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 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
  3. doi 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
  4. 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
  5. 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
  6. 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
  7. doi 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 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
  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. doi 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

  1. Determining Therapeutic Efficacy of AGE in AD
    Neelima Chauhan; Fiscal Year: 2005
  2. Determining Therapeutic Efficacy of AGE in AD
    Neelima Chauhan; Fiscal Year: 2004
  3. MOTOR EFFECTS OF ATYPICAL ANTIPSYCHOTICS
    John Salamone; Fiscal Year: 2003
  4. MOTOR EFFECTS OF ATYPICAL ANTIPSYCHOTICS
    John Salamone; Fiscal Year: 2002
  5. MOTOR EFFECTS OF ATYPICAL ANTIPSYCHOTICS
    John Salamone; Fiscal Year: 2001
  6. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATH
    Meenakshi Alreja; Fiscal Year: 2002
  7. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATHWAY
    Meenakshi Alreja; Fiscal Year: 2004
  8. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATHWAY
    Meenakshi Alreja; Fiscal Year: 2005
  9. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATHWAY
    Meenakshi Alreja; Fiscal Year: 2003
  10. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATH
    Meenakshi Alreja; Fiscal Year: 2001

Detail Information

Publications225 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 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...
  3. doi 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 ..
  4. 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 ..
  5. 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...
  6. 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 ..
  7. doi 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 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...
  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. doi 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. doi 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...
  12. 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)...
  13. doi 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...
  14. 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...
  15. 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.
  16. 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...
  17. 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 ..
  18. 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...
  19. 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 (..
  20. 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...
  21. 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...
  22. doi 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...
  23. 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...
  24. 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...
  25. doi 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, ..
  26. doi 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...
  27. 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...
  28. doi 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...
  29. 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) ..
  30. 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]-..
  31. 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...
  32. doi 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 ..
  33. 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 ..
  34. 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...
  35. 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...
  36. 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...
  37. 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...
  38. 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...
  39. 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, ..
  40. doi 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...
  41. 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...
  42. 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 ..
  43. 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...
  44. 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)...
  45. 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...
  46. 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...
  47. 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 ..
  48. doi 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).
  49. 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 ..
  50. 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...
  51. 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...
  52. 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...
  53. 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 ..
  54. 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, ..
  55. 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...
  56. 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...
  57. 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 ..
  58. 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)...
  59. 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.
  60. 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...
  61. 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...
  62. 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...
  63. 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...
  64. 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)...
  65. 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...
  66. 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 ..
  67. 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...
  68. 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...
  69. 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 ..
  70. doi 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...
  71. 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...
  72. 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...
  73. 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...
  74. 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...
  75. 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 ..
  76. 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...
  77. 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...
  78. 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...
  79. ncbi Tacrine interacts with different sites on nicotinic receptor subtypes in SH-SY5Y neuroblastoma and M10 cells
    A L Svensson
    Department of Clinical Neuroscience, Karolinska Institutet, Occupational Therapy and Elderly Care Research, Huddinge University Hospital, Sweden
    Behav Brain Res 113:193-7. 2000
    The effect of chronic treatment with the cholinesterase inhibitor tacrine on nicotinic receptor subtypes was investigated in human SH-SY5Y neuroblastoma cells and in a fibroblast cell line (M10 cells) stably transfected with alpha4beta2 ..
  80. ncbi Cholinesterase inhibition for Alzheimer disease: a meta-analysis of the tacrine trials. Dementia Trialists' Collaboration
    N Qizilbash
    Department of Clinical Geratology, University of Oxford, Radcliffe Infirmary, England
    JAMA 280:1777-82. 1998
    To determine the effects of cholinesterase inhibition with tacrine hydrochloride for the symptoms of Alzheimer disease in terms of cognitive performance, clinical global impression, behavior, and functional autonomy.
  81. 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...
  82. 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...
  83. 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)...
  84. ncbi Effect of histamine on muscimol-induced working memory deficits in radial maze performance
    Yasuko Yamamoto
    Department of Medicinal Pharmacology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama 700 8530, Japan
    J Pharmacol Sci 104:252-7. 2007
    ..On the other hand, no significant effect was observed with reference memory error. Donepezil and tacrine (cholinesterase inhibitors) antagonized the muscimol-induced spatial memory deficits. Histidine (1500 mg/kg, i.p...
  85. ncbi Acetylcholinesterase inhibition in Alzheimer's Disease
    Bernd Ibach
    Memory Disorders Clinic, Gerontopsychiatric and Clinical Pharmacology Research Unit, Department of Psychiatry, University of Regensburg, Bezirksklinikum Regensburg, Germany
    Curr Pharm Des 10:231-51. 2004
    ..This includes donepezil, galanthamine and rivastigmine. Tacrine, the first acetylcholinesterase inhibitor who became available in 1993 as a treatment for AD, does not play an ..
  86. ncbi Alzheimer's disease: will advances made in the past turn the tide?
    Todd P Semla
    Pharmacy Benefits Management and Strategic Health Group, Department of Veterans Affairs, Chicago, IL, USA
    Ann Pharmacother 41:1494-6. 2007
  87. ncbi Cholinesterase inhibitors reduce cortical Abeta in dementia with Lewy bodies
    C G Ballard
    Wolfson Centre for Age Related Diseases, Kings College London, London, UK
    Neurology 68:1726-9. 2007
    ..Treated patients with DLB had significantly less parenchymal Abeta deposition, which is relevant to disease management and treatment of dementia patients using ChEI...
  88. ncbi Effect of anti-dementia drugs on LPS induced neuroinflammation in mice
    Ethika Tyagi
    Division of Pharmacology, Central Drug Research Institute, Lucknow 226001, India
    Life Sci 80:1977-83. 2007
    ..Effect of anti-dementia (Acetylcholinesterase inhibitor) drugs tacrine, rivastigmine and donepezil were studied on neuroinflammation induced by intraperitoneal administration of ..
  89. ncbi The application of evidence-based principles of care in older persons (issue 5): Alzheimer's disease
    Barbara J Zarowitz
    Omnicare, Inc, Covington, KY 48150, USA
    J Am Med Dir Assoc 8:183-93. 2007
  90. ncbi Mechanisms behind the neuroprotective actions of cholinesterase inhibitors in Alzheimer disease
    Agneta Nordberg
    Neurotec Department, Division of Molecular Neuropharmacology, Karolinska Institutet, Karolinska University Hospital, Huddinge, Stockholm, Sweden
    Alzheimer Dis Assoc Disord 20:S12-8. 2006
    ..If such experimental in vitro observations can be extrapolated into clinical neuroprotective properties, AChE inhibitors could positively modulate the disease course of AD...
  91. ncbi Position statement of the American Association for Geriatric Psychiatry regarding principles of care for patients with dementia resulting from Alzheimer disease
    Constantine G Lyketsos
    Am J Geriatr Psychiatry 14:561-72. 2006
  92. ncbi [Mechanisms of neuroprotective effects of therapeutic acetylcholinesterase inhibitors used in treatment of Alzheimer's disease]
    Yuki Takatori
    Department of Pharmacology, Graduate School of Pharmaceutical Sciences, Kyoto University, Japan
    Yakugaku Zasshi 126:607-16. 2006
    Donepezil, galanthamine, and tacrine are therapeutic acetylcholinesterase (AChE) inhibitors used for the treatment of Alzheimer's disease...
  93. ncbi Pharmacological characterization of orally active cholinesterase inhibitory activity of Prunus persica L. Batsch in rats
    Seok Jong Suh
    Department of Biological Sciences, Sungkyunkwan University, Jangan gu, Suwon City, Kyunggi Do 440 746, Korea
    J Mol Neurosci 29:101-7. 2006
    ..of those of selective butyrylcholinesterase inhibitors of 9-amino-1,2,3,4-tetrahydroacridine hydrochloride (tacrine) and tetraidopropylpyrophosphoramide (iso-OMPA) and a selective AChE inhibitor, donepezil, on the cholinesterase ..
  94. ncbi Alzheimer disease and its management: a review
    Malay K Samanta
    Department of Pharmaceutics, J S S College of Pharmacy, Rocklands, Ootacamund 643001, Tamil Nadu, India
    Am J Ther 13:516-26. 2006
    ..This article attempts to focus on some of the important recent developments in understanding and management of Alzheimer disease...
  95. ncbi Clinical pharmacokinetics and pharmacodynamics of cholinesterase inhibitors
    Michael W Jann
    Department of Clinical and Administrative Sciences, Southern School of Pharmacy, Mercer University, Atlanta, Georgia 30341, USA
    Clin Pharmacokinet 41:719-39. 2002
    ..This article presents the latest information on their pharmacokinetic properties and pharmacodynamic activity. Tacrine was the first cholinesterase inhibitor approved by regulatory agencies, followed by donepezil, rivastigmine and ..
  96. ncbi Dual binding site acetylcholinesterase inhibitors: potential new disease-modifying agents for AD
    María Del Monte-Millán
    NeuroPharma, S A, 28760 Tres Cantos, Madrid, Spain
    J Mol Neurosci 30:85-8. 2006
    ....
  97. ncbi Understanding and managing behavioural symptoms in Alzheimer's disease and related dementias: focus on rivastigmine
    Philippe Robert
    Memory Centre UEC, Centre Hospitalier Universitaire de Nice, France
    Curr Med Res Opin 18:156-71. 2002
    ..Differences seen between the agents in terms of efficacy in BPSD, tolerability and safety profiles may be the result of differences in neuropharmacological profiles...
  98. ncbi Evaluation of centrally acting cholinesterase inhibitor exposures in adults
    Keith R McCain
    Arkansas Poison Control Center, Little Rock, AR 72205, USA
    Ann Pharmacother 41:1632-7. 2007
    There are 4 centrally acting cholinesterase inhibitors (CA-ChEI) available in the US: tacrine, galantamine, rivastigmine, and donepezil. Documented clinical experience involving exposure to these agents is limited...
  99. ncbi Evaluation of cholinergic treatment in demented patients by P300 evoked related potentials
    A E Werber
    Department of Neurology, Assaf Harofe Medical Center, Zerifin, Israel
    Neurol Neurochir Pol 35:37-43. 2001
    ..Thirty two patients were treated with ChEls for dementia (tacrine 19, donepezil 5, rivastigmine 8)...
  100. pmc Acetylcholine release by human colon cancer cells mediates autocrine stimulation of cell proliferation
    Kunrong Cheng
    Division of Gastroenterology and Hepatology, Veterans Affairs Maryland Healthcare System, University of Maryland School of Medicine, Department of Pathology, 22 S Greene St, N3W62, Baltimore, MD 21201, USA
    Am J Physiol Gastrointest Liver Physiol 295:G591-7. 2008
    ..005). We conclude that ACh is an autocrine growth factor in colon cancer. Mechanisms that regulate colon epithelial cell production and release of ACh warrant further investigation...
  101. ncbi Diagnosis and treatment of dementia with Lewy bodies
    Stacey Josif
    University of Toledo PA Program, Ohio, USA
    JAAPA 21:22-6. 2008

Research Grants58

  1. 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, ..
  2. Determining Therapeutic Efficacy of AGE in AD
    Neelima Chauhan; Fiscal Year: 2004
    ..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, ..
  3. 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 ..
  4. MOTOR EFFECTS OF ATYPICAL ANTIPSYCHOTICS
    John Salamone; Fiscal Year: 2002
    ..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. MOTOR EFFECTS OF ATYPICAL ANTIPSYCHOTICS
    John Salamone; Fiscal Year: 2001
    ..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 ..
  6. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATH
    Meenakshi Alreja; Fiscal Year: 2002
    ..In contrast, a wide array of AChEIs, including the clinically used tacrine, produce a profound increase in the firing activity of MSDB neurons, which is blocked by Atr/Scop...
  7. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATHWAY
    Meenakshi Alreja; Fiscal Year: 2004
    ..In contrast, a wide array of AChEIs, including the clinically used tacrine, produce a profound increase in the firing activity of MSDB neurons, which is blocked by Atr/Scop...
  8. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATHWAY
    Meenakshi Alreja; Fiscal Year: 2005
    ..In contrast, a wide array of AChEIs, including the clinically used tacrine, produce a profound increase in the firing activity of MSDB neurons, which is blocked by Atr/Scop...
  9. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATHWAY
    Meenakshi Alreja; Fiscal Year: 2003
    ..In contrast, a wide array of AChEIs, including the clinically used tacrine, produce a profound increase in the firing activity of MSDB neurons, which is blocked by Atr/Scop...
  10. CHOLINERGIC & GABAERGIC MECHANISM SEPTOHIPPOCAMPAL PATH
    Meenakshi Alreja; Fiscal Year: 2001
    ..In contrast, a wide array of AChEIs, including the clinically used tacrine, produce a profound increase in the firing activity of MSDB neurons, which is blocked by Atr/Scop...
  11. 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)...
  12. RECEPTOR/G-PROTEIN COUPLING IN ALZHEIMER'S DISEASE
    John Lee; Fiscal Year: 2000
    ..g. bethanechol) or enhance the synaptic availability of acetylcholine (e.g. tacrine, arecept)...
  13. RECEPTOR/G PROTEIN COUPLING IN ALZHEIMER'S DISEASE
    John Lee; Fiscal Year: 1999
    ..g. bethanechol) or enhance the synaptic availability of acetylcholine (e.g. tacrine, arecept)...
  14. CHRONIC CHANGES IN NEUROTRANSMISSION FOLLOWING TBI
    C Dixon; Fiscal Year: 1999
    ..increases in cholinergic tone produced by administration of a cholinesterase inhibitor tetrahydrominoacridine (tacrine) will attenuate behavioral and neurochemical deficits in cholinergic neurotransmission in the hippocampus and ..
  15. Consomic rat panels for pharmacogenomic studies and target identification
    Steven Nye; Fiscal Year: 2006
    ..In this latter case, we will perform testing with tacrine (a commonly used Alzheimer's medication with hepatotoxic side effects) to validate the consomic rat panels ..
  16. PSYCHOSIS IN ALZHEIMERS DISEASE
    Jason Olin; Fiscal Year: 1999
    ..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...
  17. 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...
  18. EFFECT OF DONEPEZIL IN ALZHEIMER'S DISEASE
    Steven Greenberg; Fiscal Year: 1999
    ..27 versus 0.35; p=0.34) or on specific tests of explicit memory or verbal fluency. Contrary to reports with tacrine, the presence of the apolipoprotein Ee4 allele did not predict donepezil treatment failure...
  19. NEUROMODULATORY ROLES OF MUSCARINIC RECEPTOR SUBTYPES
    P Conn; Fiscal Year: 1999
    ..Furthermore, a compound that inhibits Ach metabolism, termed tacrine, is the only approved treatment for AD...
  20. 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...
  21. 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. ..
  22. Pharmacotherapy for Minor Depression
    Robert Howland; Fiscal Year: 2003
    ..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. ..
  23. Pharmacotherapy for Minor Depression
    Robert Howland; Fiscal Year: 2001
    ..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. ..
  24. Pharmacotherapy for Minor Depression
    Robert Howland; Fiscal Year: 2002
    ..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. ..
  25. Cognitive-Behavioral Therapy & Glutametergic Neurometabolites in Pediatric OCD
    JOSEPH O NEILL; Fiscal Year: 2009
    ..This proposal aims for a better understanding of the brain mechanisms of cognitive-behavioral therapy (CBT) in order to develop novel therapies and improve the success of existing therapies. ..
  26. 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. ..
  27. Mechanisms of Cholinesterase Inhibitors on Beta-amyloid
    Debomoy Lahiri; Fiscal Year: 2006
    ..Three FDA- approved drugs (tacrine, donepezil and rivastigmine) for treating AD subjects belong to the category of cholinesterase (ChE) inhibitor (..
  28. Regulation of APP Pathway Gene Promoters in Alzheimer's
    Debomoy Lahiri; Fiscal Year: 2006
    ..Studying APP and BACE gene regulation is crucial to understand APP production leading to Aa generation. These studies should help developing suitable drug targets for the treatment of Alzheimer's disease. ..
  29. Cholinesterase Inhibitors in Alzheimer's Disease
    Debomoy Lahiri; Fiscal Year: 2009
    ..The outcome of the proposal is to identify mechanisms by which ChEIs block potentially toxic AB levels and to utilize this property in developing novel therapeutic agents. ..
  30. Magnetic Resonance Spectroscopic Imaging of the Brain in Methamphetamine Abuse
    JOSEPH O NEILL; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  31. Cognitive-Behavioral Therapy & Glutametergic Neurometabolites in Pediatric OCD
    John C Piacentini; Fiscal Year: 2010
    ..This proposal aims for a better understanding of the brain mechanisms of cognitive-behavioral therapy (CBT) in order to develop novel therapies and improve the success of existing therapies. ..
  32. Regulation of APP Pathway Gene Promoters in Alzheimer's
    Debomoy Lahiri; Fiscal Year: 2007
    ..Studying APP and BACE gene regulation is crucial to understand APP production leading to Aa generation. These studies should help developing suitable drug targets for the treatment of Alzheimer's disease. ..
  33. Cholinesterase Inhibitors in Alzheimer's Disease
    Debomoy K Lahiri; Fiscal Year: 2010
    ..The outcome of the proposal is to identify mechanisms by which ChEIs block potentially toxic AB levels and to utilize this property in developing novel therapeutic agents. ..
  34. Cognitive-Behavioral Therapy & Glutametergic Neurometabolites in Pediatric OCD
    JOSEPH O NEILL; Fiscal Year: 2008
    ..This proposal aims for a better understanding of the brain mechanisms of cognitive-behavioral therapy (CBT) in order to develop novel therapies and improve the success of existing therapies. ..
  35. Cholinesterase Inhibitors in Alzheimer's Disease
    Debomoy Lahiri; Fiscal Year: 2008
    ..The outcome of the proposal is to identify mechanisms by which ChEIs block potentially toxic AB levels and to utilize this property in developing novel therapeutic agents. ..
  36. Regulation of APP Pathway Gene Promoters in Alzheimer's
    Debomoy Lahiri; Fiscal Year: 2008
    ..Studying APP and BACE gene regulation is crucial to understand APP production leading to Aa generation. These studies should help developing suitable drug targets for the treatment of Alzheimer's disease. ..
  37. Cognitive-Behavioral Therapy & Glutametergic Neurometabolites in Pediatric OCD
    John C Piacentini; Fiscal Year: 2010
    ..This proposal aims for a better understanding of the brain mechanisms of cognitive-behavioral therapy (CBT) in order to develop novel therapies and improve the success of existing therapies. ..
  38. Magnetic Resonance Spectroscopic Imaging of the Brain in Methamphetamine Abuse
    JOSEPH O NEILL; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  39. Regulation of APP Pathway Gene Promoters in Alzheimer's
    Debomoy Lahiri; Fiscal Year: 2009
    ..Studying APP and BACE gene regulation is crucial to understand APP production leading to Aa generation. These studies should help developing suitable drug targets for the treatment of Alzheimer's disease. ..
  40. 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. ..
  41. Ion Channels and Chemicals Controlling Synapse Stability
    Joseph McArdle; Fiscal Year: 2005
    ..The knowledge gained from this research will enlighten future molecular approaches to treating pathologies which afflict children and adults. ..
  42. Mechanisms of Cholinesterase Inhibitors on Beta-amyloid
    Debomoy Lahiri; Fiscal Year: 2002
    ..Three FDA- approved drugs (tacrine, donepezil and rivastigmine) for treating AD subjects belong to the category of cholinesterase (ChE) inhibitor (..
  43. APP GENE PROMOTER IN ALZHEIMER'S DISEASE
    Debomoy Lahiri; Fiscal Year: 2002
    ..Understanding the complex interplay between the promoter domains and the transcription factors may suggest novel methods for therapeutic intervention. ..
  44. Ion Channels and Chemicals Controlling Synapse Stability
    Joseph McArdle; Fiscal Year: 2003
    ..The knowledge gained from this research will enlighten future molecular approaches to treating pathologies which afflict children and adults. ..
  45. Mechanisms of Cholinesterase Inhibitors on Beta-amyloid
    Debomoy Lahiri; Fiscal Year: 2003
    ..Three FDA- approved drugs (tacrine, donepezil and rivastigmine) for treating AD subjects belong to the category of cholinesterase (ChE) inhibitor (..
  46. 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. ..
  47. APP GENE PROMOTER IN ALZHEIMER'S DISEASE
    Debomoy Lahiri; Fiscal Year: 2003
    ..Understanding the complex interplay between the promoter domains and the transcription factors may suggest novel methods for therapeutic intervention. ..
  48. Ion Channels and Chemicals Controlling Synapse Stability
    Joseph McArdle; Fiscal Year: 2004
    ..The knowledge gained from this research will enlighten future molecular approaches to treating pathologies which afflict children and adults. ..
  49. Mechanisms of Cholinesterase Inhibitors on Beta-amyloid
    Debomoy Lahiri; Fiscal Year: 2004
    ..Three FDA- approved drugs (tacrine, donepezil and rivastigmine) for treating AD subjects belong to the category of cholinesterase (ChE) inhibitor (..
  50. APP GENE PROMOTER IN ALZHEIMER'S DISEASE
    Debomoy Lahiri; Fiscal Year: 2004
    ..Understanding the complex interplay between the promoter domains and the transcription factors may suggest novel methods for therapeutic intervention. ..
  51. Ion Channels and Chemicals Controlling Synapse Stability
    Joseph McArdle; Fiscal Year: 2005
    ..The knowledge gained from this research will enlighten future molecular approaches to treating pathologies which afflict children and adults. ..
  52. 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. ..
  53. Mechanisms of Cholinesterase Inhibitors on Beta-amyloid
    Debomoy Lahiri; Fiscal Year: 2005
    ..Three FDA- approved drugs (tacrine, donepezil and rivastigmine) for treating AD subjects belong to the category of cholinesterase (ChE) inhibitor (..
  54. 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. ..
  55. Regulation of APP Pathway Gene Promoters in Alzheimer's
    Debomoy Lahiri; Fiscal Year: 2005
    ..Studying APP and BACE gene regulation is crucial to understand APP production leading to Aa generation. These studies should help developing suitable drug targets for the treatment of Alzheimer's disease. ..
  56. 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. ..
  57. APP GENE PROMOTER IN ALZHEIMER'S DISEASE
    Debomoy Lahiri; Fiscal Year: 2001
    ..Understanding the complex interplay between the promoter domains and the transcription factors may suggest novel methods for therapeutic intervention. ..