Tacrine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in Alzheimer's disease

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Tacrine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in Alzheimer's disease is …
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scholarly articleQ13442814

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P6179Dimensions Publication ID1011504888
P356DOI10.2165/00002512-199404060-00006
P698PubMed publication ID7521234

P2093author name stringD McTavish
A J Wagstaff
P2860cites workThree-dimensional structure of acetylcholinesterase and of its complexes with anticholinesterase drugsQ28260986
Effects of four non-cholinergic cognitive enhancers in comparison with tacrine and galanthamine on scopolamine-induced amnesia in ratsQ28324606
The mechanism of tetrahydroaminoacridine-evoked release of endogenous 5-hydroxytryptamine and dopamine from rat brain tissue prismsQ28354362
Evaluation of HP 029 (Velnacrine Maleate) in Alzheimer's DiseaseaQ33296510
A double-blind, placebo controlled trial of high-dose lecithin in Alzheimer's diseaseQ33621285
Effect of tetrahydroaminoacridine on cognition, function and behaviour in Alzheimer's disease.Q34578939
Steady-state pharmacokinetics of tacrine in patients with Alzheimer's diseaseQ34636158
Clinical pharmacokinetics of intravenous and oral 9-amino-1,2,3,4-tetrahydroacridine, tacrineQ34648272
Pharmacokinetics of tacrine hydrochloride in Alzheimer's diseaseQ34669866
Serum concentrations of tacrine hydrochloride predict its adverse effects in Alzheimer's diseaseQ34731347
Muscarinic Receptor Function and Acetylcholinesterase Activity after Chronic Administration of Tacrine to Mice at Therapeutic Drug ConcentrationsQ48601207
Tetrahydroaminoacridine improves passive avoidance retention defects induced by aging and medial septal lesion but not by fimbria-fornix lesionQ48624682
The effect of tacrine (THA) on cycloheximide- and basal forebrain lesion-induced memory deficit in ratsQ48628672
Muscarinic subtype selectivity of tetrahydroaminoacridine: Possible relationship to its capricious efficacyQ48638257
Combination of atipamezole and tetrahydroaminoacridine/pilocarpine treatment suppresses high voltage spindle activity in aged ratsQ48673408
Tetrahydroaminoacridine alleviates medial septal lesion-induced and age-related spatial reference but not working memory deficitsQ48707784
Modulation of EEG rhythmicity and spike activity in the rat hippocampus by systemically administered tetrahydroaminoacridine, scopolamine and atipamezoleQ48722061
The effects of THA on scopolamine and nucleus basalis lesion-induced EEG slowingQ48739991
Negative Effects of Tacrine (Tetrahydroaminoacridine) and Methoxytacrine on the Metabolism of Acetylcholine in Brain Slices Incubated Under Conditions Stimulating Neurotransmitter ReleaseQ48764100
Tetrahydroaminoacridine induces opposite changes in muscarinic and nicotinic receptors in rat brainQ48895769
Inhibition of rat brain histamine-N-methyltransferase by 9-amino-1,2,3,4-tetrahydroacridine (THA).Q48896672
Effects of tetrahydro-9-aminoacridine on cortical and hippocampal neurons in the rat: an in vivo and in vitro studyQ48897660
Low dose tetrahydroaminoacridine (THA) improves cognitive function but does not affect brain acetylcholine in ratsQ48957090
Studies on new, centrally active and reversible acetylcholinesterase inhibitorsQ48959304
Modulation of gamma-aminobutyric acid release in cerebral cortex by fluoride, phorbol ester, and phosphodiesterase inhibitors: differential sensitivity of acetylcholine release to fluoride and K+ channel blockersQ49050274
A 30-week randomized controlled trial of high-dose tacrine in patients with Alzheimer's disease. The Tacrine Study GroupQ52026922
Tetrahydroaminoacridine-lecithin combination treatment in patients with intermediate-stage Alzheimer's disease. Results of a Canadian double-blind, crossover, multicenter studyQ52057810
The effects of tacrine and zacopride on the performance of adult rats in the working memory taskQ52062457
Delayed matching-to-sample performance during a double-blind trial of tacrine (THA) and lecithin in patients with Alzheimer's diseaseQ52067652
Discrimination of Alzheimer patients responding to cholinesterase inhibitor therapy.Q52087212
Interactions between scopolamine and muscarinic cholinergic agonists or cholinesterase inhibitors on spatial alternation performance in ratsQ52104144
Direct comparison of cognitive facilitation by physostigmine and tetrahydroaminoacridine in two primate modelsQ52104748
Multiple effects of tetrahydroaminoacridine on the cholinergic system: biochemical and behavioural aspectsQ52111280
Prevalence of Alzheimer's disease in a community population of older persons. Higher than previously reportedQ52112673
Effects of cholinergic drugs on learning impairment in ventral globus pallidus-lesioned ratsQ52116897
Tetrahydroaminoacridine selectively attenuates NMDA receptor-mediated neurotoxicityQ69925852
Tetrahydroaminoacridine inhibits high voltage spindle activity in aged rats after acute and chronic treatmentQ70147939
Blockade of voltage-dependent 42K efflux from rat brain synaptosome by minaprine and tetrahydroaminoacridineQ70180833
Physostigmine inhibition of 3',5'-cyclic AMP phosphodiesterase from cat sciatic nerveQ70198103
The effect of tacrine on acetylcholine overflow in the heartQ70244912
Interaction of tacrine at M1 and M2 cholinoceptors in guinea pig brainQ72590069
An investigation into the formation of stable, protein-reactive and cytotoxic metabolites from tacrine in vitro. Studies with human and rat liver microsomesQ72870562
Tacrine in Alzheimer's diseaseQ93879915
Effect of acute arecoline, tacrine, and arecoline + tacrine post-training administration on retention in late middle-aged miceQ52125106
Modest facilitation on memory in dementia with combined lecithin and anticholinerestase treatmentQ52222101
Chronic treatments with cholinoceptor drugs influence spatial learning in ratsQ52228711
Comparison of DuP 996, with physostigmine, THA and 3,4-DAP on hypoxia-induced amnesia in ratsQ52240599
Learning deficits in aged rats pretreated chronically with barbital and tested late in abstinence: alleviation by tetrahydroaminoacridineQ52243706
Tetrahydroaminoacridine facilitates passive avoidance learning in rats with nucleus basalis magnocellularis lesionsQ52244318
Oral tetrahydroaminoacridine in long-term treatment of senile dementia, Alzheimer typeQ52259713
Effects of nicotine on local cerebral glucose utilization in the rat.Q52267234
Physostigmine, tacrine and metrifonate: the effect of multiple doses on acetylcholine metabolism in rat brainQ52454833
In vitro effects of various cholinesterase inhibitors on acetyl- and butyrylcholinesterase of healthy volunteersQ53030770
Tacrine for treating Alzheimer's diseaseQ53179456
Tacrine in Alzheimer's disease. Time course of changes in cognitive function and practice effectsQ53180360
Somatostatin and cognitive functions in Alzheimer's disease--the relationship of cerebrospinal fluid somatostatin increase with clinical response to tetrahydroaminoacridineQ53181237
Discrimination of tetrahydroaminoacridine responders by a single dose pharmaco-EEG in patients with Alzheimer's diseaseQ53182756
Acute hepatitis after tetrahydroaminoacridine administration for Alzheimer's disease.Q53186098
Treatment of Alzheimer's disease with short- and long-term oral THA and lecithin: a double-blind studyQ53186322
Effects of 9-amino-1,2,3,4-tetrahydroacridine (THA), a potential drug for treatment of Alzheimer's disease, on the physical state of human erythrocyte membranesQ53188763
Hepatotoxicity of tetrahydroaminoacridineQ53190129
THA and Alzheimer's diseaseQ53193177
Glucose metabolism and acetylcholine synthesis in relation to neuronal activity in Alzheimer's diseaseQ53196303
Long-term use of tacrineQ53204306
An evaluation of the efficacy and safety of tetrahydroaminoacridine (THA) without lecithin in the treatment of Alzheimer's diseaseQ53207687
Mechanisms of the tetrahydroaminoacridine effect on action potential and ion currents in myelinated axonsQ53296694
Tetrahydroaminoacridine and lecithin in the treatment of Alzheimer's disease. Effect on cognition, functioning in daily life, behavioural disturbances and burden experienced by the carersQ53297359
Inhibitory effect of 9-amino-1,2,3,4-tetrahydroacridine (THA) on the potassium current of rabbit sinoatrial nodeQ53299131
Interaction of tacrine and velnacrine with neocortical synaptosomal membranes: relevance to Alzheimer's diseaseQ53317324
Tetrahydroaminoacridine blocks potassium channels and inhibits sodium inactivation in Myxicola.Q54398592
Tacrine in Alzheimer's diseaseQ56763713
Effect of acute arecoline, tacrine and arecoline + tacrine post-training administration on retention in old miceQ57136373
The Prevalence of Dementia in Europe: A Collaborative Study of 1980–1990 FindingsQ57782178
Block of the cardiac pacemaker current (If) in the rabbit sino-atrial node and in canine Purkinje fibres by 9-amino-1,2,3,4-tetrahydroacridineQ61910336
Effects of tacrine, aminopyridines, and physostigmine on acetylcholinesterase, acetylcholine release, and potassium currentsQ62900132
THA increases action potential duration of central histamine neurons in vitroQ67242674
Effects of tacrine on insulin secretion and 86Rb+ and 45Ca++ efflux from rat pancreatic isletsQ67865042
Interaction of 9-amino-1,2,3,4-tetrahydroaminoacridine (THA) with human cortical nicotinic and muscarinic receptor binding in vitroQ67960354
Prevention by choline of the depletion of membrane phosphatidylcholine by a cholinesterase inhibitorQ68251729
Functional and pharmacokinetic studies of tetrahydroaminoacridine in patients with amyotrophic lateral sclerosisQ68648020
Tacrine and lecithin in Alzheimer's diseaseQ68780451
Oral tetrahydroaminoacridine in the treatment of senile dementia, Alzheimer's typeQ69033453
Effects of THA on ionic currents in myelinated axons of Xenopus laevisQ69094425
Tetrahydroaminoacridine but not 4-aminopyridine inhibits high-affinity choline uptake in striatal and hippocampal synaptosomesQ69339864
Quantitative whole-body autoradiographic determination of tacrine tissue distribution in rats following intravenous or oral doseQ69398829
Do tetrahydroaminoacridine (THA) and physostigmine restore acetylcholine release in Alzheimer brains via nicotinic receptors?Q69449361
Changes in the regional brain histamine and histidine levels in postmortem brains of Alzheimer patientsQ69597522
Multiple in vitro interactions with and differential in vivo regulation of muscarinic receptor subtypes by tetrahydroaminoacridineQ69681544
Tacrine slows the rate of ageing of sarin-inhibited acetylcholinesteraseQ69683824
The effect of an acute nicotine infusion on the local cerebral glucose utilization of the awake ratQ69745115
Tacrine (tetrahydroaminoacridine; THA) and lecithin in senile dementia of the Alzheimer type: a multicentre trial. Groupe Français d'Etude de la TetrahydroaminoacridineQ35168053
Putative mechanisms of action of tacrine in Alzheimer's disease.Q35342313
Neuroreceptor changes in Alzheimer diseaseQ35659804
9-Amino-1,2,3,4-tetrahydroacridine (THA) is a potent blocker of cardiac potassium channelsQ35755032
Tetrahydroaminoacridine (tacrine) stimulates neurosecretion at mammalian motor endplatesQ35888481
Protease inhibitors and indoleamines selectively inhibit cholinesterases in the histopathologic structures of Alzheimer diseaseQ36067600
Tacrine: A pharmacological reviewQ36673752
Long-term treatment with tacrine (THA) in Alzheimer's disease--evaluation of neuropsychological dataQ36744692
Efficacy of tacrine and lecithin in mild to moderate Alzheimer's disease: double blind trialQ36884943
Diagnostic and pharmacological approaches in Alzheimer's diseaseQ36972797
Tacrine in relation to amino acid transmitters in Alzheimer's disease.Q37578195
Alternatives in the treatment of memory loss in patients with Alzheimer's diseaseQ37775182
Shifting patterns of cortical cholinesterases in Alzheimer's disease: implications for treatment, diagnosis, and pathogenesis.Q38137707
A psychopharmacological perspective of cognitive functions. II. Specific pharmacologic agentsQ38161282
Tacrine, a drug with therapeutic potential for dementia: post-mortem biochemical evidenceQ38365810
Clinical experience with and side-effects of tacrine hydrochloride in Alzheimer's disease: a pilot studyQ38719669
Clinical pharmacology of tetrahydroaminoacridine: a possible therapeutic agent Alzheimer's diseaseQ38723971
Neurotransmitter-related enzymes and indices of hypoxia in senile dementia and other abiotrophiesQ39125647
Pharmacokinetics and effects of 9-amino-1,2,3,4-tetrahydroacridine in the immediate postoperative period in neurosurgical patientsQ39510569
Alzheimer's Disease: A Disorder of Cortical Cholinergic InnervationQ40145746
Clinical studies in Alzheimer patients with positron emission tomographyQ40621341
Further analysis of the cognitive effects of tetrahydroaminoacridine (THA) in Alzheimer's disease: assessment of attentional and mnemonic function using CANTAB.Q41099297
Histamine-induced arousal in the conscious and pentobarbital-pretreated rat.Q41621997
Open trial of tacrine therapy in 70 HIV-infected patients.Q41893410
Effects of tacrine, velnacrine (HP029), suronacrine (HP128), and 3,4-diaminopyridine on skeletal neuromuscular transmission in vitroQ41963937
Effects of velnacrine, tacrine and physostigmine on tetanic twitch responses at the rat neuromuscular junctionQ42099013
Inhibitory effect of 1,2,3,4-tetrahydro-9-aminoacridine on the depolarization-induced release of GABA from cerebral cortexQ42144280
Correlation of brain levels of 9-amino-1,2,3,4-tetrahydroacridine (THA) with neurochemical and behavioral changesQ42193084
Tetrahydroaminoacridine inhibits human and rat brain monoamine oxidaseQ42193896
Comparison of 4-aminopyridine and tetrahydroaminoacridine on basal forebrain neuronsQ42482741
Tetrahydroaminoacridine improves the spatial acquisition deficit produced by nucleus basalis lesions in ratsQ42484825
Hepatotoxic effects of tacrine administration in patients with Alzheimer's diseaseQ42603612
Measurements of tacrine and monoamines in brain by in vivo microdialysis argue against release of monoamines by tacrine at therapeutic dosesQ42713800
The cholinergic pharmacology of tetrahydroaminoacridine in vivo and in vitroQ42847596
The cholinergic system and the excitatory amino acids in Alzheimer's diseaseQ43537493
Effect of nicotine and tacrine on acetylcholine release from rat cerebral cortical slicesQ43543591
Pharmacological significance of acetylcholinesterase inhibition by tetrahydroaminoacridineQ43782041
Pharmacokinetics of tetrahydroaminoacridine: relations to clinical and biochemical effects in Alzheimer patientsQ43852948
Investigation of the mechanism of the effect of tacrine (tetrahydroaminoacridine) on the metabolism of acetylcholine and choline in brain cortical prismsQ43888912
Tetrahydroaminoacridine block of N-methyl-D-aspartate-activated cation channels in cultured hippocampal neuronsQ43957035
Structure-activity investigation of the alteration of the physical state of the skeletal network of proteins in human erythrocyte membranes induced by 9-amino-1,2,3,4-tetrahydroacridineQ44077660
Comparison of the chromatographic characteristics of metabolites of tacrine hydrochloride in human serum and urine with those of in vitro metabolic products from hepatic microsomesQ44091007
A controlled trial of tacrine in Alzheimer's disease. The Tacrine Study GroupQ44110810
Influence of tetrahydro-9-aminoacridine on excitatory amino acid releaseQ44130586
Effects of tetrahydroaminoacridine on liver function in patients with Alzheimer's diseaseQ44223667
Reversal by tetrahydroaminoacridine of scopolamine-induced memory and performance deficits in ratsQ44324648
Tetrahydroaminoacridine, 3,4 diaminopyridine and physostigmine: direct comparison of effects on memory in aged primatesQ44458753
Tacrine restores cholinergic nicotinic receptors and glucose metabolism in Alzheimer patients as visualized by positron emission tomographyQ44486170
Reversibility of the inhibition of acetylcholinesterase by tacrineQ44714988
9-Amino-1,2,3,4-tetrahydroacridine is a potent inhibitor of histamine N-methyltransferaseQ44760156
Tacrine in Alzheimer's diseaseQ44777869
Heterogeneity of adverse hepatic reactions to tetrahydroaminoacridineQ45017014
Positive and negative effects of tacrine (tetrahydroaminoacridine) and methoxytacrine on the metabolism of acetylcholine in brain cortical prisms incubated under "resting" conditionsQ45055455
Utility of an elevated plus-maze for the evaluation of memory in mice: effects of nootropics, scopolamine and electroconvulsive shockQ45130083
Memory facilitation by histamineQ45207574
Tetrahydroaminoacridine and physostigmine have opposing effects on probability of transmitter release at the frog neuromuscular junctionQ45262334
Characterisation of dopamine and serotonin uptake inhibitory effects of tetrahydroaminoacridine in rat brainQ45272933
9-Amino-1,2,3,4-tetrahydroacridine (THA) blocks agonist-induced potassium conductance in rat hippocampal neuronesQ45385687
Effects of atipamezole and tetrahydroaminoacridine on nucleus basalis lesion-induced EEG changes.Q45999072
Cholinesterase inhibitor therapy for Alzheimer dementia: what do animal models tell us?Q46543100
Do blood pressure and age predict response to tacrine (THA) in Alzheimer's disease? A preliminary reportQ46605078
Tetrahydroaminoacridine increases acetylcholine synthesis and glucose oxidation by mouse brain slices in vitroQ46616845
SPECT brain imaging in Alzheimer's disease during treatment with oral tetrahydroaminoacridine and lecithinQ46622236
Blockade of a cardiac K+ channel by tacrine: interactions with muscarinic and adenosine receptorsQ46659151
Therapeutic trials using tacrine and other cholinesterase inhibitorsQ46914279
Evidence for histaminergic arousal mechanisms in the hypothalamus of cat.Q48119553
Further analysis of the neuropharmacological profile of 9-amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer's diseaseQ48161693
Anatomy of cholinesterase inhibition in Alzheimer's disease: effect of physostigmine and tetrahydroaminoacridine on plaques and tanglesQ48176447
Tetrahydroaminoacridine blocks voltage-dependent ion channels in hippocampal neuronsQ48195378
9-Amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer's disease, inhibits acetylcholinesterase activity and slow outward K+ currentQ48208220
Cholinesterases within neurofibrillary tangles related to age and Alzheimer's diseaseQ48222617
Reduced number of [3H]nicotine and [3H]acetylcholine binding sites in the frontal cortex of Alzheimer brainsQ48265799
Systemic administration of lithium chloride and tacrine increases nitric oxide synthase activity in the hippocampus of ratsQ48267913
Positron emission tomography study of [11C]methyl-tetrahydroaminoacridine (methyl-tacrine) in baboon brainQ48284078
THA does not affect sleep or EEG spectral power in Alzheimer's diseaseQ48284449
Differential effects of physostigmine and 1,2,3,4-tetrahydro-9-aminoacridine on the beta-adrenoceptor transduction systemQ48319946
Selective loss of central cholinergic neurons in Alzheimer's diseaseQ48342983
Distribution of tacrine across the blood-brain barrier in awake, freely moving rats using in vivo microdialysis samplingQ48360983
Psychometric discrimination of tetrahydroaminoacridine responders in Alzheimer patientsQ48372876
Oral tetrahydroaminoacridine treatment of Alzheimer's disease evaluated clinically and by regional cerebral blood flow and EEG.Q48372886
Effect of long-term treatment with tacrine (THA) in Alzheimer's disease as visualized by PET.Q48384635
The relationship of cerebrospinal fluid monoamine metabolites with clinical response to tetrahydroaminoacridine in patients with Alzheimer's diseaseQ48391011
A double-blind, placebo-controlled multicenter study of tacrine for Alzheimer's disease. The Tacrine Collaborative Study GroupQ48418557
Metrifonate and tacrine: a comparative study on their effect on acetylcholine dynamics in mouse brainQ48436093
Comparative effects of alpha-2 receptor agents and THA on the performance of adult and aged rats in the delayed non-matching to position taskQ48549306
P433issue6
P921main subjectAlzheimer's diseaseQ11081
pharmacokineticsQ323936
pharmacodynamicsQ725307
P304page(s)510-540
P577publication date1994-06-01
P13046publication type of scholarly workreview articleQ7318358
P1433published inDrugs & AgingQ5308946
P1476titleTacrine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in Alzheimer's disease
P478volume4

Reverse relations

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