Page last updated: 2024-11-07

7-methoxytacrine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

7-Methoxytacrine is a synthetic derivative of tacrine, a cholinesterase inhibitor that has been investigated for the treatment of Alzheimer’s disease. It was synthesized by modifying the structure of tacrine, adding a methoxy group at the 7-position, aiming to enhance its pharmacological properties. Research has shown that 7-methoxytacrine exhibits improved potency and selectivity for acetylcholinesterase inhibition compared to tacrine. It has demonstrated potential cognitive enhancing effects in animal models of Alzheimer’s disease. However, like tacrine, it can cause liver toxicity, limiting its clinical application. Nevertheless, 7-methoxytacrine remains a valuable tool for studying cholinesterase inhibition and its role in cognitive function, potentially leading to the development of safer and more effective drugs for the treatment of neurodegenerative diseases.'

Cross-References

ID SourceID
PubMed CID119053
CHEMBL ID1256415
SCHEMBL ID195752
MeSH IDM0066081

Synonyms (27)

Synonym
9-amino-7-methoxy-1,2,3,4-tetrahydroakridin [czech]
1,2,3,4-tetrahydro-7-methoxy-9-acridinamine
acridine, 1,2,3,4-tetrahydro-9-amino-7-methoxy-
9-amino-7-methoxy-1,2,3,4-tetrahydroacridine
brn 0477401
ta-03
9-acridinamine, 1,2,3,4-tetrahydro-7-methoxy-
7-methoxytacrine
7-meota
5778-80-3
AKOS005066169
7-methoxy-1,2,3,4-tetrahydroacridin-9-amine
bdbm50327939
CHEMBL1256415 ,
9-amino-7-methoxy-1,2,3,4-tetrahydroakridin
ta 03
h6luf2h8w4 ,
unii-h6luf2h8w4
5-22-12-00199 (beilstein handbook reference)
SCHEMBL195752
CCG-357968
DTXSID40973360
7-methoxy-1,3,4,10-tetrahydroacridin-9(2h)-imine
CS-0102391
methoxytacrine, 7-
EN300-255377
Z960971048

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Forty-eight young male volunteers divided into six dosage groups were included into a single-dose pharmacokinetic study with either oral (p."( Pharmacokinetics and tolerance of 7-methoxytacrine following the single dose administration in healthy volunteers.
Albrecht, V; Dvorák, I; Dvoráková, J; Filip, V; Fusek, J; Havlůj, J; Vachek, J, 1991
)
0.56
" The study focused on description of the pharmacokinetic behaviour of K1234, blood-brain barrier penetration, identification of the main in vitro and in vivo metabolites."( UHPLC-HRMS study of pharmacokinetics of a novel hybrid cholinesterase inhibitor K1234: A comparison between in silico, in vitro and in vivo data.
Hroch, M; Karasova-Zdarova, J; Korabecny, J; Mezeiova, E; Mzik, M; Pejchal, J; Sestak, V, 2022
)
0.72

Bioavailability

ExcerptReferenceRelevance
" The rate of absorption of 7-MEOTA during luminal perfusion with single 7-MEOTA was compared with rate of absorption during simultaneous perfusion with 7-MEOTA and CRT and with absorption rate after the premedication with CRT for period of three days before beginning of perfusion."( Intestinal single-pass in situ perfusion technique in rat: the influence of L-carnitine on absorption of 7-methoxytacrine.
Bajgar, J; Herink, J; Herout, V; Kunes, M; Kvĕtina, J; Svoboda, Z, 2005
)
0.54

Dosage Studied

ExcerptRelevanceReference
" Forty-eight young male volunteers divided into six dosage groups were included into a single-dose pharmacokinetic study with either oral (p."( Pharmacokinetics and tolerance of 7-methoxytacrine following the single dose administration in healthy volunteers.
Albrecht, V; Dvorák, I; Dvoráková, J; Filip, V; Fusek, J; Havlůj, J; Vachek, J, 1991
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
CholinesteraseHomo sapiens (human)IC50 (µMol)16.61200.00001.559910.0000AID1186584; AID1384004; AID1593211; AID1763915; AID1831859
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)3.71000.00001.403910.0000AID1384006
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)11.72730.00000.933210.0000AID1166373; AID1186583; AID1256880; AID1384003; AID1498902; AID1593210; AID1763914; AID1831860; AID517222; AID628415; AID674795
AcetylcholinesteraseHomo sapiens (human)Ki4.21500.00001.27869.7300AID1186586; AID1186587; AID674798; AID674799
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (47)

Assay IDTitleYearJournalArticle
AID674796Inhibition of human plasmatic BChE using butylthiocholne substrate preincubated for 5 mins before substrate addition by Ellman's method2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, design and biological evaluation of novel highly potent tacrine congeners for the treatment of Alzheimer's disease.
AID1384011Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay2018European journal of medicinal chemistry, Apr-25, Volume: 150The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1593213Inhibition of HFIP pretreated amyloid beta (1-42) (unknown origin) self aggregation at 50 uM incubated for 24 hrs by thioflavin T based fluorescence assay relative to control2019European journal of medicinal chemistry, Apr-15, Volume: 168Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.
AID1256880Inhibition of human recombinant AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured every 2 mins by Ellman's method2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID628417Selectivity index, ratio of IC50 for human plasmatic BChE to IC50 for human recombinant AChE2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties.
AID1593212Selectivity index, ratio of IC50 for recombinant human BChE to IC50 for recombinant human AChE2019European journal of medicinal chemistry, Apr-15, Volume: 168Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.
AID674799Inhibition of human recombinant AChE assessed as dissociation constant for enzyme-inhibitor-substrate complex using acetylthiocholine substrate preincubated for 5 mins before substrate addition by Ellman's method2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, design and biological evaluation of novel highly potent tacrine congeners for the treatment of Alzheimer's disease.
AID1437793Inhibition of amyloid beta 42 (unknown origin) self aggregation at 50 uM by ThT-based fluorometric method relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease.
AID1256875Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins by microplate reader analysis2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID674798Inhibition of human recombinant AChE assessed as dissociation constant for enzyme-inhibitor complex using acetylthiocholine substrate preincubated for 5 mins before substrate addition by Ellman's method2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, design and biological evaluation of novel highly potent tacrine congeners for the treatment of Alzheimer's disease.
AID1593210Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured over 2 mins by UV-Vis spectrophotometric analysis based Ellman's method2019European journal of medicinal chemistry, Apr-15, Volume: 168Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.
AID1186584Inhibition of human BuChE pre-incubated for 5 mins before butylthiocholine substrate addition by Ellman's method2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.
AID1384005Selectivity ratio of IC50 for human plasmatic BuChE to IC50 for human erythrocyte AChE2018European journal of medicinal chemistry, Apr-25, Volume: 150The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1593211Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured over 2 mins by UV-Vis spectrophotometric analysis based Ellman's method2019European journal of medicinal chemistry, Apr-15, Volume: 168Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.
AID1763916Selectivity index, ratio of IC50 for human BuchE to IC50 for human Ache2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
AID1763919Inhibition of recombinant human nNOS assessed as maximum inhibition relative to control2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
AID517226Selectivity index, ratio of IC50 for human plasmatic BChE to IC50 for human recombinant AChE2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease.
AID1384004Inhibition of human plasmatic BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 2 mins time interval by Ellman's method2018European journal of medicinal chemistry, Apr-25, Volume: 150The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1593220Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2019European journal of medicinal chemistry, Apr-15, Volume: 168Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.
AID674797Selectivity index, ratio of IC50 for human plasmatic BChE to IC50 for human recombinant AChE2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, design and biological evaluation of novel highly potent tacrine congeners for the treatment of Alzheimer's disease.
AID1593215Effective permeability of the compound in PBS buffer at pH 7.4 at 100 uM after 3 to 6 hrs by PAMPA2019European journal of medicinal chemistry, Apr-15, Volume: 168Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.
AID517223Inhibition of human plasmatic BChE after 5 mins2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease.
AID1166376Inhibition of amyloid beta (1-42) self-mediated aggregation (unknown origin) at 10 uM after 24 hrs by thioflavin T fluorescence method2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects.
AID1593219Cytotoxicity against CHOK1 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2019European journal of medicinal chemistry, Apr-15, Volume: 168Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.
AID1763918Inhibition of recombinant human nNOS2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
AID1384003Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 2 mins time interval by Ellman's method2018European journal of medicinal chemistry, Apr-25, Volume: 150The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1166375Selectivity ratio of IC50 for human plasmatic BChE to human recombinant AChE2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects.
AID674795Inhibition of human recombinant AChE using acetylthiocholine substrate preincubated for 5 mins before substrate addition by Ellman's method2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis, design and biological evaluation of novel highly potent tacrine congeners for the treatment of Alzheimer's disease.
AID1186587Inhibition of human recombinant AChE assessed as dissociation constant for enzyme-inhibitor-substrate complex by Lineweaver-Burk plot2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.
AID1763914Inhibition of recombinant human AChE using acetylthiocholine as substrate by DTNB-reagent based Ellman's method2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
AID1831860Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease.
AID1384006Antagonist activity at human M1 mAChR expressed in CHO cells assessed as inhibition of oxotremorine M-stimulated calcium influx preincubated for 10 mins followed by oxotremorine M addition by Fluo-4 NW dye based fluorescence assay2018European journal of medicinal chemistry, Apr-25, Volume: 150The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1166374Inhibition of human plasmatic BChE after 5 mins by Ellman method2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects.
AID1166373Inhibition of human recombinant AChE after 5 mins by Ellman method2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects.
AID517222Inhibition of human recombinant AChE after 5 mins2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease.
AID1256879Inhibition of human plasmatic BChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured every 2 mins by Ellman's method2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID1256881Hepatotoxicity in human HepG2 cells assessed as cell viability after 24 hrs by MTT assay2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID1498902Inhibition of human erythrocyte AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured at 1 min time interval by Ellman's method2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery.
AID628415Inhibition of human recombinant AChE after 5 mins using spectrophotometer by Ellman's method2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties.
AID1763915Inhibition of recombinant human BuChE using butyrylthiocholine as substrate by Ellman's method2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
AID1763917Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
AID1186585Selectivity index, ratio of IC50 for human BuChE to IC50 for human recombinant AChE2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.
AID1256878Selectivity ratio of IC50 for human plasmatic BChE to IC50 for human recombinant AChE2015Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
AID1186586Inhibition of human recombinant AChE assessed as dissociation constant for enzyme-inhibitor complex by Lineweaver-Burk plot2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.
AID1831859Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease.
AID1186583Inhibition of human recombinant AChE pre-incubated for 5 mins before acetylthiocholine substrate addition by Ellman's method2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.
AID628416Inhibition of human plasmatic BChE after 5 mins using spectrophotometer by Ellman's method2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (52)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (7.69)18.7374
1990's16 (30.77)18.2507
2000's3 (5.77)29.6817
2010's25 (48.08)24.3611
2020's4 (7.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.53

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.53 (24.57)
Research Supply Index3.99 (2.92)
Research Growth Index5.52 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.53)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.92%)5.53%
Reviews1 (1.92%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other50 (96.15%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]