Page last updated: 2024-09-05

phenserine and physostigmine

phenserine has been researched along with physostigmine in 75 studies

Compound Research Comparison

Studies
(phenserine)
Trials
(phenserine)
Recent Studies (post-2010)
(phenserine)
Studies
(physostigmine)
Trials
(physostigmine)
Recent Studies (post-2010) (physostigmine)
886396,230252331

Protein Interaction Comparison

ProteinTaxonomyphenserine (IC50)physostigmine (IC50)
AcetylcholinesteraseElectrophorus electricus (electric eel)0.1666
AcetylcholinesteraseTetronarce californica (Pacific electric ray)0.3023
CholinesteraseHomo sapiens (human)0.3055
Cytochrome P450 2D6Homo sapiens (human)0.2
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)0.857
AcetylcholinesteraseMus musculus (house mouse)0.0269
AcetylcholinesteraseHomo sapiens (human)0.0853
Acetylcholinesterase Bos taurus (cattle)0.7197
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)0.857
Delta-type opioid receptorMus musculus (house mouse)1.1821
AcetylcholinesteraseGallus gallus (chicken)0.02
AcetylcholinesteraseRattus norvegicus (Norway rat)0.0416
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)0.857
CholinesteraseEquus caballus (horse)0.4081
CholinesteraseMus musculus (house mouse)0.28
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)0.0189
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)0.018
Carboxylic ester hydrolase Equus caballus (horse)1.263

Research

Studies (75)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's10 (13.33)18.2507
2000's31 (41.33)29.6817
2010's29 (38.67)24.3611
2020's5 (6.67)2.80

Authors

AuthorsStudies
Brossi, A1
Brossi, A; Flippen-Anderson, JL; Greig, NH; Hoffman, B; Holloway, HW; Yu, Q1
Brossi, A; Greig, NH; Holloway, HW; Whittaker, NF; Yu, QS; Zhu, X1
Alley, GM; Brossi, A; Deschamps, JR; Greig, NH; Holloway, HW; Kulkarni, SS; Lahiri, DK; Luo, W; Parrish, D; Yu, QS; Zhan, M1
Duncton, MA; Emerling, DE; Kelly, MG; Nguyen, MT; Vincent, F1
Bian, HL; Shan, WG; Wang, JW; Zhan, ZJ1
Chaudhaery, SS; Nath, C; Nazir, A; Roy, KK; Sammi, SR; Saxena, AK; Saxena, G; Shakya, N1
Li, J; Liu, D; Liu, W; Shi, T; Wang, D; Wang, Y; Wang, Z; Yin, G; Zhang, H1
Li, X; Wang, S; Wang, Y; Wang, Z; Zhang, H1
Brossi, A; Greig, NH; Ikari, H; Ingram, DK; Patel, N; Pei, XF; Spangler, EL; Speer, D1
Brossi, A; Garofalo, P; Greig, NH; Heller, B; Iijima, S; Ingram, DK; Spangler, EL1
Brossi, A; Greig, NH; Ingram, DK; Pei, XF; Soncrant, TT1
Acevedo, LD; Davis, KL; Gluck, R; Greig, N; Haroutunian, V; Pei, XF; Utsuki, T; Wallace, WC1
Greig, NH; Ingram, DK; Meyer, RC; Patel, N; Spangler, EL; Yu, QS1
Brossi, A; Greig, NH; Holloway, HW; Yu, Q1
al-Jafari, AA; Alhomida, AS; Greig, NH; Kamal, MA; Perry, ER1
Brossi, A; Greig, NH; Holloway, HW; Utsuki, T; Yu, Q1
Kilbourn, MR; Sherman, PS; Snyder, SE1
Al-Jafari, AA; Alhomida, AS; Greig, NH; Kamal, MA1
Kilbourn, MR; Sherman, PS; Skaddan, MB; Snyder, SE1
Brossi, A; De Micheli, E; Deutsch, J; Greig, NH; Holloway, HW; Ingram, DK; Lahiri, DK; Perry, TA; Soncrant, TT; Utsuki, T; Yu, QS1
Brossi, A; Ge, YW; Greig, NH; Lahiri, DK; Rogers, J; Sambamurti, K; Shaw, KT; Utsuki, T; Yu, QS1
Jewett, DM; Kilbourn, MR; Sherman, PS; Skaddan, MB1
Kilbourn, MR; Koeppe, RA; Ma, B; Moskwa, JE; Sherman, PS1
Huang, A; Kodanko, JJ; Overman, LE1
Cunningham, SC; Devan, BD; Duffy, KB; Greig, NH; Holloway, HW; Ingram, DK; Janas, AM; Markowska, AL; Spangler, EL; Yu, QS1
Bush, AI; Eder, P; Giordano, T; Greig, NH; Lahiri, DK; Rogers, JT; Venti, A1
Araujo, JA; Milgram, NW; Studzinski, CM1
Brossi, A; Bruinsma, GB; Greig, NH; Lahiri, DK; Sambamurti, K; Yu, QS1
Thatte, U1
Brownell, L; Burford, RG; Canfield, CJ; Comer, P; Flanagan, DR; Greig, NH; Holloway, HW; Ruckle, J1
Castro, A; Martinez, A1
Quancard, J; Trost, BM1
Brossi, A; Chen, D; Davidson, D; Giordano, T; Greig, NH; Holloway, HW; Lahiri, DK; Sambamurti, K; Utsuki, T; Yu, QS1
Greig, NH; Holloway, HW; Kamal, MA; Klein, P; Li, Y; Tweedie, D; Yu, QS1
Chen, D; Giordano, T; Greig, NH; Holloway, HW; Lahiri, DK; Maloney, B; Sambamurti, K; Utsuki, T; Yu, QS1
Greig, NH; Holloway, HW; Ingram, DK; Irie, T; Irikura, M; Mamczarz, J; Moriuchi, H; Spangler, EL; Uchimura, N; Utsuki, T; Yu, QS1
Rigby, JH; Sidique, S1
Klein, J1
Alley, GM; Chen, D; Greig, NH; Lahiri, DK; Tweedie, D1
Greig, NH; Marutle, A; Nilbratt, M; Nordberg, A; Ohmitsu, M; Sugaya, K1
Almkvist, O; Andreasen, N; Blennow, K; Engler, H; Forsberg, A; Hagman, G; Kadir, A; Långström, B; Lärksäter, M; Nordberg, A; Wall, A; Winblad, B; Zetterberg, H1
Barak, D; Greig, NH; Ordentlich, A; Shafferman, A; Stein, D; Yu, QS1
Merchant, S; Sugaya, K1
Lahiri, DK; Schneider, LS1
Becker, RE; Bruinsma, G; Friedhoff, LT; Frölich, L; Giacobini, E; Greig, NH; Winblad, B1
Trost, BM; Zhang, Y1
Araujo, JA; de Rivera, C; Greig, NH; Ingram, DK; Milgram, NW; Sandin, J1
Hong, E; Liy-Salmeron, G; Meneses, A; Ponce-Lopez, T1
Chiou, G; Garg, NK; Schammel, AW1
Cardinale, KM; Greig, NH; Hsu, M; Manji, HK; Martinowich, K; Schloesser, RJ1
Becker, RE; Greig, NH2
Garcia, CC; Hognason, K; McArdle, JJ; Potian, JG; Routh, VH; Souayah, N; Sultatos, LG; Thyagarajan, B1
Chang, MY; Greig, NH; John, V; Maccecchini, ML; Pan, C; Zetterberg, H1
Higuchi, K; Kawasaki, T; Matsumoto, K; Narumi, F; Osada, Y; Satoh, M; Shinada, M; Tanaka, H; Yoshida, T1
Reale, M; Tata, AM1
Greig, NH; Holloway, HW; Kamal, MA; Lahiri, DK; Luo, W; Ray, B; Reale, M; Rogers, JT; Sambamurti, K; Yu, QS1
Greig, NH; Li, Y; Lilja, AM; Luo, Y; Marini, AM; Marutle, A; Nordberg, A; Röjdner, J; Yu, QS1
Gonzalez, D; Greig, NH; Lilja, AM; Marutle, A; Mustafiz, T; Nordberg, A; Röjdner, J; Storelli, E; Thomé, CM; Unger-Lithner, C1
Balleidier, A; Bandyopadhyay, S; Cahill, C; Huang, C; Huang, X; Lahiri, DK; Rogers, JT1
Darreh-Shori, T; Hosseini, SM; Nordberg, A1
Chen, C; Chen, J; Greig, NH; He, J; Iskandar, K; Jacobowitz, DM; Marini, AM; McDonough, JH; Pan, H; Piermartiri, T; Wu, W; Yu, QS1
Lilja, AM; Malmsten, L; Marutle, A; Nordberg, A; Ögren, SO; Röjdner, J; Verkhratsky, A; Voytenko, L1
Almkvist, O; Andreasen, N; Kadir, A; Långström, B; Nordberg, A; Wall, A; Zetterberg, H1
Barak, S; Becker, KG; Becker, RE; Fukui, K; Greig, NH; Hoffer, BJ; Holloway, HW; Lehrmann, E; Li, Y; Luo, Y; Perez, E; Pick, CG; Rubovitch, V; Tamargo, IA; Tweedie, D; Van Praag, H; Wood, WH; Yu, QS; Zhang, Y1
Becker, RE; Chiang, YH; Greig, NH; Hoffer, BJ; Hoffer, ME; Pick, CG1
Becker, RE; Chang, CF; Chen, KY; Chen, YH; Chiang, YH; Greig, NH; Kang, SJ; Lai, JH; Luo, Y; Wu, JC1
Aarsland, D; Ballard, C; Becker, RE; Bledsoe, J; Ferrucci, L; Flanagan, D; Govindarajan, R; Greig, NH; Kapogiannis, D; Lahiri, DK; Majercik, S; Sano, M; Schneider, LS1
Barnett, A; Casey, A; Greig, NH; Jin, Y; Kim, P; Luo, Y; Scerba, M; Selman, W; Turcato, F1
Damanhouri, GA; Tabrez, S1
Bader, M; Becker, RE; Greig, NH; Hoffer, BJ; Hoffman, AF; Hsueh, SC; Jung, YJ; Lecca, D; Lupica, CR; Pick, CG; Tweedie, D1
Becker, RE; Chiang, YH; Glotfelty, EJ; Greig, NH; Hoffer, BJ; Hsueh, SC; Kapogiannis, D; Lecca, D; Nogueras-Ortiz, C; Tweedie, D1
Chen, XQ; Kleschevnikov, AM; Maccecchini, M; Mobley, WC; Nguyen, PD; Overk, C; Pearn, ML; Salehi, A1
Greven, NJ; Hiller, W; Kaiser, M; Kruth, S; Nett, M; Pietruszka, J; Schneider, P; Winand, L1

Reviews

12 review(s) available for phenserine and physostigmine

ArticleYear
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
    Journal of medicinal chemistry, 1990, Volume: 33, Issue:9

    Topics: Animals; Chemical Phenomena; Chemistry; Colchicine; Humans; Physostigmine

1990
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
    European journal of medicinal chemistry, 2022, Oct-05, Volume: 240

    Topics: Aged; Alzheimer Disease; Carbamates; Cholinesterase Inhibitors; Humans; Ligands

2022
Phenserine and ring C hetero-analogues: drug candidates for the treatment of Alzheimer's disease.
    Medicinal research reviews, 1995, Volume: 15, Issue:1

    Topics: Alzheimer Disease; Animals; Cholinesterase Inhibitors; Humans; Physostigmine; Rats; Structure-Activity Relationship

1995
Further evidence for the cholinergic hypothesis of aging and dementia from the canine model of aging.
    Progress in neuro-psychopharmacology & biological psychiatry, 2005, Volume: 29, Issue:3

    Topics: Acetylcholine; Aging; Animals; Cognition Disorders; Dementia; Disease Models, Animal; Dogs; Humans; Physostigmine; Scopolamine

2005
An overview of phenserine tartrate, a novel acetylcholinesterase inhibitor for the treatment of Alzheimer's disease.
    Current Alzheimer research, 2005, Volume: 2, Issue:3

    Topics: Alzheimer Disease; Animals; Cholinesterase Inhibitors; Humans; Physostigmine; Tartrates

2005
Phenserine Axonyx.
    Current opinion in investigational drugs (London, England : 2000), 2005, Volume: 6, Issue:7

    Topics: Alzheimer Disease; Animals; Cholinesterase Inhibitors; Clinical Trials as Topic; Humans; Molecular Structure; Physostigmine

2005
Novel cholinesterase inhibitors as future effective drugs for the treatment of Alzheimer's disease.
    Expert opinion on investigational drugs, 2006, Volume: 15, Issue:1

    Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Animals; Butyrylcholinesterase; Carbamates; Cholinesterase Inhibitors; Clinical Trials as Topic; Drug Delivery Systems; Drug Evaluation, Preclinical; Galantamine; Humans; Physostigmine; Protein Conformation

2006
Phenserine.
    Expert opinion on investigational drugs, 2007, Volume: 16, Issue:7

    Topics: Alzheimer Disease; Animals; Clinical Trials, Phase II as Topic; Disease Models, Animal; Dogs; Dose-Response Relationship, Drug; Drug Administration Schedule; Drugs, Investigational; Female; Follow-Up Studies; Humans; Male; Maximum Tolerated Dose; Mice; Physostigmine; Risk Assessment; Sensitivity and Specificity; Treatment Outcome

2007
How to approach Alzheimer's disease therapy using stem cell technologies.
    Journal of Alzheimer's disease : JAD, 2008, Volume: 15, Issue:2

    Topics: Alzheimer Disease; Amyloid beta-Protein Precursor; Animals; Cell Differentiation; Cell Proliferation; Cholinesterase Inhibitors; Cognition; Humans; Mice; Neurons; Physostigmine; Rats; Stem Cell Transplantation; Stem Cells

2008
Repositioning drugs for traumatic brain injury - N-acetyl cysteine and Phenserine.
    Journal of biomedical science, 2017, Sep-09, Volume: 24, Issue:1

    Topics: Acetylcysteine; Animals; Anti-Inflammatory Agents; Brain Injuries, Traumatic; Cholinesterase Inhibitors; Drug Repositioning; Humans; Mice; Physostigmine; Psychotropic Drugs; Rats

2017
(-)-Phenserine and Inhibiting Pre-Programmed Cell Death: In Pursuit of a Novel Intervention for Alzheimer's Disease.
    Current Alzheimer research, 2018, Volume: 15, Issue:9

    Topics: Alzheimer Disease; Animals; Cell Death; Cholinesterase Inhibitors; Humans; Physostigmine

2018
(-)-Phenserine tartrate (PhenT) as a treatment for traumatic brain injury.
    CNS neuroscience & therapeutics, 2020, Volume: 26, Issue:6

    Topics: Animals; Brain Injuries, Traumatic; Cell Survival; Humans; Mice; Mice, Transgenic; Neuroprotective Agents; Physostigmine; Tartrates; Treatment Outcome

2020

Trials

6 trial(s) available for phenserine and physostigmine

ArticleYear
Anticholinesterase and pharmacokinetic profile of phenserine in healthy elderly human subjects.
    Current Alzheimer research, 2005, Volume: 2, Issue:4

    Topics: Acetylcholinesterase; Aged; Area Under Curve; Cholinesterase Inhibitors; Erythrocytes; Female; Humans; Male; Maximum Tolerated Dose; Middle Aged; Physostigmine

2005
Effect of phenserine treatment on brain functional activity and amyloid in Alzheimer's disease.
    Annals of neurology, 2008, Volume: 63, Issue:5

    Topics: Aged; Alzheimer Disease; Amyloid; Brain; Cholinesterase Inhibitors; Double-Blind Method; Female; Humans; Male; Physostigmine; Placebo Effect; Positron-Emission Tomography; Treatment Outcome

2008
Phenserine efficacy in Alzheimer's disease.
    Journal of Alzheimer's disease : JAD, 2010, Volume: 22, Issue:4

    Topics: Aged; Aged, 80 and over; Alzheimer Disease; Analysis of Variance; Cholinesterase Inhibitors; Double-Blind Method; Female; Humans; Male; Middle Aged; Physostigmine; Treatment Outcome

2010
Posiphen as a candidate drug to lower CSF amyloid precursor protein, amyloid-β peptide and τ levels: target engagement, tolerability and pharmacokinetics in humans.
    Journal of neurology, neurosurgery, and psychiatry, 2012, Volume: 83, Issue:9

    Topics: Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Animals; Cognitive Dysfunction; Dose-Response Relationship, Drug; Double-Blind Method; Female; Humans; Inflammation Mediators; Male; Peptide Fragments; Physostigmine; Rats; Rats, Inbred F344; tau Proteins

2012
Pharmacodynamics of cholinesterase inhibitors suggests add-on therapy with a low-dose carbamylating inhibitor in patients on long-term treatment with rapidly reversible inhibitors.
    Journal of Alzheimer's disease : JAD, 2014, Volume: 39, Issue:2

    Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Benzothiazoles; Blotting, Western; Butyrylcholinesterase; Cholinesterase Inhibitors; Donepezil; Double-Blind Method; Drug Therapy, Combination; Fluorescence; Follow-Up Studies; Humans; Indans; Physostigmine; Piperidines; Thiazoles; Time Factors

2014
Correlations between Alzheimer's Disease Cerebrospinal Fluid Biomarkers and Cerebral Glucose Metabolism after 12 Months of Phenserine Treatment.
    Journal of Alzheimer's disease : JAD, 2015, Volume: 47, Issue:3

    Topics: Aged; Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Biomarkers; Brain; Cognition; Double-Blind Method; Female; Glucose; Humans; Male; Nootropic Agents; Peptide Fragments; Phosphorylation; Physostigmine; Positron-Emission Tomography; tau Proteins; Time Factors; Treatment Outcome

2015

Other Studies

57 other study(ies) available for phenserine and physostigmine

ArticleYear
Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.
    Journal of medicinal chemistry, 2001, Nov-22, Volume: 44, Issue:24

    Topics: Acetylcholinesterase; Butyrylcholinesterase; Carbamates; Cholinesterase Inhibitors; Crystallography, X-Ray; Erythrocytes; Humans; Models, Molecular; Molecular Conformation; Physostigmine; Structure-Activity Relationship

2001
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
    Journal of medicinal chemistry, 2002, Aug-15, Volume: 45, Issue:17

    Topics: Acetylcholinesterase; Alkaloids; Butyrylcholinesterase; Cholinesterase Inhibitors; Cyclic N-Oxides; Humans; Isomerism; Oxazines; Structure-Activity Relationship

2002
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
    Journal of medicinal chemistry, 2005, Feb-24, Volume: 48, Issue:4

    Topics: Acetylcholinesterase; Amyloid beta-Protein Precursor; Benzofurans; Butyrylcholinesterase; Carbamates; Cell Line; Cell Survival; Cholinesterase Inhibitors; Crystallography, X-Ray; Humans; Models, Molecular; Molecular Structure; Neurons; Oxepins; Structure-Activity Relationship

2005
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
    Bioorganic & medicinal chemistry letters, 2009, Dec-01, Volume: 19, Issue:23

    Topics: Amidohydrolases; Carbamates; Dose-Response Relationship, Drug; Drug Design; Enzyme Inhibitors; Humans; Models, Molecular; Molecular Structure; Piperazines; Stereoisomerism; Structure-Activity Relationship

2009
Synthesis of physostigmine analogues and evaluation of their anticholinesterase activities.
    Bioorganic & medicinal chemistry letters, 2010, Mar-01, Volume: 20, Issue:5

    Topics: Acetylcholinesterase; Animals; Butyrylcholinesterase; Cholinesterase Inhibitors; Indoles; Neurotransmitter Agents; Physostigmine; Rats; Structure-Activity Relationship

2010
Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based virtual screening, synthesis, and pharmacology.
    Journal of medicinal chemistry, 2010, Sep-09, Volume: 53, Issue:17

    Topics: Acetylcholinesterase; Administration, Oral; Animals; Avoidance Learning; Caenorhabditis elegans; Carbamates; Catalytic Domain; Cholinesterase Inhibitors; Databases, Factual; Hydrogen Bonding; Hydrophobic and Hydrophilic Interactions; Male; Mice; Models, Molecular; Nootropic Agents; Quantitative Structure-Activity Relationship; Scopolamine

2010
Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease.
    European journal of medicinal chemistry, 2022, Feb-05, Volume: 229

    Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Animals; Binding Sites; Blood-Brain Barrier; Butyrylcholinesterase; Carbamates; Cholinesterase Inhibitors; Drug Design; Humans; Male; Maze Learning; Molecular Docking Simulation; Neuroprotective Agents; Protein Aggregates; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Tryptamines

2022
Maze learning in aged rats is enhanced by phenserine, a novel anticholinesterase.
    Neuroreport, 1995, Feb-15, Volume: 6, Issue:3

    Topics: Aging; Animals; Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Male; Maze Learning; Memory; Physostigmine; Rats; Rats, Inbred F344

1995
Phenserine: a physostigmine derivative that is a long-acting inhibitor of cholinesterase and demonstrates a wide dose range for attenuating a scopolamine-induced learning impairment of rats in a 14-unit T-maze.
    Psychopharmacology, 1993, Volume: 112, Issue:4

    Topics: Acetylcholinesterase; Animals; Avoidance Learning; Cholinesterase Inhibitors; Electroshock; Male; Maze Learning; Physostigmine; Rats; Rats, Inbred F344; Scopolamine

1993
Pharmacological modulation of Alzheimer's beta-amyloid precursor protein levels in the CSF of rats with forebrain cholinergic system lesions.
    Brain research. Molecular brain research, 1997, Volume: 46, Issue:1-2

    Topics: Alzheimer Disease; Amyloid beta-Protein Precursor; Animals; Cholinesterase Inhibitors; Isoflurophate; Male; Muscarinic Antagonists; Physostigmine; Prosencephalon; Rats; Rats, Sprague-Dawley; Scopolamine

1997
Phenserine, a novel acetylcholinesterase inhibitor, attenuates impaired learning of rats in a 14-unit T-maze induced by blockade of the N-methyl-D-aspartate receptor.
    Neuroreport, 1998, Jan-05, Volume: 9, Issue:1

    Topics: Animals; Cholinesterase Inhibitors; Excitatory Amino Acid Antagonists; Learning Disabilities; Male; Maze Learning; Physostigmine; Piperazines; Rats; Rats, Inbred F344; Receptors, N-Methyl-D-Aspartate

1998
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.
    Journal of medicinal chemistry, 1998, Jun-18, Volume: 41, Issue:13

    Topics: Acetylcholinesterase; Butyrylcholinesterase; Carbamates; Cholinesterase Inhibitors; Erythrocytes; Humans; Hydrolysis; In Vitro Techniques; Indoles; Oxidation-Reduction; Phenylcarbamates; Physostigmine; Stereoisomerism; Structure-Activity Relationship

1998
Kinetics of human erythrocyte acetylcholinesterase inhibition by a novel derivative of physostigmine: phenserine.
    Biochemical and biophysical research communications, 1998, Jul-09, Volume: 248, Issue:1

    Topics: Acetylcholinesterase; Acetylthiocholine; Cholinesterase Inhibitors; Erythrocytes; Humans; Kinetics; Male; Physostigmine

1998
Synthesis of novel phenserine-based-selective inhibitors of butyrylcholinesterase for Alzheimer's disease.
    Journal of medicinal chemistry, 1999, May-20, Volume: 42, Issue:10

    Topics: Acetylcholinesterase; Alzheimer Disease; Butyrylcholinesterase; Cholinesterase Inhibitors; Erythrocytes; Humans; Physostigmine; Structure-Activity Relationship

1999
Simplified methods for in vivo measurement of acetylcholinesterase activity in rodent brain.
    Nuclear medicine and biology, 1999, Volume: 26, Issue:5

    Topics: Acetylcholinesterase; Animals; Brain; Carbon Radioisotopes; Female; Kinetics; Mice; Neostigmine; Physostigmine; Piperidines; Reproducibility of Results; Tissue Distribution

1999
Kinetics of human acetylcholinesterase inhibition by the novel experimental Alzheimer therapeutic agent, tolserine.
    Biochemical pharmacology, 2000, Aug-15, Volume: 60, Issue:4

    Topics: Acetylcholinesterase; Alzheimer Disease; Binding, Competitive; Cholinesterase Inhibitors; Humans; Kinetics; Physostigmine

2000
Acetylcholinesterase inhibition increases in vivo N-(2-[18F]fluoroethyl)-4-piperidyl benzilate binding to muscarinic acetylcholine receptors.
    Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 2001, Volume: 21, Issue:2

    Topics: Acetylcholine; Animals; Benzilates; Brain; Cerebellum; Cerebral Cortex; Cholinesterase Inhibitors; Corpus Striatum; Fluorine Radioisotopes; Hypothalamus; Male; Muscarinic Antagonists; Physostigmine; Piperidines; Rats; Receptors, Muscarinic

2001
The experimental Alzheimer drug phenserine: preclinical pharmacokinetics and pharmacodynamics.
    Acta neurologica Scandinavica. Supplementum, 2000, Volume: 176

    Topics: Administration, Oral; Alzheimer Disease; Animals; Brain; Cholinesterase Inhibitors; Disease Models, Animal; Half-Life; Infusions, Intravenous; Male; Physostigmine; Rats; Rats, Inbred F344; Tacrine

2000
Phenserine regulates translation of beta -amyloid precursor protein mRNA by a putative interleukin-1 responsive element, a target for drug development.
    Proceedings of the National Academy of Sciences of the United States of America, 2001, Jun-19, Volume: 98, Issue:13

    Topics: 5' Untranslated Regions; Amyloid beta-Protein Precursor; Astrocytoma; Cell Survival; Chloramphenicol O-Acetyltransferase; Cholinesterase Inhibitors; Chromones; Culture Media, Conditioned; Drug Design; Enzyme Inhibitors; Flavonoids; Gene Expression Regulation; Humans; Interleukin-1; L-Lactate Dehydrogenase; Mitogen-Activated Protein Kinases; Morpholines; Neuroblastoma; Phosphatidylinositol 3-Kinases; Physostigmine; Protein Biosynthesis; Recombinant Proteins; RNA, Messenger; Transfection; Tumor Cells, Cultured

2001
(R)-N-[11C]methyl-3-pyrrolidyl benzilate, a high-affinity reversible radioligand for PET studies of the muscarinic acetylcholine receptor.
    Synapse (New York, N.Y.), 2002, Volume: 45, Issue:1

    Topics: Animals; Benzilates; Binding, Competitive; Brain; Carbon Radioisotopes; Cholinesterase Inhibitors; Female; Ligands; Macaca nemestrina; Male; Mice; Mice, Inbred Strains; Physostigmine; Piperidines; Pyrrolidines; Radioactive Tracers; Rats; Receptors, Muscarinic; Tissue Distribution; Tomography, Emission-Computed

2002
Sensitivity of [11C]N-methylpyrrolidinyl benzilate ([11C]NMPYB) to endogenous acetylcholine: PET imaging vs tissue sampling methods.
    Nuclear medicine and biology, 2004, Volume: 31, Issue:4

    Topics: Acetylcholine; Animals; Benzilates; Brain; Isotope Labeling; Male; Physostigmine; Pyrrolidines; Radiopharmaceuticals; Rats; Reproducibility of Results; Sensitivity and Specificity; Tissue Distribution; Tomography, Emission-Computed

2004
Asymmetric synthesis of pyrrolidinoindolines. Application for the practical total synthesis of (-)-phenserine.
    Journal of the American Chemical Society, 2004, Nov-03, Volume: 126, Issue:43

    Topics: Alkylation; Indoles; Physostigmine; Pyrrolidines; Stereoisomerism

2004
The cholinesterase inhibitor, phenserine, improves Morris water maze performance of scopolamine-treated rats.
    Life sciences, 2005, Jan-21, Volume: 76, Issue:10

    Topics: Animals; Cholinesterase Inhibitors; Male; Maze Learning; Physostigmine; Rats; Rats, Inbred F344; Scopolamine

2005
The integrated role of desferrioxamine and phenserine targeted to an iron-responsive element in the APP-mRNA 5'-untranslated region.
    Annals of the New York Academy of Sciences, 2004, Volume: 1035

    Topics: 5' Untranslated Regions; Amyloid beta-Protein Precursor; Cell Line, Tumor; Cholinesterase Inhibitors; Deferoxamine; Dose-Response Relationship, Drug; Gene Expression Regulation; Humans; Neuroblastoma; Physostigmine; RNA, Messenger; Siderophores; Transfection

2004
Palladium-catalyzed enantioselective C-3 allylation of 3-substituted-1H-indoles using trialkylboranes.
    Journal of the American Chemical Society, 2006, May-17, Volume: 128, Issue:19

    Topics: Alkenes; Boranes; Catalysis; Indoles; Palladium; Physostigmine; Stereoisomerism

2006
Identification of novel small molecule inhibitors of amyloid precursor protein synthesis as a route to lower Alzheimer's disease amyloid-beta peptide.
    The Journal of pharmacology and experimental therapeutics, 2006, Volume: 318, Issue:2

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Animals; Blotting, Western; Cell Line, Tumor; Cell Survival; Cholinesterase Inhibitors; Drug Evaluation, Preclinical; Enzyme-Linked Immunosorbent Assay; Extracellular Space; Humans; Male; Mice; Mice, Inbred C57BL; Nerve Tissue Proteins; Neuroprotective Agents; Physostigmine; RNA, Messenger; Stereoisomerism; Structure-Activity Relationship

2006
Kinetics of human serum butyrylcholinesterase and its inhibition by a novel experimental Alzheimer therapeutic, bisnorcymserine.
    Journal of Alzheimer's disease : JAD, 2006, Volume: 10, Issue:1

    Topics: Alzheimer Disease; Amyloid beta-Protein Precursor; Brain; Butyrylcholinesterase; Cholinesterase Inhibitors; Humans; Physostigmine; Time Factors

2006
The experimental Alzheimer's disease drug posiphen [(+)-phenserine] lowers amyloid-beta peptide levels in cell culture and mice.
    The Journal of pharmacology and experimental therapeutics, 2007, Volume: 320, Issue:1

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Amyloid Precursor Protein Secretases; Animals; Cell Line, Tumor; Cerebral Cortex; Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Humans; Male; Mice; Mice, Inbred C57BL; Physostigmine; RNA, Messenger; Stereoisomerism

2007
Preclinical investigation of the topical administration of phenserine: transdermal flux, cholinesterase inhibition, and cognitive efficacy.
    The Journal of pharmacology and experimental therapeutics, 2007, Volume: 321, Issue:1

    Topics: Acetylcholinesterase; Administration, Cutaneous; Animals; Avoidance Learning; Butyrylcholinesterase; Cerebral Cortex; Chemistry, Pharmaceutical; Cholinesterase Inhibitors; Cognition; Diffusion Chambers, Culture; Electroshock; Excipients; Male; Muscarinic Antagonists; Ointments; Physostigmine; Rats; Rats, Inbred F344; Scopolamine; Skin Absorption

2007
Total synthesis of (+/-) -phenserine via [4+1] cyclization of a bis(alkylthio)carbene and an indole isocyanate.
    Organic letters, 2007, Mar-29, Volume: 9, Issue:7

    Topics: Cyclization; Hydrocarbons; Indoles; Isocyanates; Methane; Molecular Structure; Physostigmine; Sulfides

2007
Differential effects of two hexahydropyrroloindole carbamate-based anticholinesterase drugs on the amyloid beta protein pathway involved in Alzheimer's disease.
    Neuromolecular medicine, 2007, Volume: 9, Issue:2

    Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Butyrylcholinesterase; Carbamates; Cell Line; Cell Survival; Cholinesterase Inhibitors; Humans; Indoles; Molecular Structure; Neurons; Physostigmine; Pyrroles

2007
Modulation of human neural stem cell differentiation in Alzheimer (APP23) transgenic mice by phenserine.
    Proceedings of the National Academy of Sciences of the United States of America, 2007, Jul-24, Volume: 104, Issue:30

    Topics: Alzheimer Disease; Amyloid; Animals; Cell Differentiation; Cells, Cultured; Gene Expression Regulation; Glial Fibrillary Acidic Protein; Humans; Mice; Mice, Transgenic; Neuroglia; Neurons; Physostigmine; Stem Cell Transplantation; Stem Cells

2007
Accommodation of physostigmine and its analogues by acetylcholinesterase is dominated by hydrophobic interactions.
    The Biochemical journal, 2009, Jan-01, Volume: 417, Issue:1

    Topics: Acetylcholinesterase; Binding Sites; Catalysis; Cholinesterase Inhibitors; Humans; Hydrophobic and Hydrophilic Interactions; Kinetics; Models, Molecular; Molecular Structure; Mutation; Phenylcarbamates; Physostigmine; Protein Binding; Pyridostigmine Bromide; Rivastigmine; Structure-Activity Relationship

2009
The perils of Alzheimer's drug development.
    Current Alzheimer research, 2009, Volume: 6, Issue:1

    Topics: Alzheimer Disease; Animals; Biomedical Research; Clinical Trials as Topic; Data Interpretation, Statistical; Dose-Response Relationship, Drug; Drug Evaluation; Drug Industry; Humans; Observer Variation; Physostigmine; Selection Bias

2009
Molybdenum-catalyzed asymmetric allylic alkylation of 3-alkyloxindoles: reaction development and applications.
    Chemistry (Weinheim an der Bergstrasse, Germany), 2011, Mar-01, Volume: 17, Issue:10

    Topics: Alkaloids; Alkylation; Catalysis; Heterocyclic Compounds, 4 or More Rings; Hydrocarbons, Halogenated; Indoles; Molecular Structure; Molybdenum; Oxindoles; Physostigmine; Stereoisomerism

2011
Cholinesterase inhibitors improve both memory and complex learning in aged beagle dogs.
    Journal of Alzheimer's disease : JAD, 2011, Volume: 26, Issue:1

    Topics: Aging; Analysis of Variance; Animals; Behavior, Animal; Cholinergic Antagonists; Cholinesterase Inhibitors; Discrimination, Psychological; Disease Models, Animal; Dogs; Donepezil; Dose-Response Relationship, Drug; Female; Follow-Up Studies; Indans; Learning Disabilities; Male; Memory Disorders; Neuropsychological Tests; Odorants; Physostigmine; Piperidines; Scopolamine

2011
Lithium, phenserine, memantine and pioglitazone reverse memory deficit and restore phospho-GSK3β decreased in hippocampus in intracerebroventricular streptozotocin induced memory deficit model.
    Brain research, 2011, Dec-02, Volume: 1426

    Topics: Animals; Conditioning, Classical; Disease Models, Animal; Enzyme Inhibitors; Glycogen Synthase Kinase 3; Hippocampus; Hypoglycemic Agents; Infusions, Intraventricular; Lithium; Male; Memantine; Memory Disorders; Neuroprotective Agents; Physostigmine; Pioglitazone; Prefrontal Cortex; Rats; Rats, Wistar; Statistics, Nonparametric; Streptozocin; Thiazolidinediones

2011
Synthesis of (+)-phenserine using an interrupted Fischer indolization reaction.
    The Journal of organic chemistry, 2012, Jan-06, Volume: 77, Issue:1

    Topics: Alzheimer Disease; Cholinesterase Inhibitors; Indoles; Molecular Structure; Physostigmine; Pyrrolidines; Stereoisomerism

2012
Acetylcholinesterase inhibition ameliorates deficits in motivational drive.
    Behavioral and brain functions : BBF, 2012, Mar-20, Volume: 8

    Topics: Anhedonia; Animals; Anxiety; Behavior, Animal; Body Weight; Cholinesterase Inhibitors; Chronic Disease; Drive; Habituation, Psychophysiologic; Hindlimb Suspension; Image Processing, Computer-Assisted; Immunohistochemistry; Male; Mice; Mice, Inbred C57BL; Motivation; Nervous System; Phenotype; Physostigmine; Proto-Oncogene Proteins c-fos; Quinine; Restraint, Physical; Stress, Psychological; Swimming; Taste

2012
Fire in the ashes: can failed Alzheimer's disease drugs succeed with second chances?
    Alzheimer's & dementia : the journal of the Alzheimer's Association, 2013, Volume: 9, Issue:1

    Topics: Alzheimer Disease; Animals; Cholinesterase Inhibitors; Clinical Trials as Topic; Humans; Physostigmine; Research Design; Treatment Failure

2013
Acetylcholinesterase deficiency contributes to neuromuscular junction dysfunction in type 1 diabetic neuropathy.
    American journal of physiology. Endocrinology and metabolism, 2012, Aug-15, Volume: 303, Issue:4

    Topics: Acetylcholinesterase; Animals; Butyrylcholinesterase; Cholinesterase Inhibitors; Diabetes Mellitus, Experimental; Diabetes Mellitus, Type 1; Diabetic Neuropathies; GPI-Linked Proteins; Hyperglycemia; Male; Mice; Motor Endplate; Muscle Weakness; Neuromuscular Junction Diseases; Physostigmine

2012
Synthesis of phenserine analogues and evaluation of their cholinesterase inhibitory activities.
    Bioorganic & medicinal chemistry, 2012, Aug-15, Volume: 20, Issue:16

    Topics: Acetylcholinesterase; Animals; Brain; Butyrylcholinesterase; Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Molecular Structure; Physostigmine; Rats; Structure-Activity Relationship

2012
Was phenserine a failure or were investigators mislead by methods?
    Current Alzheimer research, 2012, Volume: 9, Issue:10

    Topics: Alzheimer Disease; Cholinesterase Inhibitors; Clinical Trials, Phase III as Topic; Humans; MEDLINE; Physostigmine; Randomized Controlled Trials as Topic; Research Design; Treatment Failure

2012
Editorial (hot topic:modulation of cholinergic system activity in neuronal and non-neuronal tissues: therapeutic implications).
    Anti-inflammatory & anti-allergy agents in medicinal chemistry, 2013, Volume: 12, Issue:2

    Topics: Acetylcholine; Alzheimer Disease; Butyrylcholinesterase; Cholinergic Agents; Humans; Inflammation; MicroRNAs; Physostigmine

2013
Synthesis of the Alzheimer drug Posiphen into its primary metabolic products (+)-N1-norPosiphen, (+)-N8-norPosiphen and (+)-N1, N8-bisnorPosiphen, their inhibition of amyloid precursor protein, α-Synuclein synthesis, interleukin-1β release, and cholinergi
    Anti-inflammatory & anti-allergy agents in medicinal chemistry, 2013, Volume: 12, Issue:2

    Topics: alpha-Synuclein; Alzheimer Disease; Amyloid beta-Protein Precursor; Humans; Interleukin-1beta; Physostigmine; Plaque, Amyloid; Receptors, Muscarinic; Receptors, Nicotinic; Stereoisomerism

2013
Neurotrophic and neuroprotective actions of (-)- and (+)-phenserine, candidate drugs for Alzheimer's disease.
    PloS one, 2013, Volume: 8, Issue:1

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Animals; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Doublecortin Protein; Drug Discovery; Gene Expression Regulation; Humans; Mice; Mice, Transgenic; Mutation; Neural Stem Cells; Neurons; Neuroprotective Agents; Oxidative Stress; Peptide Fragments; Physostigmine; Stereoisomerism

2013
Age-dependent neuroplasticity mechanisms in Alzheimer Tg2576 mice following modulation of brain amyloid-β levels.
    PloS one, 2013, Volume: 8, Issue:3

    Topics: Age Factors; Alzheimer Disease; Amyloid beta-Peptides; Animals; Brain; Cell Proliferation; Disease Models, Animal; Doublecortin Protein; Female; Hippocampus; Interleukin-1beta; Male; Mice; Mice, Transgenic; Neuronal Plasticity; Neurons; Physostigmine; Plaque, Amyloid; Synapses; Tumor Necrosis Factor-alpha

2013
Novel 5' untranslated region directed blockers of iron-regulatory protein-1 dependent amyloid precursor protein translation: implications for down syndrome and Alzheimer's disease.
    PloS one, 2013, Volume: 8, Issue:7

    Topics: 5' Untranslated Regions; alpha-Synuclein; Alzheimer Disease; Amyloid beta-Protein Precursor; Aniline Compounds; Animals; Base Sequence; Benzimidazoles; Blotting, Western; Cell Line, Tumor; Cell Survival; Cells, Cultured; Down Syndrome; Humans; Iron; Iron Regulatory Protein 1; Mice; Mice, Transgenic; Molecular Sequence Data; Neurons; Physostigmine; Protein Binding; Protein Biosynthesis; Response Elements; RNA, Messenger; Sequence Homology, Nucleic Acid

2013
(-)-Phenserine attenuates soman-induced neuropathology.
    PloS one, 2014, Volume: 9, Issue:6

    Topics: Animals; Carrier Proteins; Chemical Warfare Agents; Cholinesterase Inhibitors; Gene Expression Regulation; Homer Scaffolding Proteins; Male; Physostigmine; Rats; Rats, Sprague-Dawley; Soman; Status Epilepticus

2014
Neural Stem Cell Transplant-Induced Effect on Neurogenesis and Cognition in Alzheimer Tg2576 Mice Is Inhibited by Concomitant Treatment with Amyloid-Lowering or Cholinergic α7 Nicotinic Receptor Drugs.
    Neural plasticity, 2015, Volume: 2015

    Topics: alpha7 Nicotinic Acetylcholine Receptor; Alzheimer Disease; Amyloid beta-Peptides; Animals; Astrocytes; Carbamates; Cell Proliferation; Cognition; Doublecortin Protein; Female; Hippocampus; Humans; Male; Maze Learning; Memory; Mice; Nerve Regeneration; Neural Stem Cells; Neurogenesis; Nicotinic Agonists; Physostigmine; Quinuclidines; Stem Cell Transplantation

2015
Cognitive Impairments Induced by Concussive Mild Traumatic Brain Injury in Mouse Are Ameliorated by Treatment with Phenserine via Multiple Non-Cholinergic and Cholinergic Mechanisms.
    PloS one, 2016, Volume: 11, Issue:6

    Topics: Animals; Brain Concussion; Cholinergic Agents; Cholinesterase Inhibitors; Cognitive Dysfunction; Disease Models, Animal; Gene Expression Regulation; Glutamic Acid; Hippocampus; Humans; Lipid Peroxidation; Maze Learning; Mice; Neurons; Oxidative Stress; Physostigmine

2016
(-)-Phenserine inhibits neuronal apoptosis following ischemia/reperfusion injury.
    Brain research, 2017, Dec-15, Volume: 1677

    Topics: Animals; Apoptosis; Brain Ischemia; Cell Hypoxia; Cell Line, Tumor; Cell Survival; Cholinesterase Inhibitors; Dose-Response Relationship, Drug; Glucose; Humans; Male; Neurons; Neuroprotective Agents; Physostigmine; Rats; Rats, Sprague-Dawley; Reperfusion Injury; Stroke

2017
Sequential combined Treatment of Pifithrin-α and Posiphen Enhances Neurogenesis and Functional Recovery After Stroke.
    Cell transplantation, 2018, Volume: 27, Issue:4

    Topics: Animals; Atrophy; Benzothiazoles; Cell Differentiation; Cell Proliferation; Cell Self Renewal; Cell Survival; Cells, Cultured; Cognition; Drug Therapy, Combination; Lateral Ventricles; Male; Mice, Inbred C57BL; Microtubule-Associated Proteins; Motor Activity; Neural Stem Cells; Neurogenesis; Physostigmine; Recovery of Function; Spheroids, Cellular; Stroke; Toluene

2018
Computational and Kinetic Studies of Acetylcholine Esterase Inhibition by Phenserine.
    Current pharmaceutical design, 2019, Volume: 25, Issue:18

    Topics: Acetylcholinesterase; Animals; Cholinesterase Inhibitors; Electrophorus; Kinetics; Molecular Docking Simulation; Physostigmine

2019
(-)-Phenserine and the prevention of pre-programmed cell death and neuroinflammation in mild traumatic brain injury and Alzheimer's disease challenged mice.
    Neurobiology of disease, 2019, Volume: 130

    Topics: Alzheimer Disease; Animals; Brain Concussion; Cell Death; Cerebral Cortex; Disease Models, Animal; Hippocampus; Mice; Mice, Transgenic; Neurons; Physostigmine

2019
Targeting increased levels of APP in Down syndrome: Posiphen-mediated reductions in APP and its products reverse endosomal phenotypes in the Ts65Dn mouse model.
    Alzheimer's & dementia : the journal of the Alzheimer's Association, 2021, Volume: 17, Issue:2

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Amyloid beta-Protein Precursor; Animals; Cholinesterase Inhibitors; Disease Models, Animal; Down Syndrome; Endosomes; Humans; Mice; Neurons; Phenotype; Phosphorylation; Physostigmine

2021
Mutasynthesis of Physostigmines in
    Organic letters, 2021, 08-20, Volume: 23, Issue:16

    Topics: Molecular Structure; Myxococcus xanthus; Physostigmine

2021