N N Lermontova
    Department of Biological Research, Institute of Physiologically Active Substances, Russian Academy of Sciences, Chernogolovka, Moscow Region
    Bull Exp Biol Med 132:1079-83. 2001
    ..Antialzheimer preparations tacrine and dimebon improve survival of cerebellar granule cells during long-term incubation with Abeta25-35, the ..
  64. ncbi Tacrine and rate of progression in Alzheimer's disease--relation to ApoE allele genotype
    M Sjogren
    Institute of Clinical Neuroscience, Goteborg University, Sahlgrenska University Hospital Molndal, Sweden
    J Neural Transm 108:451-8. 2001
    ..To investigate the relation between tacrine treatment, inheritance of ApoE epsilon4 alleles, and rate of progression, the differences in MMSE and CIBIC ..
  65. ncbi Investigation into the in vivo effects of five novel tacrine/ferulic acid and beta-carboline derivatives on scopolamine-induced cognitive impairment in rats using radial maze paradigm
    Christian Fleck
    Institute of Pharmacology and Toxicology, Friedrich Schiller University, Jena, Germany
    Arzneimittelforschung 60:299-306. 2010
    Two tacrine-ferulic acid hybrids (1 A, 1 B) and three beta-carboline derivatives (BCs; 2A, 2B, 2C) were tested in vivo on 3-month-old female rats as multi-potent anti-Alzheimer drug candidates...
  66. ncbi Effects of four non-cholinergic cognitive enhancers in comparison with tacrine and galanthamine on scopolamine-induced amnesia in rats
    P Chopin
    Centre de Recherche Pierre Fabre, Castres, France
    Psychopharmacology (Berl) 106:26-30. 1992
    ..b>Tacrine or galanthamine, inhibitors of acetylcholinesterase, given in conjunction with scopolamine partially reversed the ..
  67. ncbi Effects of zonisamide on c-Fos expression under conditions of tacrine-induced tremulous jaw movements in rats: a potential mechanism underlying its anti-parkinsonian tremor effect
    Hideto Miwa
    Department of Neurology, Wakayama Medical University, 811 1 Kimiidera, Wakayama City, Wakayama 641 8510, Japan
    Parkinsonism Relat Disord 15:30-5. 2009
    To examine the mechanisms underlying the anti-tremor effect of zonisamide in rats under conditions of tacrine-induced tremulous jaw movements (TJMs).
  68. ncbi Promising anti-Alzheimer's dimer bis(7)-tacrine reduces beta-amyloid generation by directly inhibiting BACE-1 activity
    Hongjun Fu
    Department of Biochemistry, The Hong Kong University of Science and Technology, Hong Kong, China
    Biochem Biophys Res Commun 366:631-6. 2008
    ..In this study, the effect and mechanisms of bis(7)-tacrine (a promising anti-Alzheimer's dimer) on Abeta generation were investigated. Bis(7)-tacrine (0...
  69. ncbi Evidence for the involvement of central serotonergic mechanisms in cholinergic tremor induced by tacrine in Balb/c mice
    Hina Mehta
    Division of Clinical and Experimental Neurosciences, Indian Institute of Chemical Biology, Jadavpur, Calcutta
    Behav Brain Res 163:227-36. 2005
    b>Tacrine is a potent and reversible inhibitor of acetylcholinesterase (AChE) in the brain. It produces tremor in animals, which is believed to be due to an increase in the brain acetylcholine level following AChE inhibition...
  70. ncbi Tacrine-induced liver damage: an analysis of 19 candidate genes
    Ana Alfirevic
    Department of Pharmacology and Therapeutics, The University of Liverpool, Sherrington Building, Ashton Street, Liverpool, UK
    Pharmacogenet Genomics 17:1091-100. 2007
    b>Tacrine, the first acetylcholinesterase inhibitor used in the treatment of Alzheimer's disease, is associated with transaminase elevation in up to 50% of patients...
  71. ncbi Blockade of adenosine A2A receptors antagonizes parkinsonian tremor in the rat tacrine model by an action on specific striatal regions
    Nicola Simola
    Department of Toxicology and Centre of Excellence for Neurobiology of Dependence, University of Cagliari, 09124, Cagliari, Italy
    Exp Neurol 189:182-8. 2004
    Acute administration of the acetylcholinesterase inhibitor tacrine to rats induces tremulous jaw movements which can be used as a valuable model of parkinsonian tremor...
  72. ncbi East meets West in the search for Alzheimer's therapeutics - novel dimeric inhibitors from tacrine and huperzine A
    W M Li
    Department of Biochemistry, Hong Kong University of Science and Technology, Hong Kong Special Administrative Region, China
    Curr Alzheimer Res 4:386-96. 2007
    ..The novel dimers, derived from tacrine and the fragment of huperzine A (HA'), have been demonstrated to be potent and selective reversible inhibitors of ..
  73. ncbi Choline pivaloyl ester strengthened the benefit effects of Tacrine and Galantamine on electroencephalographic and cognitive performances in nucleus basalis magnocellularis-lesioned and aged rats
    V Rispoli
    Department of Pharmacobiological Sciences, University Magna Graecia of Catanzaro, Complesso Nini Barbieri, I 88021 Roccelletta di Borgia CZ, Italy
    Pharmacol Biochem Behav 84:453-67. 2006
    ..2,2-dimethylpropionate (choline pivaloyl ester) (CPE) and the Cholinesterase inhibitors (ChEIs) Tacrine (THA) and Galantamine (GAL)...
  74. ncbi Plasma levels of Abeta42 and Abeta40 in Alzheimer patients during treatment with the acetylcholinesterase inhibitor tacrine
    Hans Basun
    Department of Neurotec, Karolinska Institutet, Huddinge University Hospital, Sweden
    Dement Geriatr Cogn Disord 14:156-60. 2002
    ..could change the levels of Abeta in plasma, we measured Abeta42 and Abeta40 plasma levels in AD subjects before tacrine treatment and at weeks 2 and 6 of treatment...
  75. ncbi Tacrine-huperzine A hybrids (huprines): a new class of highly potent and selective acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease
    P Camps
    Laboratori de Química Farmacèutica, Facultat de Farmacia, Universitat de Barcelona, Av Diagonal 643, E 08028, Barcelona, Spain
    Mini Rev Med Chem 1:163-74. 2001
    b>Tacrine-huperzine A hybrids (huprines) are a new class of very potent and selective acetylcholinesterase (AChE) inhibitors. Huprines were designed from tacrine and (-)-huperzine A through a conjunctive approach...
  76. ncbi (+/-)-huprine Y, (-)-huperzine A and tacrine do not show neuroprotective properties in an apoptotic model of neuronal cytoskeletal alteration
    E G Jordà
    Unitat de Farmacologia i Farmacognosia, Barcelona, Spain
    J Alzheimers Dis 6:577-83; discussion 673-81. 2004
    ..b>Tacrine, (-)-huperzine A and (+/-)-huprine Y, the AChEI tested in the study, did not reverse the loss of neuronal ..
  77. ncbi Action of tacrine on muscarinic receptors in rat intestinal smooth muscle
    M A Becerra
    , Facultad de Farmacia, Universidad de Sevilla, , 41012 Sevilla, Spain
    J Auton Pharmacol 21:113-9. 2001
    1. The reversible cholinesterase inhibitor, tacrine (THA) was examined against the contractions of rat duodenum to acetylcholine and carbachol (cholinesterase resistant). 2...
  78. ncbi Possible role of hydroxylated metabolites of tacrine in drug toxicity and therapy of Alzheimer's disease
    Jiri Patocka
    Center of Advanced Studies, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic
    Curr Drug Metab 9:332-5. 2008
    b>Tacrine belongs to the group of acetylcholinesterse (AChE) inhibitors used as drugs for treatment of Alzheimer's disease (AD)...
  79. ncbi Bis(7)-tacrine, a promising anti-Alzheimer's dimer, affords dose- and time-dependent neuroprotection against transient focal cerebral ischemia
    Yuming Zhao
    Department of Biochemistry, Hong Kong University of Science and Technology, Hong Kong SAR, China
    Neurosci Lett 439:160-4. 2008
    Bis(7)-tacrine, a promising anti-Alzheimer's dimer, has been shown to have multiple neuroprotective activities in vitro. Here, we investigate whether bis(7)-tacrine attenuates focal cerebral ischemic impairment in vivo...
  80. ncbi Inhibition of NMDA-gated ion channels by bis(7)-tacrine: whole-cell and single-channel studies
    Yu Wei Liu
    Department of Neurobiology, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China
    Neuropharmacology 54:1086-94. 2008
    Bis(7)-tacrine is a novel dimeric acetylcholinesterase inhibitor derived from tacrine, and has been proposed as a promising agent to treat Alzheimer's disease...
  81. ncbi Actions of tacrine and galanthamine on histamine-N-methyltransferase
    O D Taraschenko
    Center for Neuropharmacology and Neuroscience, Albany Medical College, New York 12208, USA
    Methods Find Exp Clin Pharmacol 27:161-5. 2005
    ..The AD medication tacrine was previously shown to inhibit some forms of rodent histamine-N-methyltransferase (HNMT), but the effects of AD ..
  82. ncbi Development of a high performance liquid chromatography-tandem mass method for determination of bis(7)-tacrine, a promising anti-Alzheimer's dimer, in rat blood
    Hua Yu
    Department of Biochemistry, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, SAR, PR China
    J Pharm Biomed Anal 44:1133-8. 2007
    ..mass spectrometry with electrospray ionization was developed and applied for the quantification of bis(7)-tacrine (B7T) in rat blood...
  83. ncbi Acute nicotine effects on auditory sensory memory in tacrine-treated and nontreated patients with Alzheimer's disease: an event-related potential study
    C Engeland
    Department of Psychiatry and Psychology, University of Western Ontario, London, ON, Canada
    Pharmacol Biochem Behav 72:457-64. 2002
    ..Thirteen patients with Alzheimer's disease (AD), 6 receiving treatment with the cholinesterase inhibitor, tacrine [tetrahydroaminoacridine (THA)], and 7 receiving no treatment, were administered 2 mg of nicotine polacrilex and ..
  84. ncbi Tacrine inhibits topoisomerases and DNA synthesis to cause mitochondrial DNA depletion and apoptosis in mouse liver
    Abdellah Mansouri
    INSERM Unité 481, Faculte de Medecine Xavier Bichat, Paris, France
    Hepatology 38:715-25. 2003
    ..After several weeks of treatment, levels of alanine aminotransferase (ALT) increase in 50% of patients treated with tacrine for Alzheimer's disease. We looked for progressive effects on DNA to explain delayed toxicity...
  85. ncbi New performance of biosensor technology for Alzheimer's disease drugs: in vitro comparison of tacrine and 7-methoxytacrine
    Miroslav Pohanka
    Center of Advanced Studies, Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic
    Neuro Endocrinol Lett 29:755-8. 2008
    ..The first was commercialized drug tacrine (known also as Cognex) used for treatment of cognitive manifestation of Alzheimer\'s disease (AD)...
  86. ncbi Bis(7)-tacrine attenuates beta amyloid-induced neuronal apoptosis by regulating L-type calcium channels
    Hongjun Fu
    Department of Biochemistry, Hong Kong University of Science and Technology, Hong Kong, P R China
    J Neurochem 98:1400-10. 2006
    ..In the current study, we investigated the effects of bis(7)-tacrine, a novel dimeric AChE inhibitor, on Abeta-induced neurotoxicity in primary cortical neurons...
  87. ncbi Quantitative structure-activity relationship (QSAR) of tacrine derivatives against acetylcholinesterase (AChE) activity using variable selections
    Mankil Jung
    Department of Chemistry, Yonsei University, Seoul 120 749, Republic of Korea
    Bioorg Med Chem Lett 17:1082-90. 2007
    A diverse approach to the quantitative structure-activity relationship (QSAR) of tacrine derivatives against acetylcholinesterase (AChE) activity was studied using variable selections of stepwise multiple linear regression (MLR), genetic ..
  88. ncbi Bis(7)-tacrine prevents glutamate-induced excitotoxicity more potently than memantine by selectively inhibiting NMDA receptors
    Yu Wei Liu
    Wuhan Institute of Neuroscience and Drug Research, Jianghan University, Wuhan 430056, PR China
    Biochem Biophys Res Commun 369:1007-11. 2008
    We have recently reported that bis(7)-tacrine could prevent glutamate-induced neuronal apoptosis through NMDA receptors. In this study, we demonstrated that in cultured rat cortical neurons, bis(7)-tacrine (IC(50), 0...
  89. ncbi Novel dimeric bis(7)-tacrine proton-dependently inhibits NMDA-activated currents
    Jialie Luo
    Department of Biochemistry, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, PR China
    Biochem Biophys Res Commun 361:505-9. 2007
    Bis(7)-tacrine has been shown to prevent glutamate-induced neuronal apoptosis by blocking NMDA receptors. However, the characteristics of the inhibition have not been fully elucidated...
  90. ncbi Combined glutathione-S-transferase M1 and T1 genetic polymorphism and tacrine hepatotoxicity
    T Simon
    Pharmacology Department, INSERM SC4, Saint Antoine University, Paris, France
    Clin Pharmacol Ther 67:432-7. 2000
    Glutathione conjugation of tacrine reactive metabolites depends in part on the activity of glutathione-S-transferases (GST), of which two isozymes (GST M1 and GST T1) are polymorphically expressed.
  91. ncbi Selective and sensitive determination of bis(7)-tacrine, a high erythrocyte binding acetylcholinesterase inhibitor, in rat plasma by high-performance liquid chromatography-tandem mass spectrometry
    Li Zhang
    Department of Biochemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, SAR, People s Republic of China
    Biomed Chromatogr 22:414-20. 2008
    The current study aims to develop a specific and sensitive LC-MS/MS method for determination of bis(7)-tacrine (B7T) in rat plasma. A 100 microL plasma sample was extracted with ethyl acetate...
  92. ncbi Synergistic neuroprotection by bis(7)-tacrine via concurrent blockade of N-methyl-D-aspartate receptors and neuronal nitric-oxide synthase
    Wenming Li
    Department of Biochemistry, Hong Kong University of Science and Technology, Hong Kong, China
    Mol Pharmacol 71:1258-67. 2007
    ..the NO synthase (NOS) inhibitor, N(G)-monomethyl-L-arginine (L-NMMA), and the NMDAR antagonist memantine, bis(7)-tacrine was found to be more potent in reducing NO-mediated excitotoxicity and the release of NO caused by glutamate...
  93. ncbi Neuroprotection via inhibition of nitric oxide synthase by bis(7)-tacrine
    Wenming Li
    Department of Biochemistry, Hong Kong University of Science and Technology, Hong Kong, China
    Neuroreport 17:471-4. 2006
    Here we report that bis(7)-tacrine, a novel acetylcholinesterase inhibitor, exerts neuroprotective effects by inhibition of nitric oxide synthase...
  94. ncbi Controlled release tacrine delivery system for the treatment of Alzheimer's disease
    Q Yang
    College of Pharmacy and Pharmaceutical Sciences, Florida A and M University, Tallahassee, USA
    Drug Deliv 8:93-8. 2001
    ..b>Tacrine is one of the three drugs approved by the FDA for the treatment of Alzheimer's disease...
  95. ncbi SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues
    M Recanatini
    Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro 6, I 40126 Bologna, Italy
    J Med Chem 43:2007-18. 2000
    ..to derive a comprehensive SAR picture for the class of acetylcholinesterase (AChE) inhibitors related to tacrine, a drug currently in use for the treatment of the Alzheimer's disease...
  96. ncbi Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties
    María Isabel Rodríguez-Franco
    Instituto de Quimica Medica CSIC, 28006 Madrid, Spain
    J Med Chem 49:459-62. 2006
    b>Tacrine and melatonin are well-known drugs with activities as an acetylcholinesterase (AChE) inhibitor and free radical scavenger, respectively...
  97. ncbi The effects of chronic tacrine therapy on d-tubocurarine blockade in the soleus and tibialis muscles of the rat
    C Ibebunjo
    Department of Anaesthesia, Royal Victoria Hospital and McGill University, Montreal, Quebec, Canada
    Anesth Analg 85:431-6. 1997
    b>Tacrine (THA) is an anticholinesterase drug used to manage Alzheimer's dementia, but it is not clear how its chronic use might affect response to nondepolarizing muscle relaxants...
  98. ncbi Schisandrin B protects against tacrine- and bis(7)-tacrine-induced hepatotoxicity and enhances cognitive function in mice
    S Y Pan
    Department of Biochemistry, Hong Kong University of Science and Technology, China
    Planta Med 68:217-20. 2002
    Intragastric administration (100-200 micromol/kg) of tacrine (THA) or bis(7)-THA could cause an acute and dose-dependent increase in plasma alanine aminotransferases activity in mice at 6 h after the drug administration...
  99. ncbi Effect of tacrine on intracellular calcium in cholinergic SN56 neuronal cells
    V Dolezal
    Institute of Physiology, Academy of Sciences of the Czech Republic, Videnska, Prague
    Brain Res 769:219-24. 1997
    ..We have found earlier that the depolarization-induced release of acetylcholine from the brain could be inhibited by tacrine (tetrahydroaminoacridine) but the mechanism of this action of tacrine was not clarified (S. Tucek, V. Dolezal, J...
  100. ncbi New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease
    P Camps
    Laboratori de Quimica Farmaceutica and Departament de Fisico Quimica, Facultat de Farmacia, Universitat de Barcelona, Av Diagonal 643, E 08028 Barcelona, Spain
    J Med Chem 43:4657-66. 2000
    Several new 12-amino-6,7,10,11-tetrahydro-7, 11-methanocycloocta[b]quinoline derivatives (tacrine-huperzine A hybrids, huprines) have been synthesized and tested as acetylcholinesterase (AChE) inhibitors...
  101. ncbi Combined tacrine and estrogen replacement therapy in patients with Alzheimer's disease
    L S Schneider
    Department of Psychiatry, School of Medicine, Los Angeles, California, USA
    Ann N Y Acad Sci 826:317-22. 1997
    ..possible effects of estrogen replacement therapy (ERT) on clinical response to the cholinesterase inhibitor tacrine in women with Alzheimer's disease (AD)...

Research Grants15

  1. Persistent Attenuation of Cocaine-Reinforced Behavior
    KENNETH W GRASING; Fiscal Year: 2013
    ..Cholinesterase inhibitors such as tacrine increase synaptic levels of ACh by preventing its inactivation by AChE or BuChE, and can improve learning and ..
  2. Tacrine Effects on Cocaine Self-Administration and Pharmacokinetic Measures
    KENNETH W GRASING; Fiscal Year: 2012
    ..Cholinesterase inhibitors such as tacrine increase synaptic levels of ACh by preventing its inactivation by acetylcholinesterase (AChE) or ..
  3. Determining Therapeutic Efficacy of AGE in AD
    Neelima Chauhan; Fiscal Year: 2005
    ..and cholinergic system regulate APP processing, current Alzheimer's therapy targets cholinergic enhancement [Tacrine, Aricept/Donezepil, Rivastigmine, Galantamine]; and regulation of inflammation by NSAIDs [Aspirin, Ibuprofen, ..
  4. MOTOR EFFECTS OF ATYPICAL ANTIPSYCHOTICS
    John Salamone; Fiscal Year: 2003
    ..In addition, clozapine acts to suppress the jaw movements induce by the anticholinesterase tacrine. The suppression of tacrine-induced jaw movements by clozapine occurs at a relatively low dose; clozapine ..
  5. RECEPTOR/G-PROTEIN COUPLING IN ALZHEIMER'S DISEASE
    John Lee; Fiscal Year: 2001
    ..g. bethanechol) or enhance the synaptic availability of acetylcholine (e.g. tacrine, arecept)...
  6. PSYCHOSIS IN ALZHEIMERS DISEASE
    Jason Olin; Fiscal Year: 2000
    ..pathology will enter a 4-week parallel-group, randomized, placebo controlled trial of a cholinesterase inhibitor (tacrine) to test for a differential response in sensitivity. 2...
  7. NEUROMODULATORY ROLES OF MUSCARINIC RECEPTOR SUBTYPES
    P Conn; Fiscal Year: 2000
    ..Furthermore, a compound that inhibits Ach metabolism, termed tacrine, is the only approved treatment for AD...
  8. Pharmacotherapy for Minor Depression
    Robert Howland; Fiscal Year: 2004
    ..The results of this study will have profound public health implications by improving our understanding of the efficacy of SJW and standard antidepressants for the treatment of MinorD. ..
  9. FMRI in Pre-Symptomatic PS1-related Alzheimer's Disease
    John Ringman; Fiscal Year: 2005
    ..UCI, with its strong dementia research program, growing MRI capabilities and opportunity to collaborate at the nearby UCLA Brain Imaging Center, is an excellent environment for this endeavor. ..
  10. SOCIAL FACTORS AND EPIDEMIOLOGY OF COGNITIVE DECLINE
    Marie Florence Shadlen; Fiscal Year: 2005
    ..Hence, these projects will allow Dr Shadlen to achieve her 5-year goal of synthesis of her interests in racial differences, dementia, and epidemiology into an independent, thought-provoking research program. ..
  11. 1H MRSI/Response Inhibition/Methamphetamine Abusers
    JOSEPH O NEILL; Fiscal Year: 2005
    ..This project will examine the chemistry of parts of the brain thought to be responsible for inhibition and/or damaged by methamphetamine in methamphetamine addicts. ..
  12. Ion Channels and Chemicals Controlling Synapse Stability
    Joseph McArdle; Fiscal Year: 2006
    ..The knowledge gained from this research will enlighten future molecular approaches to treating pathologies which afflict children and adults. ..
  13. Magnetic Resonance Spectroscopic Imaging of the Brain in Methamphetamine Abuse
    JOSEPH O NEILL; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  14. NEURAL CIRCUITRY MEDIATING SUCROSE INDUCED ANALGESIA
    Matthew Ennis; Fiscal Year: 2003
    ..This work will lead to a better understanding of neural circuits controlling taste and pain and how these circuits regulate analgesia in newborns. ..
  15. CANDIDATE GENES FOR ALZHEIMER'S DISEASE RISK IN BLACKS
    Rebecca Evans; Fiscal Year: 2005
    ..This career enhancement plan will enable Dr. Evans to develop expertise in patient-oriented research, and help her accomplish her goal of becoming an independent investigator. ..