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galantamine

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Description

Galantamine is an alkaloid derived from the bulbs of the snowdrop (Galanthus nivalis) and the summer snowflake (Leucojum aestivum). It is a cholinesterase inhibitor, meaning it blocks the breakdown of acetylcholine, a neurotransmitter important for memory and learning. Galantamine is used clinically to treat mild to moderate Alzheimer's disease. It has also been investigated for its potential to treat other conditions, such as Parkinson's disease, cognitive decline in healthy aging, and myasthenia gravis. Galantamine's synthesis can be achieved through different methods, including chemical synthesis and extraction from natural sources. Researchers study galantamine because of its potential to enhance cognitive function and its potential to treat neurodegenerative diseases. It is believed to work by increasing the levels of acetylcholine in the brain, which is essential for communication between nerve cells.'

Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

galanthamine : A benzazepine alkaloid isolated from certain species of daffodils. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

FloraRankFlora DefinitionFamilyFamily Definition
GalanthusgenusA plant genus in the family Amaryllidaceae. Galanthus nivalis L. is the source of GALANTHAMINE.[MeSH]AmaryllidaceaeA family of herbaceous plants with bulbs or rhizomes in the order Asparagales.[MeSH]
GalanthusgenusA plant genus in the family Amaryllidaceae. Galanthus nivalis L. is the source of GALANTHAMINE.[MeSH]AmaryllidaceaeA family of herbaceous plants with bulbs or rhizomes in the order Asparagales.[MeSH]

Cross-References

ID SourceID
PubMed CID3449
CHEMBL ID1623394
CHEBI ID91735
SCHEMBL ID220427
MeSH IDM0008951
PubMed CID9651
CHEMBL ID659
CHEBI ID42944
SCHEMBL ID2577
SCHEMBL ID3293474
MeSH IDM0008951

Synonyms (166)

Synonym
BRD-A49148672-004-01-6
6h-benzofuro(3a,3,2-ef)(2)benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, (4as-(4a.alpha.,6.beta.,8ar*))-
OPREA1_098077
OPREA1_097473
galantamin
6h-benzofuro[3a,2-ef][2]benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, [4as-(4a.alpha.,6.beta.,8ar*)]-
mls000766281 ,
nsc100058 ,
smr000528869
NCI60_000004
FT-0668943
FT-0667895
AKOS000635322
HMS2269H23
STL146336
AKOS021856294
SCHEMBL220427
BBL028838
Q-201144
galanthamine,(3.alpha.-
epigalanthamin
galanthamine #
CHEMBL1623394
HMS3561F13
CHEBI:91735
FT-0668941
epigalanthamine
galantamine; hsdb 7361
BCP28966
Q27163546
lsm-1597
FT-0668942
BRD-A49148672-001-07-9
9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-14-ol
(1s,12s,14r)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.0^{1,12.0^{6,17]heptadeca-6(17),7,9,15-tetraen-14-ol
DTXSID70859345
cerapp_13557
ent- galanthamine
BIDD:GT0517
AC-20240
AB00053614-09
BRD-K49481516-004-03-5
BRD-K49481516-004-04-3
DIVK1C_000590
KBIO1_000590
SDCCGMLS-0066737.P001
SPECTRUM_001271
SPECTRUM5_001673
PRESTWICK3_000588
nsc 100058
6h-benzofuro(3a,3,2-ef)(2)benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, (4as,6r,8as)-
(4as,6r,8as)-4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6h-benzofuro(3a,3,2-ef)(2)benzazepin-6-ol
galantaminum [inn-latin]
galantamina [inn-spanish]
galanthaminum
hsdb 7361
brn 0093736
BPBIO1_000480
SMP1_000131
6h-benzofuro(3a,3,2-ef)(2)benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-
gnt ,
(-)-galanthamine
6h-benzofuro[3a,3,2-ef][2]benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, (4as,6r,8as)-
galantamine (usan/inn)
IDI1_000590
D04292
BSPBIO_003416
PRESTWICK2_000588
PROBES2_000395
PROBES1_000055
galantamine
lycoremin
357-70-0
galanthamine
jilkon
nsc-100058
lycoremine
C08526
inchi=1/c17h21no3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,12,14,19h,7-10h2,1-2h3/t12-,14-,17-/m0/s1
asutzqlvashgkv-jdfrzjqesa-
CHEBI:42944 ,
1QTI
chembl659 ,
galanthamine, 12
1DX6
DB00674
(1s,12s,14r)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.0^{1,12}.0^{6,17}]heptadeca-6,8,10(17),15-tetraen-14-ol
bdbm10404
NCGC00024731-02
KBIO3_002636
KBIO2_004319
KBIO2_006887
KBIOSS_001751
KBIOGR_001417
KBIO2_001751
PRESTWICK1_000588
SPECTRUM3_001738
SPBIO_002655
NINDS_000590
PRESTWICK0_000588
SPECTRUM4_000839
BSPBIO_000436
HMS2089H03
(-)-galantamine
4-27-00-02184 (beilstein handbook reference)
0d3q044kca ,
galantamine [usan:inn:ban]
unii-0d3q044kca
galantamina
galantaminum
nsc759861
nsc-759861
pharmakon1600-01501202
dtxsid2045606 ,
S3866
AKOS015965330
AM62710
NCGC00017256-05
HY-76299
CS-1217
galantamine [hsdb]
(4as,6r,8as)-4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6h-benzofuro[3a,3,2-ef][2]benzazepin-6-ol
galantamine [who-dd]
galantamine [vandf]
galantamine [inn]
galantamine [mi]
galantamine [usan]
6h-benzofuro(3a,3,2-ef)(2)benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, (4as,6r,8as)
(4as,6r,8as)-4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6h-benzofurol[3a,3,2,-ef][2]benzazepin-6-ol
gtpl6693
(1s,12s,14r)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-14-ol
CCG-212961
SCHEMBL2577
ASUTZQLVASHGKV-JDFRZJQESA-N
SCHEMBL3293474
AC-34328
AB00053614_10
6h-benzofuro(3a,3,2-ef)(2)benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, (4a.alpha.,6.beta.,8ar*)-
galanthamine, (+/-)-
(+/-)-galantamine
6h-benzofuro(3a,3,2-ef)(2)benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, (4aalpha,6beta,8ar*)-
unii-1t835z585r
galantamine, (+/-)-
(+/-)-galanthamine
23173-12-8
6h-benzofuro(3a,3,2-ef)(2)benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, (4ar,6s,8ar)-rel-
1t835z585r ,
bodamine
SR-05000001783-4
SBI-0051689.P002
NCGC00017256-11
(4as,6r,8as)-3-methoxy-11-methyl-4a,5,9,10,11,12-hexahydro-6h-benzo[2,3]benzofuro[4,3-cd]azepin-6-ol
(4as,6r,8as)-3-methoxy-11-methyl-5,6,9,10,11,12-hexahydro-4ah-benzo[2,3]benzofuro[4,3-cd]azepin-6-ol
Q412690
mfcd00867189
1008759-59-8
BRD-K49481516-004-09-2
HMS3885C10
NCGC00017256-17
AS-56354
EN300-708805
(1s,12s,14r)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.0^{1,12}.0^{6,17}]heptadeca-6(17),7,9,15-tetraen-14-ol
galantaminum (inn-latin)
galantamina (inn-spanish)
(4as,6r,8as)-3-methoxy-11-methyl-5,6,9,10,11,12-hexahydro-4ah-(1)benzofuro(3a,3,2-ef)(2)benzazepin-6-ol
n06da04

Research Excerpts

Toxicity

Galantamine is a centrally acting cholinesterase (ChE) inhibitor and a nicotinic allosteric potentiating ligand used to treat Alzheimer's disease. Galantamine appears to be an effective and safe therapy for patients with DLB. 183 of 207 patients who received galantamine and 177 of 200 who received placebo had adverse events, which were mostly mild to moderate.

ExcerptReferenceRelevance
" There were no serious adverse events (AEs) or premature withdrawals from the study because of AEs."( Pharmacokinetics and safety of galantamine in subjects with hepatic impairment and healthy volunteers.
Iyer, GR; Truyen, L; Verhaeghe, T; Zhao, Q, 2002
)
0.31
" Safety and tolerability were monitored throughout the trial by recording adverse events, laboratory tests, and cardiovascular parameters."( Galantamine pharmacokinetics, safety, and tolerability profiles are similar in healthy Caucasian and Japanese subjects.
Brett, M; Huang, F; Hust, R; Raoult, A; Van Osselaer, N; Van Peer, A; Verhaeghe, T; Zhao, Q, 2002
)
0.31
" Galantamine and risperidone were both safe and well tolerated administered either alone or together."( Pharmacokinetic and safety assessments of galantamine and risperidone after the two drugs are administered alone and together.
Huang, F; Janssens, L; Lasseter, KC; Lau, H; Verhaeghe, T; Zhao, Q, 2002
)
0.31
" Incidence of adverse events in patients > 80 years was similar to that in the overall study population."( Galantamine demonstrates efficacy and safety in elderly patients with Alzheimer disease.
Bullock, R; Gauthier, S; Kurz, A; Marcusson, J; Schwalen, S,
)
0.13
" The most frequently reported adverse events, characteristic of older dementia patients, included depression, agitation, and insomnia."( Long-term safety and cognitive effects of galantamine in the treatment of probable vascular dementia or Alzheimer's disease with cerebrovascular disease.
Damaraju, CR; Erkinjuntti, T; Kurz, AF; Lilienfeld, S; Small, GW, 2003
)
0.32
" Motor scores, as measured by the UPDRS motor subscale, showed mild improvement, which demonstrates that galantamine has no adverse effect on parkinsonian symptoms."( Efficacy and safety of galantamine in patients with dementia with Lewy bodies: a 12-week interim analysis.
Bednarczyk, EM; Edwards, KR; Farlow, M; Hershey, L; Johnson, S; Lichter, D; Wray, L, 2004
)
0.32
"6 %)treatment was withdrawn because of mostly gastrointestinal adverse events."( Effectiveness and safety of cholinesterase inhibitors in elderly subjects with Alzheimer's disease: a "real world" study.
Bardelli, F; Bencini, F; Biagini, CA; Caleri, V; Cantini, C; Cavallini, MC; Marini, M; Masotti, G; Mecacci, R; Mossello, E; Razzi, E; Sarcone, E; Tilli, S; Tonon, E, 2004
)
0.32
" Adverse events (AEs) were coded to WHO preferred terms, including AEs begun in previous trials."( Long-term efficacy and safety of galantamine in patients with mild-to-moderate Alzheimer's disease: multicenter trial.
Damaraju, CV; Pirttilä, T; Truyen, L; Wilcock, G, 2004
)
0.32
"To provide a systematic review of the best quality evidence of the effects of donepezil, rivastigmine and galantamine on cognition, quality of life and adverse events in people with mild to moderately-severe AD."( A systematic review of the clinical effectiveness of donepezil, rivastigmine and galantamine on cognition, quality of life and adverse events in Alzheimer's disease.
Clegg, A; Green, C; Kirby, J; Loveman, E; Payne, E; Picot, J; Takeda, A, 2006
)
0.33
" Adverse events were generally related to the gastrointestinal system, with a tendency for these to be more common in the treatment arms."( A systematic review of the clinical effectiveness of donepezil, rivastigmine and galantamine on cognition, quality of life and adverse events in Alzheimer's disease.
Clegg, A; Green, C; Kirby, J; Loveman, E; Payne, E; Picot, J; Takeda, A, 2006
)
0.33
" All the adverse events (AE) reported were recorded."( [Observational study on safety, tolerability and effectiveness of galantamine in patients with mild to moderately severe Alzheimer's disease].
Amer, G; Barquero, M; Blesa, R; Ezpeleta, D; Galdós, L; García Ribas, G; Marey López, J; Marsall, C; Olascoaga, J,
)
0.13
"Galantamine is a safe and well-tolerated treatment, and provides cognitive, functional, and behavioral benefits in patients with mild to moderately severe AD."( [Observational study on safety, tolerability and effectiveness of galantamine in patients with mild to moderately severe Alzheimer's disease].
Amer, G; Barquero, M; Blesa, R; Ezpeleta, D; Galdós, L; García Ribas, G; Marey López, J; Marsall, C; Olascoaga, J,
)
0.13
"Cardiovascular disorders are the most frequently reported adverse effects of drugs used to treat Alzheimer's disease."( Anti-Alzheimer drugs: life-threatening adverse effects.
, 2007
)
0.34
" Adverse events were generally mild and transient."( Efficacy and safety of galantamine in patients with dementia with Lewy bodies: a 24-week open-label study.
Edwards, K; Farlow, M; Hake, A; Hershey, L; Johnson, S; Lichter, D; Pasquier, F; Royall, D, 2007
)
0.34
"Galantamine appears to be an effective and safe therapy for patients with DLB."( Efficacy and safety of galantamine in patients with dementia with Lewy bodies: a 24-week open-label study.
Edwards, K; Farlow, M; Hake, A; Hershey, L; Johnson, S; Lichter, D; Pasquier, F; Royall, D, 2007
)
0.34
" Trial methods, clinical characteristics, outcomes, and adverse events were extracted and checked."( Efficacy and adverse effects of cholinesterase inhibitors and memantine in vascular dementia: a meta-analysis of randomised controlled trials.
Kavirajan, H; Schneider, LS, 2007
)
0.34
" Compared with placebo, more dropouts and adverse events (anorexia, nausea, vomiting, diarrhoea, and insomnia) occurred with the cholinesterase inhibitors, but not with memantine."( Efficacy and adverse effects of cholinesterase inhibitors and memantine in vascular dementia: a meta-analysis of randomised controlled trials.
Kavirajan, H; Schneider, LS, 2007
)
0.34
" The most frequently reported adverse event was nausea (galantamine, 29%; placebo, 10%)."( Safety and efficacy of galantamine in subjects with mild cognitive impairment.
Brashear, HR; Feldman, H; Gauthier, S; Mayorga, AJ; Nye, JS; Scinto, L; Truyen, L; Wang, D; Wilcock, GK; Winblad, B, 2008
)
0.35
" Adverse events (drooling, postural hypotension, nausea, dysuria) were observed in 7 (30%) of galantamine treated patients."( [Efficacy and safety of galantamine (reminyl) in the treatment of dementia in patients with Parkinson's disease (open-label controlled trial)].
Emelin, AIu; Litvinenko, IV; Mogil'naia, VI; Odinak, MM, 2007
)
0.34
" Galantamine appears to be safe and tolerable in patients with epilepsy."( The safety and tolerability of galantamine in patients with epilepsy and memory difficulties.
Andrews, S; Faught, E; Griffith, HR; LeBron Paige, A; Martin, R; Ware, J; Welty, T, 2008
)
0.35
" Across trials, the incidence of adverse events was generally lowest for donepezil and highest for rivastigmine."( Efficacy and safety of donepezil, galantamine, and rivastigmine for the treatment of Alzheimer's disease: a systematic review and meta-analysis.
Gartlehner, G; Hansen, RA; Jonas, DE; Moore, CG; Morgan, LC; Webb, AP, 2008
)
0.35
" Adverse events, vital signs, laboratory parameters, and electrocardiograms were monitored."( Safety and efficacy of galantamine (Reminyl) in severe Alzheimer's disease (the SERAD study): a randomised, placebo-controlled, double-blind trial.
Bernabei, R; Bullock, R; Burns, A; Came, E; Cruz Jentoft, AJ; Frölich, L; Hammond, GL; Hock, C; Raivio, M; Schwalen, S; Triau, E; Van Baelen, B; van Oene, JC; Vandewoude, M; Wimo, A, 2009
)
0.35
" 183 of 207 patients (88%) who received galantamine and 177 of 200 (89%) who received placebo had adverse events, which were mostly mild to moderate."( Safety and efficacy of galantamine (Reminyl) in severe Alzheimer's disease (the SERAD study): a randomised, placebo-controlled, double-blind trial.
Bernabei, R; Bullock, R; Burns, A; Came, E; Cruz Jentoft, AJ; Frölich, L; Hammond, GL; Hock, C; Raivio, M; Schwalen, S; Triau, E; Van Baelen, B; van Oene, JC; Vandewoude, M; Wimo, A, 2009
)
0.35
" The most common adverse events were nausea, dizziness, and weight loss which more often occurred during the dose-escalation phase."( Safety and tolerability of galantamine in possible Alzheimer's disease with or without cerebrovascular disease and vascular dementia in Thai patients.
Chankrachang, S; Nidhinandana, S; Phanthumchinda, K; Poungvarin, N; Praditsuwan, R; Senanarong, V; Thavichachart, N, 2009
)
0.35
"Galantamine, a centrally acting cholinesterase (ChE) inhibitor and a nicotinic allosteric potentiating ligand used to treat Alzheimer's disease, is an effective and safe antidote against poisoning with nerve agents, including soman."( Effectiveness of donepezil, rivastigmine, and (+/-)huperzine A in counteracting the acute toxicity of organophosphorus nerve agents: comparison with galantamine.
Adler, M; Akkerman, M; Albuquerque, EX; Aracava, Y; Pereira, EF, 2009
)
0.35
" Fewer donepezil-treated subjects withdrew due to adverse events (AEs) compared with rivastigmine and galantamine-treated subjects."( Safety and tolerability of donepezil, rivastigmine and galantamine for patients with Alzheimer's disease: systematic review of the 'real-world' evidence.
Kelly, S; Lockhart, IA; Mitchell, SA, 2009
)
0.35
" Their known adverse effects include bradycardia."( Bradycardia due to cholinesterase inhibitors: identify adverse effects and take them into account.
, 2011
)
0.37
"Diisopropylfluorophosphate exerts its toxic effect by irreversibly inhibiting acetylcholinesterase."( Galantamine as a preventive of diisopropylphosphorofluoridate toxicity effects in rat brain.
Pregelj, P; Saghafi, MM; Živin, M, 2013
)
0.39
" Compared with placebo, more dropouts and adverse events occurred with the cholinesterase inhibitors, but not with memantine."( Efficacy and safety of donepezil, galantamine, rivastigmine, and memantine for the treatment of Alzheimer's disease: a systematic review and meta-analysis.
Jiang, T; Meng, XF; Tan, CC; Tan, L; Tan, MS; Wang, C; Wang, HF; Yu, JT; Zhu, XC, 2014
)
0.4
" The outcome measurements were as follows: the changes of Alzheimer's Disease Assessment Scale-cognitive subscale (ADAS-cog), Mini-Mental State Examination (MMSE), Activities of Daily Living (ADL), Neuropsychiatric Inventory (NPI), Clinicians' Interview-Based Impression of Change with Caregiver's Input (CIBIC+), adverse effects and dropouts."( Efficacy and safety of galantamine treatment for patients with Alzheimer's disease: a meta-analysis of randomized controlled trials.
Jiang, D; Li, M; Wang, Y; Yang, X, 2015
)
0.42
"This survey analyzes two national pharmacovigilance databases in order to determine the major adverse reactions observed with the use of cholinesterase inhibitors in dementia."( Adverse Effects of Cholinesterase Inhibitors in Dementia, According to the Pharmacovigilance Databases of the United-States and Canada.
Abagyan, R; Ali, TB; Chen, WY; Reilly, BM; Schleret, TR, 2015
)
0.42
" Withdrawals due to adverse events and number of patients experiencing nausea, vomiting, diarrhoea and dizziness were examined as safety profiles."( The comparative efficacy and safety of cholinesterase inhibitors in patients with mild-to-moderate Alzheimer's disease: a Bayesian network meta-analysis.
Kobayashi, H; Nakagawa, R; Ohnishi, T; Yoshizawa, K, 2016
)
0.43
" Acetylcholinesterase inhibitors (AChEIs) aim to provide symptomatic benefit for cognitive decline, however these drugs are not without adverse events (AEs)."( Acetylcholinesterase inhibitors for treating dementia symptoms - a safety evaluation.
Bradley, J; Chan, P; Herrmann, N; Lanctôt, K; Mohammad, D, 2017
)
0.46
"The purpose of this study was to perform a comparative analysis of the number of reported pneumonia cases in individuals prescribed rivastigmine relative to the number of reported cases by patients using other therapeutics including over-the-counter drugs and other AD therapeutics, as reported to the FDA Adverse Event Reporting System (FAERS) database."( The Association Between Use of Rivastigmine and Pneumonia: Systematic Analysis of FDA Adverse Event Reporting System.
Bu, K; Cheng, F; Morris, R; Umeukeje, G, 2021
)
0.62
"Patients prescribed rivastigmine were more likely to report pneumonia as an adverse event than many drugs except galantamine."( The Association Between Use of Rivastigmine and Pneumonia: Systematic Analysis of FDA Adverse Event Reporting System.
Bu, K; Cheng, F; Morris, R; Umeukeje, G, 2021
)
0.62
"We aimed to perform an updated umbrella review to identify an efficacious and safe treatment for AD patients."( The Efficacy and Safety of Alzheimer's Disease Therapies: An Updated Umbrella Review.
Ai, Y; Cheng, Y; Fan, F; Liu, H; Liu, Q; Shi, X, 2022
)
0.72
" We examined the cognitive functions, behavioral symptoms, global clinical assessment, and Activities of Daily Living as efficacy endpoints, and the incidence of adverse events as safety profiles."( The Efficacy and Safety of Alzheimer's Disease Therapies: An Updated Umbrella Review.
Ai, Y; Cheng, Y; Fan, F; Liu, H; Liu, Q; Shi, X, 2022
)
0.72
"We included trials assessing cognition with the Mini-Mental State Examination (MMSE), and adverse events."( Comparative safety and efficacy of cognitive enhancers for Alzheimer's dementia: a systematic review with individual patient data network meta-analysis.
Ashoor, HM; Clarke, M; Hemmelgarn, BR; Holroyd-Leduc, J; Mavridis, D; Rios, P; Seitidis, G; Stewart, L; Straus, SE; Tricco, AC; Tudur-Smith, C; Veroniki, AA, 2022
)
0.72
" This study evaluated the risk of serious adverse events (SAEs) associated with individual ChEIs in older adults with dementia and also examined sex-based and dose-based effects on this risk."( Risk of Serious Adverse Events Associated With Individual Cholinesterase Inhibitors Use in Older Adults With Dementia: A Population-Based Cohort Study.
Aparasu, RR; Chatterjee, S; Chen, H; Johnson, ML; Masurkar, PP; Sherer, JT, 2022
)
0.72
"Dysphagia has been reported as an adverse event for patients receiving rivastigmine for Alzheimer's disease (AD) treatment."( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System.
Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022
)
0.72
"The purpose of this study was to determine the association between dysphagia and the usage of rivastigmine by using the pharmacovigilance data from the FDA Adverse Event Reporting System (FAERS)."( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System.
Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022
)
0.72
"When compared to patients prescribed donepezil, galantamine, or memantine, individuals prescribed rivastigmine were almost twice as likely to report dysphagia as an adverse event."( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System.
Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022
)
0.72
"Patients prescribed rivastigmine were at greater risk of reporting dysphagia as an adverse event than patients prescribed many other medicines."( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System.
Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022
)
0.72
"While these drugs are known to induce classic cholinergic adverse events such as diarrhea, their potential to cause psychiatric adverse events has yet to be thoroughly examined."( Psychiatric Adverse Events of Acetylcholinesterase Inhibitors in Alzheimer's Disease and Parkinson's Dementia: Systematic Review and Meta-Analysis.
Algharably, EEA; Bermpohl, F; Bittner, N; Brandl, EJ; Funk, CSM; Kreutz, R; Riemer, TG; Schmidt, A, 2023
)
0.91
"We sought to determine the risk of psychiatric adverse events associated with the use of AChEIs through a systematic review and meta-analysis of double-blind randomized controlled trials involving patients with Alzheimer's dementia and Parkinson's dementia."( Psychiatric Adverse Events of Acetylcholinesterase Inhibitors in Alzheimer's Disease and Parkinson's Dementia: Systematic Review and Meta-Analysis.
Algharably, EEA; Bermpohl, F; Bittner, N; Brandl, EJ; Funk, CSM; Kreutz, R; Riemer, TG; Schmidt, A, 2023
)
0.91
" Anorexia was the most commonly reported psychiatric adverse event, followed by agitation, insomnia, and depression."( Psychiatric Adverse Events of Acetylcholinesterase Inhibitors in Alzheimer's Disease and Parkinson's Dementia: Systematic Review and Meta-Analysis.
Algharably, EEA; Bermpohl, F; Bittner, N; Brandl, EJ; Funk, CSM; Kreutz, R; Riemer, TG; Schmidt, A, 2023
)
0.91
" Lowering the dose may resolve some psychiatric adverse events, as may switching to galantamine in the case of insomnia."( Psychiatric Adverse Events of Acetylcholinesterase Inhibitors in Alzheimer's Disease and Parkinson's Dementia: Systematic Review and Meta-Analysis.
Algharably, EEA; Bermpohl, F; Bittner, N; Brandl, EJ; Funk, CSM; Kreutz, R; Riemer, TG; Schmidt, A, 2023
)
0.91

Pharmacokinetics

Intravenous and oral 6-h blood sampling profiles in old and young rats revealed pharmacokinetic changes similar to those in humans. Galantamine bioavailability in brain by intranasal drug delivery through thiolated chitosan nanoparticles was compared to nasal and oral delivery.

ExcerptReferenceRelevance
" A biexponential decline of concentrations in plasma, with a terminal half-life of 43."( Galanthamine: pharmacokinetics, tissue distribution and cholinesterase inhibition in brain of mice.
Bickel, U; Fischer, JP; Kewitz, H; Thomsen, T; Weber, W, 1991
)
0.28
" The plasma AUC, Cmax, tmax and ka suggest that the subcutaneous and oral Nivalin formulations are bioequivalent."( Pharmacokinetics of galanthamine hydrobromide after single subcutaneous and oral dosage in humans.
Jovovich, V; Mihailova, D; Tencheva, J; Yamboliev, I; Zhivkova, Z, 1989
)
0.28
" Galanthamine has an elimination half-life of 40-50 min, a volume of distribution over 2 liters/kg, a plasma clearance of about 2 liters/h X kg and an oral bioavailability of about 65%."( Pharmacokinetics of galanthamine hydrobromide (Nivalin) following single intravenous and oral administration in rats.
Mihailova, D; Yamboliev, I, 1986
)
0.27
"The pharmacokinetic of some centrally acting cholinesterase inhibitors that have been used to improve memory in patients with dementia of Alzheimer's type, was compared."( Pharmacokinetic studies of cholinesterase inhibitors.
Johansson, M; Nordberg, A, 1993
)
0.29
" Specifically, certain metabolic parameters (ie, half-life and route of metabolism/elimination) can affect a drug's tolerability and become important when a switch from one agent to another is contemplated."( Pharmacokinetic profiles of current therapies for Alzheimer's disease: implications for switching to galantamine.
Farlow, MR, 2001
)
0.31
" The pharmacokinetic parameters of galantamine were similar in subjects with mild hepatic impairment compared with healthy controls."( Pharmacokinetics and safety of galantamine in subjects with hepatic impairment and healthy volunteers.
Iyer, GR; Truyen, L; Verhaeghe, T; Zhao, Q, 2002
)
0.31
" The mean plasma concentration-time profiles of galantamine were very similar after single doses of galantamine (4 and 8 mg), and there was an approximate dose proportionality of galantamine pharmacokinetic parameters in both Caucasian and Japanese ethnic groups."( Galantamine pharmacokinetics, safety, and tolerability profiles are similar in healthy Caucasian and Japanese subjects.
Brett, M; Huang, F; Hust, R; Raoult, A; Van Osselaer, N; Van Peer, A; Verhaeghe, T; Zhao, Q, 2002
)
0.31
"To explore the steady-state pharmacokinetic profile after coadministration of galantamine and risperidone, an open-label, randomized, single-center, two-way crossover drug-drug interaction study was conducted in 16 healthy elderly subjects, ages 60 years and older."( Pharmacokinetic and safety assessments of galantamine and risperidone after the two drugs are administered alone and together.
Huang, F; Janssens, L; Lasseter, KC; Lau, H; Verhaeghe, T; Zhao, Q, 2002
)
0.31
" Data from 15 clinical studies (1089 individuals, 7480 concentration measurements in total) were used to examine the effect of body size, demographic characteristics, and concomitant disease status on galantamine pharmacokinetic parameters."( Galantamine population pharmacokinetics in patients with Alzheimer's disease: modeling and simulations.
Aerssens, J; Armstrong, M; Piotrovsky, V; Van Osselaer, N; Van Peer, A, 2003
)
0.32
" Elimination half-life of galantamine was relatively large in rat and dog and smaller in mouse and rabbit."( Pharmacokinetics of galantamine, a cholinesterase inhibitor, in several animal species.
Bode, W; Lavrijsen, K; Meuldermans, W; Monbaliu, J; Verhaeghe, T; Willems, B, 2003
)
0.32
" Population pharmacokinetic modelling with galantamine has shown that the variables affecting clearance are age, sex, and bodyweight."( Clinical pharmacokinetics of galantamine.
Farlow, MR, 2003
)
0.32
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" The pharmacokinetic profile and parameters of galantamine at steady state were similar after administration of a 16-mg dose of galantamine once daily alone and after administration with a 10-mg dose of memantine twice daily."( Steady-state pharmacokinetics of galantamine are not affected by addition of memantine in healthy subjects.
Gold, M; Nye, JS; Padmanabhan, M; Ramael, S; Raoufinia, A; Verhaeghe, T; Walschap, Y; Yao, C; Zhao, Q, 2005
)
0.33
"To demonstrate using pharmacokinetic (PK) modeling and simulation, that the PK that the PK parameters for drug exposure with galantamine parameters for drug exposure with galantamine immediate-release (IR) tablet and galantamine extended-release (ER) capsule are comparable in patients with Alzheimer's disease (AD) during in patients with Alzheimer's disease (AD) during the switch from twice-daily IR tablet at steady state to the new once-daily ER capsule, and to support a recommendation that patients receiving the IR tablet at steady state can be successfully switched to the ER capsule at the same daily dosage with no titration period."( Pharmacokinetic simulation for switching from galantamine immediate-release to extended-release formulation.
Brashear, HR; Hing, JP; Kimko, H; Piotrovsky, V; Zhao, Q, 2005
)
0.33
" After steady state was achieved with ER galantamine, values for peak concentration and trough concentration were slightly lower (5% and 18%, respectively) than those seen at steady state for IR galantamine; this finding is considered to have no clinical implications."( Pharmacokinetic simulation for switching from galantamine immediate-release to extended-release formulation.
Brashear, HR; Hing, JP; Kimko, H; Piotrovsky, V; Zhao, Q, 2005
)
0.33
" Pharmacokinetic parameters of GAL at steady state were determined after morning intake on Day 7 of each treatment week."( Pharmacokinetics of extended-release and immediate-release formulations of galantamine at steady state in healthy volunteers.
Brashear, HR; Janssens, L; Truyen, L; Verhaeghe, T; Zhao, Q, 2005
)
0.33
" The treatment ratios and 90% confidence intervals for all above mentioned pharmacokinetic parameters demonstrated bioequivalence (with the range of 80-125%), indicating that food had no effect on GAL-ER bioavailability."( Pharmacokinetics of extended-release and immediate-release formulations of galantamine at steady state in healthy volunteers.
Brashear, HR; Janssens, L; Truyen, L; Verhaeghe, T; Zhao, Q, 2005
)
0.33
" From plasma concentrations, AUC(0-->t) (the area under the plasma concentration-time curve from time 0 to the last sampling time, 32 hr), AUC(0-->infinity) (the area under the plasma concentration-time curve from time 0 to infinity), t((1/2)) (elimination of half-life of the terminal log linear phase), C(max) (maximum plasma drug concentration) and T(max) (time to reach C(max)) were evaluated through noncompartmental pharmacokinetic analysis."( Pharmacokinetics and bioequivalence studies of galantamine hydrobromide dispersible tablet in healthy male Chinese volunteers.
Fang, XL; Han, LM; Li, XN; Sha, XY; Wang, QS; Zhang, LJ; Zhang, ZW, 2007
)
0.34
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" The elimination half-life of galantamine is about 7-8 hours."( A review of clinical pharmacokinetics and pharmacodynamics of galantamine, a reversible acetylcholinesterase inhibitor for the treatment of Alzheimer's disease, in healthy subjects and patients.
Fu, Y; Huang, F, 2010
)
0.36
" Intravenous and oral 6-h blood sampling profiles in old (30 months old) and young (7 months old) rats revealed pharmacokinetic changes similar to those in humans with an approximately 40% increase in C(max) of galantamine and prolonged t(1/2) (1."( Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
Aw, CC; Browne, ER; Chen, CP; Goh, CW; Lee, JH, 2011
)
0.37
" Hence, the effects of intranasal administration of GH loaded flexible liposomes have been investigated for the first time on the efficiency of acetylcholinesterase inhibition, as well as the pharmacokinetic behavior of GH in rat brain."( Pharmacokinetic behavior and efficiency of acetylcholinesterase inhibition in rat brain after intranasal administration of galanthamine hydrobromide loaded flexible liposomes.
Hao, B; Kong, P; Li, W; Wang, X; Zhao, N; Zhou, Y, 2012
)
0.38
" Donepezil, galantamine and rivastigmine are acetylcholinesterase inhibitors with different pharmacodynamic and pharmacokinetic profiles."( Pharmacodynamic, pharmacokinetic and pharmacogenetic aspects of drugs used in the treatment of Alzheimer's disease.
Eap, CB; Noetzli, M, 2013
)
0.39
" This novel method has been applied to a pharmacokinetic study in rats."( Highly sensitive LC-MS/MS method for determination of galantamine in rat plasma: application to pharmacokinetic studies in rats.
Mullangi, R; Sukumaran, SK; Suresh, PS, 2014
)
0.4
" The validated method was successfully applied to monitoring the concentrations and pharmacokinetic studies of two Amaryllidaceous alkaloids in rat plasma after an oral administration of Lycoris radiata extract."( An LC-MS/MS method for the simultaneous determination of lycorine and galanthamine in rat plasma and its application to pharmacokinetic study of Lycoris radiata extract in rats.
Huang, S; Liu, Y; Liu, YB; Zhou, X, 2014
)
0.4
"The present investigation was carried out to improve the galantamine bioavailability in brain by intranasal drug delivery through thiolated chitosan nanoparticles and compared to nasal and oral delivery of its solution using pharmacodynamic activity as well as biochemical estimation."( Nose to Brain Delivery of Galantamine Loaded Nanoparticles: In-vivo Pharmacodynamic and Biochemical Study in Mice.
Mishra, DN; Singh, SK, 2019
)
0.51
"05) as compared to oral and nasal administration of its solution, by pharmacodynamic study and biochemical estimation of acetylcholinesterase activity in Swiss albino mice brain."( Nose to Brain Delivery of Galantamine Loaded Nanoparticles: In-vivo Pharmacodynamic and Biochemical Study in Mice.
Mishra, DN; Singh, SK, 2019
)
0.51
" Cell-based oxidative stress assays and pharmacokinetic studies were performed using C6 glial cell lines, and Sprague Dawley rats, respectively."( Comparative evaluation of fish oil and butter oil in modulating delivery of galantamine hydrobromide to brain via intranasal route: pharmacokinetic and oxidative stress studies.
Katdare, A; Khunt, D; Misra, M; Polaka, SN; Thakkar, S, 2020
)
0.56
" Unfortunately, it showed a suboptimal pharmacokinetic profile, which required intracerebroventricular administration for in vivo studies."( Galantamine-memantine hybrids for Alzheimer's disease: The influence of linker rigidity in biological activity and pharmacokinetic properties.
Armirotti, A; Bartolini, M; Basagni, F; Bedeschi, M; Bertorelli, R; Bertozzi, SM; Bottegoni, G; Cavalli, A; Lembo, V; Mellor, IR; Minarini, A; Ortega, JA; Rosini, M; Summa, M, 2023
)
0.91

Compound-Compound Interactions

Galantamine (GAL) and nimodipine (NIM) in Alzheimer disease (AD) with cerebrovascular disease (mixed dementia) have not been explored. We investigated the effects of galantamine in patients with a diagnosis of probable vascular dementia.

ExcerptReferenceRelevance
" We investigated the effects of galantamine in patients with a diagnosis of probable vascular dementia or Alzheimer's disease combined with cerebrovascular disease."( Efficacy of galantamine in probable vascular dementia and Alzheimer's disease combined with cerebrovascular disease: a randomised trial.
Bullock, R; Damaraju, CV; Erkinjuntti, T; Gauthier, S; Kurz, A; Lilienfeld, S, 2002
)
0.31
"Cholinesterase inhibitors (ChEIs) could be involved in several drug-drug interactions (DDIs) because of their complex pharmacodynamic and/or pharmacokinetic properties."( Drug interactions with cholinesterase inhibitors: an analysis of the French pharmacovigilance database and a comparison of two national drug formularies (Vidal, British National Formulary).
Bagheri, H; Lapeyre-Mestre, M; Montrastruc, JL; Sommet, A; Tavassoli, N, 2007
)
0.34
"The effects of galantamine (GAL) on quality of life (QoL) and cognitive speed, as well its effects combined with nimodipine (NIM) in Alzheimer disease (AD) with cerebrovascular disease (mixed dementia), have not been explored."( Effects of galantamine and galantamine combined with nimodipine on cognitive speed and quality of life in mixed dementia: a 24-week, randomized, placebo-controlled exploratory trial (the REMIX study).
Barbosa, MT; Bottino, CM; Caramelli, P; Charchat-Fichman, H; Chaves, ML; Forlenza, OV; Laks, J; Lawson, FL; Machado, JC; Nitrini, R; Palmini, AL; Vale, Fde A, 2014
)
0.4

Bioavailability

The chronic ingestion of high doses of CAP will decrease the bioavailability of galantamine to a significant extent in rats. Memogain has more than 15-fold higher bioavailability in the brain than the same doses of Galantamine.

ExcerptReferenceRelevance
" Galanthamine has an elimination half-life of 40-50 min, a volume of distribution over 2 liters/kg, a plasma clearance of about 2 liters/h X kg and an oral bioavailability of about 65%."( Pharmacokinetics of galanthamine hydrobromide (Nivalin) following single intravenous and oral administration in rats.
Mihailova, D; Yamboliev, I, 1986
)
0.27
" The results showed that risperidone, when administered with galantamine, did not change the bioavailability of galantamine at steady state."( Pharmacokinetic and safety assessments of galantamine and risperidone after the two drugs are administered alone and together.
Huang, F; Janssens, L; Lasseter, KC; Lau, H; Verhaeghe, T; Zhao, Q, 2002
)
0.31
" Absolute oral bioavailability of a gavage dose was high in rat (77%) and dog (78%)."( Pharmacokinetics of galantamine, a cholinesterase inhibitor, in several animal species.
Bode, W; Lavrijsen, K; Meuldermans, W; Monbaliu, J; Verhaeghe, T; Willems, B, 2003
)
0.32
"5-10 mg/kg), galantamine was rapidly absorbed in both sexes, with an absolute oral bioavailability of 77%."( Pharmacokinetics and tissue distribution of galantamine and galantamine-related radioactivity after single intravenous and oral administration in the rat.
Bode, W; Geerts, R; Lavrijsen, K; Meuldermans, W; van Beijsterveldt, L; Verhaeghe, T; Willems, B, 2004
)
0.32
"To assess the steady-state galantamine (GAL) bioavailability of the extended-release 24-mg qd capsule (GAL-ER) with and without food and to evaluate the relative bioavailability of GAL-ER with the immediate-release 12-mg bid tablet (GAL-IR) at steady state."( Pharmacokinetics of extended-release and immediate-release formulations of galantamine at steady state in healthy volunteers.
Brashear, HR; Janssens, L; Truyen, L; Verhaeghe, T; Zhao, Q, 2005
)
0.33
"Food had no effect on the GAL bioavailability of GAL-ER at steady state."( Pharmacokinetics of extended-release and immediate-release formulations of galantamine at steady state in healthy volunteers.
Brashear, HR; Janssens, L; Truyen, L; Verhaeghe, T; Zhao, Q, 2005
)
0.33
" Pharmacokinetic testing in rats confirmed the improved drug bioavailability and demonstrated an in vitro-in vivo correlation."( In vitro formulation optimization of intranasal galantamine leading to enhanced bioavailability and reduced emetic response in vivo.
Brandt, GC; Costantino, HR; Foerder, CA; Leonard, AK; Quay, SC; Sileno, AP, 2007
)
0.34
" Memogain has more than 15-fold higher bioavailability in the brain than the same doses of galantamine."( Memogain is a galantamine pro-drug having dramatically reduced adverse effects and enhanced efficacy.
Hoeffle-Maas, A; Jordis, U; Koepke, AK; Ludwig, J; Maelicke, A; Maus, A; Samochocki, M, 2010
)
0.36
" The secondary objectives were: a) to verify Galantamine bioavailability through buccal delivery; b) to evaluate the permeation enhancement effect of iontophoresis; and, finally, c) to assess any histomorphological changes in the buccal mucosae after transbuccal delivery."( New prospectives in the delivery of galantamine for elderly patients using the IntelliDrug intraoral device: in vivo animal studies.
Campisi, G; De Caro, V; Florena, AM; Giannola, LI; Paderni, C; Wolff, A, 2010
)
0.36
" Oral bioavailability was improved by using syringe feeding with donepezil but not galantamine."( Alternative method of oral dosing for rats.
Atcha, Z; Aw, CC; Browne, ER; Goh, CW; Lim, JS; Neo, AH; Pemberton, DJ; Rourke, C, 2010
)
0.36
" These results demonstrate that the chronic ingestion of high doses of CAP will decrease the bioavailability of galantamine to a significant extent in rats."( Food-drug interactions: effect of capsaicin on the pharmacokinetics of galantamine in rats.
Lu, YN; Zhai, XJ, 2012
)
0.38
" Its poor brain penetration results in lower bioavailability to the target site."( Galantamine-loaded solid-lipid nanoparticles for enhanced brain delivery: preparation, characterization, in vitro and in vivo evaluations.
Chopra, K; Medhi, B; Misra, S; Sinha, VR, 2016
)
0.43
" Presence of drug in the olfactory bulb, in turn, increases the drug bioavailability in the brain and reduces the drug degradation as well as wastage of the drug through` systemic clearance."( Nose-to-brain drug delivery: An update on clinical challenges and progress towards approval of anti-Alzheimer drugs.
Agrawal, M; Alexander, A; Antimisiaris, SG; Chougule, MB; Saraf, S; Shoyele, SA, 2018
)
0.48
"The present investigation was carried out to improve the galantamine bioavailability in brain by intranasal drug delivery through thiolated chitosan nanoparticles and compared to nasal and oral delivery of its solution using pharmacodynamic activity as well as biochemical estimation."( Nose to Brain Delivery of Galantamine Loaded Nanoparticles: In-vivo Pharmacodynamic and Biochemical Study in Mice.
Mishra, DN; Singh, SK, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Therefore, to overcome such issues, various nanoformulations of nutraceuticals have been developed, that allow their effective delivery into the brain owing to reduced particle size, increased lipophilicity, increased bioavailability and avoidance of fast hepatic metabolism."( Nutraceuticals and their Derived Nano-Formulations for the Prevention and Treatment of Alzheimer's Disease.
Fazal, SA; Haque, SE; Iqubal, A; Iqubal, MK; Pottoo, FH, 2022
)
0.72
" In this study, a combination of several formulation factors was integrated and exploited to augment the bioavailability of galantamine hydrobromide (GAL) via the intranasal route."( Nose-to-brain delivery of galantamine loaded nanospray dried polyacrylic acid/taurodeoxycholate mixed matrix as a protective therapy in lipopolysaccharide-induced Alzheimer's in mice model.
Elhabak, M; Salama, AAA; Salama, AH, 2023
)
0.91

Dosage Studied

Galantamine drug-in-adhesive patches might be the alternative dosage form to have good efficacy and tolerability for the treatment of Alzheimer disease. Galantamine's adverse effects appear similar to those of other cholinesterase inhibitors.

ExcerptRelevanceReference
" In order to maximize and prolong positive drug effects, it is important to start early and adjust dosage during the treatment."( Cholinesterase inhibitors stabilize Alzheimer's disease.
Giacobini, E, 2000
)
0.31
" Galantamine's adverse effects appear similar to those of other cholinesterase inhibitors, in that it tends to produce gastrointestinal effects acutely and with dosage increases."( Galantamine for Alzheimer's disease.
Olin, J; Schneider, L, 2001
)
0.31
" Galantamine's adverse effects appear similar to those of other cholinesterase inhibitors, in that it tends to produce gastrointestinal effects acutely and with dosage increases."( Galantamine for Alzheimer's disease.
Olin, J; Schneider, L, 2001
)
0.31
" In addition, although there was not a statistically significant dose-response effect, doses above 8mg/d were, for the most part, consistently statistically significant."( Galantamine for Alzheimer's disease.
Olin, J; Schneider, L, 2001
)
0.31
" Excretion of radioactivity was rapid and nearly complete at 96 h after dosing in all species."( The metabolism and excretion of galantamine in rats, dogs, and humans.
Bode, W; Hendrickx, J; Lavrijsen, K; Le Jeune, L; Leempoels, J; Mannens, GS; Meuldermans, W; Snel, CA; van Beijsterveldt, L; Van Osselaer, N; Van Peer, A; Verhaeghe, T, 2002
)
0.31
" Galantamine's adverse effects appear similar to those of other cholinesterase inhibitors, in that it tends to produce gastrointestinal symptoms acutely and with dosage increases."( Galantamine for Alzheimer's disease.
Olin, J; Schneider, L, 2002
)
0.31
" In addition, although there was not a statistically significant dose-response effect, benefits associated with doses above 8mg/d were, for the most part, consistently statistically significant."( Galantamine for Alzheimer's disease.
Olin, J; Schneider, L, 2002
)
0.31
"Cholinesterase inhibitors (ChEIs) are dosed in two phases for the treatment of dementia, an initial dose-escalation phase to achieve a therapeutic dose and a maintenance phase where the therapeutic dose is given for long-term therapy."( The tolerability and safety of cholinesterase inhibitors in the treatment of dementia.
Inglis, F, 2002
)
0.31
" Parallel groups of healthy Japanese (n = 13; 6 males and 7 females)and Caucasian (n = 12; 6 males and 6 females) subjects matched for weight and age received single oral doses of galantamine 4 mg, or galantamine 8 mg, or placebo in a double-blind, three-way crossover trial according to a randomized dosing schedule."( Galantamine pharmacokinetics, safety, and tolerability profiles are similar in healthy Caucasian and Japanese subjects.
Brett, M; Huang, F; Hust, R; Raoult, A; Van Osselaer, N; Van Peer, A; Verhaeghe, T; Zhao, Q, 2002
)
0.31
" The recommended starting dosage is 4 mg (as the hydrobromide) twice daily."( Galantamine hydrobromide: an agent for Alzheimer's disease.
Cutler, NR; Sramek, JJ; Zarotsky, V, 2003
)
0.32
"1-1 microM), which correlates with the cerebrospinal fluid concentration of the drug at the recommended daily dosage of 16 to 24 mg."( Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors.
Albuquerque, EX; Christner, C; Fehrenbacher, A; Höffle, A; Jostock, R; Lübbert, H; Ludwig, J; Maelicke, A; Pereira, EF; Radina, M; Samochocki, M; Ullmer, C; Zerlin, M, 2003
)
0.32
" It is safe and very well tolerated when dosage is escalated gradually."( Update on Alzheimer drugs (galantamine).
Raskind, MA, 2003
)
0.32
" NMDA currents recorded in Mg2+-free media without addition of glycine were reversibly potentiated by bath and U-tube applications of galantamine at 10 to 10,000 nM, showing a bell-shaped dose-response relationship."( Mechanism of action of galantamine on N-methyl-D-aspartate receptors in rat cortical neurons.
Marszalec, W; Moriguchi, S; Narahashi, T; Yeh, JZ; Zhao, X, 2004
)
0.32
"The authors estimated the effects of each of the three commonly used drugs for Alzheimer disease (donepezil, galantamine, and rivastigmine) in terms of predefined clinical outcomes and trial completion rates, by dosing level, and described differences among them."( Metaanalysis of randomized trials of the efficacy and safety of donepezil, galantamine, and rivastigmine for the treatment of Alzheimer disease.
Ames, D; Clayton, T; Lai, R; Ritchie, CW,
)
0.13
" At concentrations that include their prescribed dosage ranges, donepezil (1-1000 nM) and galantamine (50-1000 nM) increase action potential-dependent dopamine release."( Cholinergic drugs for Alzheimer's disease enhance in vitro dopamine release.
Dani, JA; Zhang, L; Zhou, FM, 2004
)
0.32
" Three head-to-head trials of ChEIs in the treatment of AD have been published to date, but are limited due to their open-label design, rates of titration, and the drug dosage levels utilised."( The benefits and risks associated with cholinesterase inhibitor therapy in Alzheimer's disease.
Herrmann, N; Lanctôt, KL; Thompson, S, 2004
)
0.32
" Treatment with galantamine led to a significantly greater proportion of subjects with improved or unchanged global rating scale rating (k=7), at all dosing levels except for 8mg/d ."( Galantamine for Alzheimer's disease.
Loy, C; Schneider, L, 2004
)
0.32
" Although there was not a statistically significant dose-response effect, doses above 8mg/d were, for the most part, consistently statistically significant."( Galantamine for Alzheimer's disease.
Loy, C; Schneider, L, 2004
)
0.32
" Nefiracetam has been shown to potentiate ACh currents in the alpha4beta2 receptor of rat cortical neurons with a bell-shaped dose-response relationship and the maximum effect at 1 nM."( Mechanisms of action of cognitive enhancers on neuroreceptors.
Marszalec, W; Moriguchi, S; Narahashi, T; Yeh, JZ; Zhao, X, 2004
)
0.32
" Results demonstrated a robust dose-response relationship between ADAS-cog/11-K and galantamine dosage compared with baseline and controls at 16 weeks."( A prospective, double-blind, community-controlled comparison of three doses of galantamine in the treatment of mild to moderate Alzheimer's disease in a Korean population.
Choi, S; Ho Lee, J; Hong, I; Hoon Oh, B; Ju, YS; Jung, HY; Kil Yeon, B; Nam Bae, J; Park, J; Suh, GH; Uk Lee, C; Yeon Jung, H, 2004
)
0.32
" Higher dosages often did not exert beneficial effects in accordance with inverted U-shaped dose-response curves described for cholinomimetics."( Symptomatic effect of donepezil, rivastigmine, galantamine and memantine on cognitive deficits in the APP23 model.
Abramowski, D; De Deyn, PP; Staufenbiel, M; Van Dam, D, 2005
)
0.33
" The author provides information on recommended dosing for all three medications, noting that cholinesterase inhibitors must be titrated carefully."( Cholinesterase inhibitors in the treatment of dementia.
Ellis, JM, 2005
)
0.33
"To demonstrate using pharmacokinetic (PK) modeling and simulation, that the PK that the PK parameters for drug exposure with galantamine parameters for drug exposure with galantamine immediate-release (IR) tablet and galantamine extended-release (ER) capsule are comparable in patients with Alzheimer's disease (AD) during in patients with Alzheimer's disease (AD) during the switch from twice-daily IR tablet at steady state to the new once-daily ER capsule, and to support a recommendation that patients receiving the IR tablet at steady state can be successfully switched to the ER capsule at the same daily dosage with no titration period."( Pharmacokinetic simulation for switching from galantamine immediate-release to extended-release formulation.
Brashear, HR; Hing, JP; Kimko, H; Piotrovsky, V; Zhao, Q, 2005
)
0.33
" The once-daily dosage regimen of ER galantamine without a titration period should prove convenient for AD patients and their caregivers and should increase treatment compliance."( Pharmacokinetic simulation for switching from galantamine immediate-release to extended-release formulation.
Brashear, HR; Hing, JP; Kimko, H; Piotrovsky, V; Zhao, Q, 2005
)
0.33
"The primary objective of this study was to evaluate the efficacy and tolerability of a flexible dosing regimen (16 or 24 mg/day) of galantamine prolonged-release capsule (PRC) compared with placebo in subjects with mild to moderate Alzheimer's disease (AD)."( Galantamine prolonged-release formulation in the treatment of mild to moderate Alzheimer's disease.
Brodaty, H; Corey-Bloom, J; Damaraju, CR; Gold, M; Potocnik, FC; Truyen, L, 2005
)
0.33
" The treatment duration was 16 weeks with elevation of the drug dosage every 4 weeks--from 8mg to 12 mg twice a day."( [Reminyl efficacy in dementia with Levi bodies].
Levin, OS, 2005
)
0.33
" We hypothesized that cholinergic malfunction may underlie memory impairment in these subjects and applied a low dosage of an acetylcholinesterase inhibitor and modulator of nicotinic acetylcholine receptors, galantamine (4 mg bid), for 7 days."( Inhibition of hippocampal function in mild cognitive impairment: targeting the cholinergic hypothesis.
Brandenburg, I; Grön, G; Riepe, MW; Wunderlich, AP, 2006
)
0.33
" Treatment with galantamine led to a significantly greater proportion of subjects with improved or unchanged global rating scale rating (k = 8 studies), at all dosing levels except for 8 mg/d ."( Galantamine for Alzheimer's disease and mild cognitive impairment.
Loy, C; Schneider, L, 2006
)
0.33
" Although there was not a statistically significant dose-response effect, doses above 8 mg/d were, for the most part, consistently statistically significant."( Galantamine for Alzheimer's disease and mild cognitive impairment.
Loy, C; Schneider, L, 2006
)
0.33
" Sedation limited higher dosing in one patient, and a second patient experienced sedation and tremor."( Galantamine treatment of cognitive impairment in bipolar disorder: four cases.
Ghaemi, SN; Schrauwen, E, 2006
)
0.33
" The reminyl treatment has been conducted in dosage of 16 mg/kg daily during 6 months in 30 patients (20 female, 10 male) aged from 59 to 86 years."( [Use of reminyl (galantamine) in the treatment of dementia].
Lemeshko, ID; Mazal'skaia, OV; Petrukhin, AS; Pylaeva, OA; Voronkova, KV, 2006
)
0.33
" In addition, a formulation containing PYY(3-36) and TJM peptide was dosed intranasally in rabbits, resulting in a dramatic increase in bioavailability."( Therapeutic utility of a novel tight junction modulating peptide for enhancing intranasal drug delivery.
Chen, SC; Costantino, HR; Cui, K; Eiting, K; Farber, K; Houston, ME; Johnson, PH; Leonard, AK; Li, CY; Morris, D; Quay, SC; Sileno, AP, 2006
)
0.33
"This study compared dosing and utilization patterns of the cholinesterase inhibitors (ChEIs) donepezil, rivastigmine, and galantamine in the nursing home setting."( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis.
Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006
)
0.33
" The mean daily dosage of donepezil was above the effective dose throughout the study period, whereas the mean daily dosage was below the effective dose for the first 3 months with rivastigmine and did not approach the effective dose for galantamine until month 12."( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis.
Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006
)
0.33
"The results of this study suggest that early effective dosing occurred more often with donepezil than with rivastigmine or galantamine in these nursing home residents."( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis.
Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006
)
0.33
" In vivo studies in rats compared pharmacokinetic (PK) profiles of different formulations dosed intranasally."( In vitro formulation optimization of intranasal galantamine leading to enhanced bioavailability and reduced emetic response in vivo.
Brandt, GC; Costantino, HR; Foerder, CA; Leonard, AK; Quay, SC; Sileno, AP, 2007
)
0.34
" Nevertheless, whereas in the case of donepezil there seems to be a positive relation between the maximum dosage and response, for galanthamine doses above 24 mg/day do not seem to offer any improvement."( [Galanthamine versus donepezil in the treatment of Alzheimer's disease].
Garre-Olmo, J; López-Pousa, S; Vilalta-Franch, J,
)
0.13
" A 1-week titration may permit dosing flexibility and promote increased adherence to medication regimens."( One-week dose titration of extended release galantamine in patients with Alzheimer's disease.
Amatniek, J; Scharre, DW; Shiovitz, T; Zhu, Y, 2008
)
0.35
" We determine the effects of sub-chronic dosing of ChEIs on alpha7 and non-alpha7 nAChRs and determine if differences can be observed between them."( Effects of cholinesterase inhibitors on rat nicotinic receptor levels in vivo and in vitro.
Reid, RT; Sabbagh, MN, 2008
)
0.35
" Galantamine treatment increased calcium/calmodulin-dependent protein kinase II (CaMKII) and protein kinase Calpha (PKCalpha) activities with a bell-shaped dose-response curve peaked at 1 microM, thereby increasing the phosphorylation of AMPA receptor, myristoylated alanine-rich protein kinase C, and NMDA receptor as downstream substrates of CaMKII and/or PKCalpha."( Galantamine enhancement of long-term potentiation is mediated by calcium/calmodulin-dependent protein kinase II and protein kinase C activation.
Fukunaga, K; Han, F; Moriguchi, S; Narahashi, T; Shioda, N; Yeh, JZ, 2009
)
0.35
" Patients with moderate AD trended toward greater response with the 24 mg/day dosage than with the 16 mg/day dosage."( Optimal dosing of galantamine in patients with mild or moderate Alzheimer's disease: post Hoc analysis of a randomized, double-blind, placebo-controlled trial.
Aronson, S; Kavanagh, S; Schwalen, S; Van Baelen, B, 2009
)
0.35
"This post hoc analysis suggests that galantamine 16 mg/day is the optimal dosage for patients with mild AD, as similar efficacy is observed with the 24 mg/day dose."( Optimal dosing of galantamine in patients with mild or moderate Alzheimer's disease: post Hoc analysis of a randomized, double-blind, placebo-controlled trial.
Aronson, S; Kavanagh, S; Schwalen, S; Van Baelen, B, 2009
)
0.35
"Twenty-five patients with Alzheimer's disease (AD) in moderate-severe and severe stages received galantamine in dosage 8 mg daily during the 1st month with the following increasing to 16 mg daily."( [Galantamine (reminyl) in the treatment of severe Alzheimer's disease].
Gavrilova, SI; Kalyn, IaB; Kolykhanov, IV; Selezneva, ND, 2009
)
0.35
" A dose-response effect was observed for donepezil, with the highest-dose group at greatest risk (HR=2."( Cholinesterase inhibitors and incidence of bradycardia in patients with dementia in the veterans affairs new England healthcare system.
Cantor, MD; Farwell, W; Hernandez, RK; Lawler, EV, 2009
)
0.35
"05) tests as compared to those dosed with the vehicle."( Metabolic profiling of rat brain and cognitive behavioral tasks: potential complementary strategies in preclinical cognition enhancement research.
Atcha, Z; Aw, CC; Browne, ER; Chan, EC; Chen, WS; Goh, CW; Goh, DP; Neo, AH; New, LS, 2009
)
0.35
" We show that galantamine (1 pM-300 microM) inhibits selectively Islow, exhibiting a dual dose-response relationship, in both differentiated N1E-115 cells and CA1 neurones."( Galantamine inhibits slowly inactivating K+ currents with a dual dose-response relationship in differentiated N1E-115 cells and in CA1 neurones.
Costa, PF; Lima, PA; Vicente, MI, 2010
)
0.36
"The transbuccal delivery of drugs could assist several categories of chronic, especially elderly, patients in adhering to a correct dosage regimen."( New prospectives in the delivery of galantamine for elderly patients using the IntelliDrug intraoral device: in vivo animal studies.
Campisi, G; De Caro, V; Florena, AM; Giannola, LI; Paderni, C; Wolff, A, 2010
)
0.36
" The aim of this study was to assess an alternative oral dosing method that could reduce the distress and morbidity associated with standard gavage techniques."( Alternative method of oral dosing for rats.
Atcha, Z; Aw, CC; Browne, ER; Goh, CW; Lim, JS; Neo, AH; Pemberton, DJ; Rourke, C, 2010
)
0.36
" The 3 mg/kg dosage of galanthamine had the most significant inhibition on circulating TNF-alpha level at all the three tested doses."( Effect of cholinesterase inhibitor galanthamine on circulating tumor necrosis factor alpha in rats with lipopolysaccharide-induced peritonitis.
Gan, JX; Jiang, GY; Liu, ZH; Ma, YF; Wu, JS; Xu, SW, 2010
)
0.36
" The dosage of ChEI treatment could possibly lead to a different functional outcome."( Long-term outcome and prediction models of activities of daily living in Alzheimer disease with cholinesterase inhibitor treatment.
Londos, E; Minthon, L; Wallin, ÅK; Wattmo, C,
)
0.13
" The starting dosage was 8 mg once daily."( Evaluation of the effects of galantamine on cardiac function in elderly patients with Alzheimer's disease.
Bozoglu, E; Isik, AT; Kilic, S; Naharci, MI, 2010
)
0.36
" We demonstrate that a two-phase trial design in which drug dosing is administered after a certain level of disease severity has been reached, coupled with a method to account more accurately for the progression of the disease, may allow us to compensate for these factors, and thus enable us to make treatment effects more apparent."( A novel subject synchronization clinical trial design for Alzheimer's disease.
DiBernardo, A; Farnum, M; Lobanov, V; Narayan, V; Novak, G; Raghavan, N; Samtani, MN; Schultz, T; Shi, Y; Verbeeck, R; Yang, E, 2012
)
0.38
" The results suggest that the transdermal application of galantamine drug-in-adhesive patches might be the alternative dosage form to have good efficacy and tolerability for the treatment of Alzheimer disease."( Investigation of formulation factors affecting in vitro and in vivo characteristics of a galantamine transdermal system.
Ha, JM; Kim, JY; Oh, TO; Park, CW; Park, ES; Rhee, YS; Son, DD, 2012
)
0.38
"Socio-demographic characteristics and data on comorbidity, number of medications, type and dosage of CER, use of care, cognitive function, behaviour and nutritional status (weight, Body Mass Index (BMI)) were recorded at the time the diagnosis AD was made and at subsequent outpatient clinic visits."( Effect of long-term treatment with galantamine on weight of patients with Alzheimer's dementia.
Droogsma, E; Huinink, EJ; Schuur, T; van Asselt, DZ; van Steijn, JH, 2013
)
0.39
" Demographic variables, quantity and rate of prescriptions, dosage forms and strengths were analyzed."( [Drugs used for cognitive impairment. Analysis of 1.5 million prescriptions in Argentina].
Arizaga, RL; Demey, I; Rojas, G, 2013
)
0.39
" However, as an acetylcholinesterase inhibitor, gastrointestinal side effects limit the dosage and duration of treatment."( Nasal Application of the Galantamine Pro-drug Memogain Slows Down Plaque Deposition and Ameliorates Behavior in 5X Familial Alzheimer's Disease Mice.
Bhattacharya, S; Maelicke, A; Montag, D, 2015
)
0.42
" The strategy adopted included (a) in vitro biological assays, against eel AChE (EeAChE) and equine serum BuChE (EqBuChE) in order to determine the compounds IC50 and their dose-response activity, consolidated by (b) molecular docking studies to evaluate the docking poses and interatomic interactions in the case of the hit compounds, validated by STD-NMR studies."( New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives.
Arantes, S; Bacalhau, P; Burke, AJ; Caldeira, AT; Goth, A; Guarda, C; Marques, CS; Martins, R; Peixoto, D; San Juan, AA; Silva, M, 2016
)
0.43
" (summer snowflake) grown in Turkish habitats (Black Sea Region) and pharmaceutical dosage forms by capillary zone electrophoresis with direct UV detection form."( Development and validation of a capillary zone electrophoretic method for rapid and sensitive determination of galanthamine: Application in plant and pharmaceuticals.
Bulduk, I; Ozkan, SA; Ozkurt, H; Sanli, N; Şanli, S, 2016
)
0.43
" To select sub-efficacious doses of both drugs, dose-response studies were first performed on the scopolamine-induced deficits of spontaneous alternation in the Y-maze task and of acquisition and retrieval processes in a passive avoidance task."( Co-modulation of an allosteric modulator of nicotinic receptor-cholinesterase inhibitor (galantamine) and a 5-HT4 receptor agonist (RS-67333): effect on scopolamine-induced memory deficit in the mouse.
Boulouard, M; Dauphin, F; Freret, T; Hamidouche, K; Lecouflet, P; Lelong-Boulouard, V, 2017
)
0.46
" We therefore hypothesize a combinatorial antioxidant-metal-chelator approach by formulating a single dosage form that has the ability to prevent the formation of free radicals, plaques and accumulation of iron in the brain."( Hypothesis: apo-lactoferrin-Galantamine Proteo-alkaloid Conjugate for Alzheimer's disease Intervention.
Akilo, OD; Choonara, YE; du Toit, LC; Kumar, P; Pillay, V; Pradeep, P, 2018
)
0.48
" However, it exhibits poor brain penetration, low intestinal permeation and requires frequent dosing in AD treatment."( QbD-steered development of mixed nanomicelles of galantamine: Demonstration of enhanced brain uptake, prolonged systemic retention and improved biopharmaceutical attributes.
Beg, S; Dhull, D; Kumar, A; Lohan, S; Raza, K; Saini, S; Sharma, T; Singh, B; Swami, R, 2021
)
0.62
"0 mg/kg), donepezil tended to promote depression-like behavior, suggesting a u-shaped dose-response curve for FST immobility."( Multiple cholinesterase inhibitors have antidepressant-like properties in the mouse forced swim test.
Fitzgerald, PJ; Ghimire, A; Hale, PJ; Watson, BO, 2021
)
0.62
"These baseline-dependent nicotinic effects on early auditory information processing warrant different dosage and repeated administration assessments in patients with low baseline deviance detection levels."( An α7 nAChR approach for the baseline-dependent modulation of deviance detection in schizophrenia: A pilot study assessing the combined effect of CDP-choline and galantamine.
Blais, CM; Choueiry, J; Fisher, D; Knott, V; Labelle, A; Shah, D; Smith, D, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
antidote to curare poisoningA role borne by a molecule that acts to counteract or neutralize the deleterious effects of curare.
EC 3.1.1.7 (acetylcholinesterase) inhibitorAn EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of enzyme acetylcholinesterase (EC 3.1.1.7), which helps breaking down of acetylcholine into choline and acetic acid.
cholinergic drugAny drug used for its actions on cholinergic systems. Included here are agonists and antagonists, drugs that affect the life cycle of acetylcholine, and drugs that affect the survival of cholinergic neurons.
EC 3.1.1.8 (cholinesterase) inhibitorAn EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of cholinesterase (EC 3.1.1.8).
plant metaboliteAny eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
alkaloidAny of the naturally occurring, basic nitrogen compounds (mostly heterocyclic) occurring mostly in the plant kingdom, but also found in bacteria, fungi, and animals. By extension, certain neutral compounds biogenetically related to basic alkaloids are also classed as alkaloids. Amino acids, peptides, proteins, nucleotides, nucleic acids, amino sugars and antibiotics are not normally regarded as alkaloids. Compounds in which the nitrogen is exocyclic (dopamine, mescaline, serotonin, etc.) are usually classed as amines rather than alkaloids.
benzazepine alkaloid
benzazepine alkaloid fundamental parent
organic heterotetracyclic compound
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

PathwayProteinsCompounds
Amaryllidacea alkaloids biosynthesis225
Amaryllidacea alkaloids biosynthesis236

Protein Targets (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency29.09290.000811.382244.6684AID686978
67.9K proteinVaccinia virusPotency0.89130.00018.4406100.0000AID720579
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency0.50120.251215.843239.8107AID504327
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency15.84890.011212.4002100.0000AID1030
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.12510.354828.065989.1251AID504847
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, ACETYLCHOLINESTERASETetronarce californica (Pacific electric ray)IC50 (µMol)0.65200.65200.65200.6520AID977608
Chain A, AcetylcholinesteraseTetronarce californica (Pacific electric ray)IC50 (µMol)0.36000.36000.36000.3600AID977608
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50 (µMol)3.66100.00000.94539.9400AID1063992; AID1073062; AID1077144; AID1129233; AID1140465; AID1167622; AID1230202; AID1246442; AID1267380; AID1273004; AID1315225; AID1317852; AID1322224; AID1328951; AID1335318; AID1337747; AID1339189; AID1389180; AID1400271; AID1426027; AID1427875; AID1466563; AID1466635; AID1491305; AID1493769; AID1498442; AID1498899; AID1507309; AID1557015; AID1593770; AID1594568; AID1597699; AID1636642; AID1780622; AID1796450; AID1797820; AID1800998; AID1801040; AID1801810; AID1801887; AID1802055; AID1802058; AID1802583; AID1802597; AID1802939; AID1802975; AID1854483; AID1861404; AID256692; AID260079; AID271048; AID284418; AID302143; AID30543; AID30544; AID307545; AID315115; AID378482; AID383197; AID421514; AID456905; AID479753; AID480448; AID482856; AID486994; AID514203; AID526489; AID527152; AID569581; AID593738; AID603787; AID635414; AID656680; AID666573; AID726768; AID730448; AID747035; AID749373; AID752001; AID754043; AID765550; AID776491
AcetylcholinesteraseElectrophorus electricus (electric eel)Ki1.29760.00121.25638.9000AID1564162; AID256692; AID260079; AID499448; AID726768
Bile salt export pumpHomo sapiens (human)IC50 (µMol)134.00000.11007.190310.0000AID1443980; AID1473738
AcetylcholinesteraseTetronarce californica (Pacific electric ray)IC50 (µMol)0.48800.00570.42855.1200AID1796450; AID1796451; AID1797820; AID294501; AID30666; AID343772; AID404434
AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki16.09500.00000.76714.3000AID1799683
CholinesteraseHomo sapiens (human)IC50 (µMol)681.19870.00001.559910.0000AID1140466; AID1162590; AID1179994; AID1331321; AID1356517; AID1406252; AID1443224; AID1472441; AID1493770; AID1524946; AID1537270; AID1545272; AID1567163; AID1570261; AID1646342; AID1657596; AID1736860; AID1739254; AID1779364; AID1796482; AID1796572; AID1797821; AID1799735; AID1802080; AID1807566; AID1865085; AID1872733; AID276346; AID298279; AID302144; AID345206; AID362528; AID365699; AID407781; AID422296; AID594821; AID724167; AID746378
CholinesteraseHomo sapiens (human)Ki9.55830.00001.51739.7300AID1186579; AID1312278; AID694074
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)12.73000.00011.753610.0000AID1322224
Vascular endothelial growth factor receptor 1 Homo sapiens (human)IC50 (µMol)0.59000.00010.29147.0000AID263610
AcetylcholinesteraseMus musculus (house mouse)IC50 (µMol)2.29000.00071.11818.4000AID1066955; AID1175427
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)27.82150.00000.933210.0000AID1054126; AID1066956; AID1070090; AID1127083; AID1129497; AID1162589; AID1176926; AID1179993; AID1237656; AID1254737; AID1272326; AID1301459; AID1332254; AID1350115; AID1356515; AID1406251; AID1443223; AID1472442; AID1501977; AID1507310; AID1524945; AID1537269; AID1545271; AID1556710; AID1567161; AID1646341; AID1657594; AID1678836; AID1682145; AID1736859; AID1739253; AID1779363; AID1796482; AID1796572; AID1797820; AID1802080; AID1807563; AID1853195; AID1865084; AID1872732; AID241692; AID262754; AID263610; AID276345; AID281636; AID298278; AID31036; AID311339; AID31163; AID345205; AID362527; AID365698; AID378483; AID381366; AID407780; AID422295; AID446351; AID482855; AID566361; AID568572; AID594820; AID600978; AID600980; AID625193; AID656684; AID670563; AID676724; AID724168; AID729911; AID746379; AID746749
AcetylcholinesteraseHomo sapiens (human)Ki0.16850.00001.27869.7300AID1186578; AID1231568; AID501440; AID694073
Acetylcholinesterase Bos taurus (cattle)IC50 (µMol)4.53000.00000.61068.7000AID1797820; AID462833
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)8.39730.00010.729810.0000AID276346
Vascular endothelial growth factor receptor 3Homo sapiens (human)IC50 (µMol)0.59000.00010.22644.9000AID263610
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC50 (µMol)0.59000.00000.48308.8000AID263610
AcetylcholinesteraseRattus norvegicus (Norway rat)IC50 (µMol)0.80060.00020.52597.2000AID31964; AID31968; AID32105; AID333566; AID416453
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)3.20000.00030.71237.0700AID514203
Prolyl endopeptidaseHomo sapiens (human)IC50 (µMol)200.00000.00111.98969.7500AID1537274
Small conductance calcium-activated potassium channel protein 3Rattus norvegicus (Norway rat)IC50 (µMol)12.70000.00151.68587.0000AID754042
CholinesteraseEquus caballus (horse)IC50 (µMol)15.92950.00002.22149.4000AID1063991; AID1070089; AID1077145; AID1129234; AID1140466; AID1167623; AID1246443; AID1267381; AID1273007; AID1293781; AID1315224; AID1317853; AID1335319; AID1337749; AID1339190; AID1389181; AID1400272; AID1466564; AID1466636; AID1491306; AID1498443; AID1498900; AID1593769; AID1594569; AID1597702; AID1636643; AID1780623; AID1854475; AID1861405; AID421515; AID456906; AID462834; AID479754; AID480449; AID482854; AID486995; AID566384; AID569582; AID603880; AID666575; AID670564; AID729524; AID730447; AID746748; AID749372; AID752000; AID754042; AID765549; AID776489
CholinesteraseEquus caballus (horse)Ki7.70000.00203.45989.3700AID1564164
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Carboxylic ester hydrolase Equus caballus (horse)IC50 (µMol)11.45880.00512.69848.5000AID260080; AID271049; AID294502; AID307546; AID383199; AID593739; AID635415
Carboxylic ester hydrolase Equus caballus (horse)Ki8.00000.00200.95708.0000AID260080
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AcetylcholinesteraseHomo sapiens (human)EC50 (µMol)1.10000.01900.57551.1400AID73711
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AcetylcholinesteraseHomo sapiens (human)MIC0.00000.00000.00000.0000AID550178
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (164)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
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)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 1 Homo sapiens (human)
monocyte chemotaxisVascular endothelial growth factor receptor 1 Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of phospholipase C activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
cell migrationVascular endothelial growth factor receptor 1 Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 1 Homo sapiens (human)
cell differentiationVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 1 Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 1 Homo sapiens (human)
vascular endothelial growth factor receptor-1 signaling pathwayVascular endothelial growth factor receptor 1 Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of MAP kinase activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of angiogenesisVascular endothelial growth factor receptor 1 Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 1 Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 1 Homo sapiens (human)
blood vessel morphogenesisVascular endothelial growth factor receptor 1 Homo sapiens (human)
embryonic morphogenesisVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionVascular endothelial growth factor receptor 1 Homo sapiens (human)
negative regulation of vascular endothelial cell proliferationVascular endothelial growth factor receptor 1 Homo sapiens (human)
hyaloid vascular plexus regressionVascular endothelial growth factor receptor 1 Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 1 Homo 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)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of protein phosphorylationVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of endothelial cell proliferationVascular endothelial growth factor receptor 3Homo sapiens (human)
vasculature developmentVascular endothelial growth factor receptor 3Homo sapiens (human)
lymph vessel developmentVascular endothelial growth factor receptor 3Homo sapiens (human)
lymphangiogenesisVascular endothelial growth factor receptor 3Homo sapiens (human)
sprouting angiogenesisVascular endothelial growth factor receptor 3Homo sapiens (human)
respiratory system processVascular endothelial growth factor receptor 3Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of endothelial cell migrationVascular endothelial growth factor receptor 3Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 3Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 3Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 3Homo sapiens (human)
negative regulation of apoptotic processVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of JNK cascadeVascular endothelial growth factor receptor 3Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 3Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 3Homo sapiens (human)
lung alveolus developmentVascular endothelial growth factor receptor 3Homo sapiens (human)
blood vessel morphogenesisVascular endothelial growth factor receptor 3Homo sapiens (human)
regulation of blood vessel remodelingVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of protein kinase C signalingVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 3Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 3Homo sapiens (human)
regulation of MAPK cascadeVascular endothelial growth factor receptor 3Homo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 3Homo sapiens (human)
branching involved in blood vessel morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of macroautophagyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial depolarizationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial fissionVascular endothelial growth factor receptor 2Homo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
ovarian follicle developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of protein phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
lymph vessel developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell maturationVascular endothelial growth factor receptor 2Homo sapiens (human)
endocardium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of cell shapeVascular endothelial growth factor receptor 2Homo sapiens (human)
mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of gene expressionVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of BMP signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
embryonic hemopoiesisVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor-2 signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
surfactant homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of neuron apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
cell fate commitmentVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
lung alveolus developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
post-embryonic camera-type eye morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of positive chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of focal adhesion assemblyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionVascular endothelial growth factor receptor 2Homo sapiens (human)
calcium ion homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
blood vessel endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular wound healingVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
semaphorin-plexin signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of hematopoietic progenitor cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of bone developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to hydrogen sulfideVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of endothelial cell apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
proteolysisProlyl endopeptidaseHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (73)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
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)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 1 Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 1 Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 1 Homo sapiens (human)
placental growth factor receptor activityVascular endothelial growth factor receptor 1 Homo 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)
amyloid-beta bindingAcetylcholinesterase Bos taurus (cattle)
protein bindingAcetylcholinesterase Bos taurus (cattle)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 3Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 3Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 3Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 3Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 3Homo sapiens (human)
protein phosphatase bindingVascular endothelial growth factor receptor 3Homo sapiens (human)
protein homodimerization activityVascular endothelial growth factor receptor 3Homo sapiens (human)
protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
integrin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
coreceptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
identical protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
cadherin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
Hsp90 protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
serine-type endopeptidase activityProlyl endopeptidaseHomo sapiens (human)
protein bindingProlyl endopeptidaseHomo sapiens (human)
serine-type peptidase activityProlyl endopeptidaseHomo sapiens (human)
oligopeptidase activityProlyl endopeptidaseHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (44)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
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)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
extracellular spaceVascular endothelial growth factor receptor 1 Homo sapiens (human)
endosomeVascular endothelial growth factor receptor 1 Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 1 Homo sapiens (human)
focal adhesionVascular endothelial growth factor receptor 1 Homo sapiens (human)
actin cytoskeletonVascular endothelial growth factor receptor 1 Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 1 Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 1 Homo 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)
synapseAcetylcholinesterase Bos taurus (cattle)
side of membraneAcetylcholinesterase Bos taurus (cattle)
extracellular regionVascular endothelial growth factor receptor 3Homo sapiens (human)
nucleoplasmVascular endothelial growth factor receptor 3Homo sapiens (human)
cytosolVascular endothelial growth factor receptor 3Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 3Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 3Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 3Homo sapiens (human)
extracellular regionVascular endothelial growth factor receptor 2Homo sapiens (human)
nucleusVascular endothelial growth factor receptor 2Homo sapiens (human)
endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
early endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
endoplasmic reticulumVascular endothelial growth factor receptor 2Homo sapiens (human)
Golgi apparatusVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
external side of plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
cell junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
membrane raftVascular endothelial growth factor receptor 2Homo sapiens (human)
anchoring junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
sorting endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 2Homo sapiens (human)
nucleusProlyl endopeptidaseHomo sapiens (human)
cytoplasmProlyl endopeptidaseHomo sapiens (human)
cytosolProlyl endopeptidaseHomo sapiens (human)
membraneProlyl endopeptidaseHomo sapiens (human)
cytosolProlyl endopeptidaseHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (585)

Assay IDTitleYearJournalArticle
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID44417Ratio of inhibitory activity against butyrylcholinesterase (BChE) to that of acetylcholinesterase (AChE)2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and structure-activity relationships of open D-Ring galanthamine analogues.
AID256692Inhibitory activity AChE from Electrophorus electricus using ATCh substrate and DTNB by spectrophotometry2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Synthesis of tricyclic 1,3-oxazin-4-ones and kinetic analysis of cholesterol esterase and acetylcholinesterase inhibition.
AID271048Inhibition of electric eel AChE2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase.
AID307546Inhibition of equine serum BuChE2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors.
AID1507318Inhibition of equine serum BChE at 1 mM2017European journal of medicinal chemistry, Aug-18, Volume: 136Discorhabdin alkaloids from Antarctic Latrunculia spp. sponges as a new class of cholinesterase inhibitors.
AID499448Competitive inhibition of Electrophorus electricus AChE by Lineweaver-Burke plot analysis2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Multipotent drugs with cholinergic and neuroprotective properties for the treatment of Alzheimer and neuronal vascular diseases. I. Synthesis, biological assessment, and molecular modeling of simple and readily available 2-aminopyridine-, and 2-chloropyri
AID1070090Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Ionic liquid mediated synthesis of mono- and bis-spirooxindole-hexahydropyrrolidines as cholinesterase inhibitors and their molecular docking studies.
AID48733Maximum reversal of vecuronium-induced neuromuscular block in-vivo in anaesthetised cats; NT denotes not tested2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
AID480448Inhibition of electric eel AChE by modified Ellman's method2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents.
AID1076766Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 1 uM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay relat2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1350115Inhibition of human erythrocyte AChE using S-acetylthiocholine iodide as substrate pretreated for 20 mins followed by substrate addition measured after 30 mins by Ellman's method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Mucroniferanines A-G, Isoquinoline Alkaloids from Corydalis mucronifera.
AID1498449Inhibition of electric eel AChE at 12.5 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1406251Inhibition of AChE (unknown origin)2018European journal of medicinal chemistry, Aug-05, Volume: 156Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.
AID749371Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Microwave assisted synthesis, cholinesterase enzymes inhibitory activities and molecular docking studies of new pyridopyrimidine derivatives.
AID1567160Inhibition of human recombinant AChE at 25 uM using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's spectrophotometric method relative to control2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
AID1271111Inhibition of BuChE (unknown origin) using butyrylthiocholine iodide as substrate by Ellman spectrophotometric method2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and evaluation of bis-thiazole derivatives as new anticancer agents.
AID569581Inhibition of electric eel AChE by Ellman's method2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Probing the mid-gorge of cholinesterases with spacer-modified bivalent quinazolinimines leads to highly potent and selective butyrylcholinesterase inhibitors.
AID376663Inhibition of AChE2006Journal of natural products, May, Volume: 69, Issue:5
Bioactive diterpenes from the fruits of Detarium microcarpum.
AID593737Ratio of IC50 for equine serum Butyrylcholinesterase to IC50 for electric eel Acetylcholinesterase2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors.
AID1466636Inhibition of horse serum BChE using butyrylcholine chloride as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric method2017Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13
Antioxidant and anticholinesterase potential of diterpenoid alkaloids from Aconitum heterophyllum.
AID1556703Inhibition of AChE in human erythrocytes using acetylthiocholine iodide as substrate at 100 uM preincubated with enzyme for 10 mins followed by substrate addition measured for 15 mins by Ellman's method relative to control2019European journal of medicinal chemistry, Oct-01, Volume: 179Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.
AID108857Active dose for reversal of Scopolamine dementia(SDDA) activity in mouse administered subcutaneously1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Synthesis and evaluation of 5-amino-5,6,7,8-tetrahydroquinolinones as potential agents for the treatment of Alzheimer's disease.
AID600980Inhibition of human erythrocytes BChE2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
AID1498899Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition 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.
AID603880Inhibition of equine serum BChE by colorimetric Ellman's assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Mycobacterium tuberculosis and cholinesterase inhibitors from Voacanga globosa.
AID729911Inhibition of AChE (unknown origin) using acetylthiocholine iodide substrate by Ellman's method based spectrophotometry2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and discovery of novel piperidone-grafted mono- and bis-spirooxindole-hexahydropyrrolizines as potent cholinesterase inhibitors.
AID362527Inhibition of acetylcholinesterase2008Journal of natural products, Aug, Volume: 71, Issue:8
Bioactive 5alpha-pregnane-type steroidal alkaloids from Sarcococca hookeriana.
AID437947Antibacterial activity against Bacillus subtilis after 18 hrs2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1315224Inhibition of equine serum BuChE using ATCI as substrate preincubated for 30 mins followed by substrate addition measured after 5 mins by DTNB-based spectrophotometric analysis2016Journal of natural products, 05-27, Volume: 79, Issue:5
Alkaloids from Hippeastrum argentinum and Their Cholinesterase-Inhibitory Activities: An in Vitro and in Silico Study.
AID1646341Inhibition of AChE (unknown origin)2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Design, synthesis and cholinesterase inhibitory activity of novel spiropyrrolidine tethered imidazole heterocyclic hybrids.
AID1507309Inhibition of electric eel AChE2017European journal of medicinal chemistry, Aug-18, Volume: 136Discorhabdin alkaloids from Antarctic Latrunculia spp. sponges as a new class of cholinesterase inhibitors.
AID1077156Neuroprotective activity in rat PC12 cells assessed as decrease in amyloid beta (1 to 42)-induced cytotoxicity at 0.08 to 10 uM after 24 hrs by MTT assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents.
AID639464Neuroprotective activity against okadaic acid-induced cell death in human SH-SY5Y cells assessed as LDH release at 0.3 uM treated 24 hrs before okadaic acid challenge measured after 24 hrs relative to control2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1498455Inhibition of electric eel AChE at 0.098 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1578097Antitrypanosomal activity against Leishmania donovani2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID1545272Inhibition of human Cholinesterase2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID1066956Inhibition of AChE (unknown origin) using 2-nitrobenzoate-5-mercaptothiocholine as substrate after 15 to 60 mins by microplate assay2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Synthesis of aminoalkyl-substituted coumarin derivatives as acetylcholinesterase inhibitors.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID729526Selectivity index, ratio of IC50 for AChE (unknown origin) to IC50 for equine serum BuChE2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and discovery of novel piperidone-grafted mono- and bis-spirooxindole-hexahydropyrrolizines as potent cholinesterase inhibitors.
AID527152Inhibition of electric eel AChE by Ellman's method2010Journal of natural products, Oct-22, Volume: 73, Issue:10
Characterization of Acetylcholinesterase Inhibitory Constituents from Annona glabra Assisted by HPLC Microfractionation.
AID1076772Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 10 nM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 242014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID676724Inhibition of human AChE pre-incubated for 10 mins before acetylthiocholine iodide substrate addition2012Journal of natural products, Jul-27, Volume: 75, Issue:7
Geranylphenazinediol, an acetylcholinesterase inhibitor produced by a Streptomyces species.
AID1301458Inhibition AChE (unknown origin) using ATCI as substrate assessed as hydrolysis of ATCI at 5 uM measured every 1 min for 10 times2016Journal of natural products, Feb-26, Volume: 79, Issue:2
Bioactive Constituents of Glycyrrhiza uralensis (Licorice): Discovery of the Effective Components of a Traditional Herbal Medicine.
AID1337749Inhibition of horse serum BChE pretreated for 20 mins followed by butyrylthiocholine iodide substrate addition measured for 5 mins by Ellman's method2017European journal of medicinal chemistry, Jan-05, Volume: 125New azepino[4,3-b]indole derivatives as nanomolar selective inhibitors of human butyrylcholinesterase showing protective effects against NMDA-induced neurotoxicity.
AID48700Mean arterial pressure change was detected in anaesthetised cats on administration of the compound2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
AID437950Antioxidant activity in Wistar rat brain assessed as catalase content2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID746377Inhibition of BuChE (unknown origin) at 10 uM by Ellman method2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease.
AID666578Selectivity ratio of IC50 for equine serum butyrylcholinesterase to IC50 for electric eel acetylcholine esterase2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents.
AID1807563Inhibition of human AChE using acetylthiocholine as substrate by Ellman's method2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID1272326Inhibition of human acetylcholine esterase preincubated for 10 mins followed by the addition of 550 uM of acetylcholine iodide as substrate measured after 20 mins by Ellman's method2016European journal of medicinal chemistry, Jan-27, Volume: 108Cardanol-derived AChE inhibitors: Towards the development of dual binding derivatives for Alzheimer's disease.
AID416455Selectivity ratio of IC50 for rat serum BChE to IC50 for rat cortex AChE2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.
AID1179993Inhibition of AChE (unknown origin)2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Coumarin hybrids as novel therapeutic agents.
AID1077153Inhibition of amyloid beta (1 to 42) aggregation (unknown origin) at 5 to 100 uM after 1 hr by thioflavin T fluorescence assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents.
AID1501977Inhibition of AChE (unknown origin)2017Journal of natural products, 09-22, Volume: 80, Issue:9
Acetylcholinesterase Inhibitory Alkaloids from the Whole Plants of Zephyranthes carinata.
AID1493769Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 15 mins followed by substrate addition measured after 5 mins by Ellman's method2018European journal of medicinal chemistry, Jan-01, Volume: 1432-Arylbenzofurans from Artocarpus lakoocha and methyl ether analogs with potent cholinesterase inhibitory activity.
AID383197Inhibition of electric eel AChE type 6S by Ellman's assay2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Design, synthesis and pharmacological evaluation of hybrid molecules out of quinazolinimines and lipoic acid lead to highly potent and selective butyrylcholinesterase inhibitors with antioxidant properties.
AID1854483Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pre-incubated for 5 mins followed by substrate addition and measured after 6 mins by Ellman's method2022European journal of medicinal chemistry, Nov-05, Volume: 241New naphtho/thienobenzo-triazoles with interconnected anti-inflammatory and cholinesterase inhibitory activity.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1129497Inhibition of human AChE by spectrophotometry2014Journal of natural products, Apr-25, Volume: 77, Issue:4
Alkaloids from the roots of Stichoneuron caudatum and their acetylcholinesterase inhibitory activities.
AID302144Inhibition of human serum BuChE by Ellman's method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.
AID1267380Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents.
AID1646344Selectivity ratio of IC50 for AChE (unknown origin) to IC50 for BChE (unknown origin)2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Design, synthesis and cholinesterase inhibitory activity of novel spiropyrrolidine tethered imidazole heterocyclic hybrids.
AID716206Selectivity index, ratio of IC50 for electric eel AChE to horse BChE2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo.
AID31163Ex vivo inhibition of human erythrocyte Acetylcholinesterase.2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
AID1524947Selectivity index, ratio of IC50 for inhibition of AChE (unknown origin) to IC50 for inhibition of BChE (unknown origin)2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.
AID1537269Inhibition of human AChE using acetylthiocholine iodide as substrate measured for 1 min by Ellman's method2019Journal of natural products, 02-22, Volume: 82, Issue:2
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.
AID276345Inhibition of AChE2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
AID1077158Antialzheimer activity in Wistar rat scopolamine-induced cognition impairment model assessed as total exploration time at 1 umol/100 g body weight, ip treated for 5 mins prior to scopolamine-challenge by eight-arm radial maze test relative to control2014European journal of medicinal chemistry, Apr-09, Volume: 76Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents.
AID437944Inhibition of catalase in Wistar rat brain2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1578098Antitrypanosomal activity against Trypanosoma brucei rhodesiense2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID1129237Selectivity ratio of IC50 for electric eel AChE to IC50 for equine serum BChE2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and discovery of highly functionalized mono- and bis-spiro-pyrrolidines as potent cholinesterase enzyme inhibitors.
AID1537277Permeability of the compound after 2.45 hrs by PAMPA2019Journal of natural products, 02-22, Volume: 82, Issue:2
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.
AID1175431Reversal of scopolamine-induced memory deficit in ICR mouse assessed as latency time at 1 mg/kg, po administered 30 min before acquisition trial by passive avoidance test (Rvb =271.0 +/- 14.49 seconds)2015Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1
Synthesis of aminoalkyl-substituted aurone derivatives as acetylcholinesterase inhibitors.
AID656684Inhibition of human AChE by Ellman's method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Prospective acetylcholinesterase inhibitory activity of indole and its analogs.
AID707697Inhibition of mouse recombinant GST-tagged CLK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
AID1498443Inhibition of horse serum BChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1140466Inhibition of BuChE in equine serum using S-butyrylthiocholine iodide as substrate preincubated with enzyme for 6 mins followed by substrate addition by Ellman's method2014Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease.
AID1246446Selectivity index, ratio of IC50 for horse serum butyrylcholinesterase to IC50 for electric eel acetylcholinesterase2015European journal of medicinal chemistry, Sep-18, Volume: 102Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease.
AID1498442Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID114806Compound was evaluated for the cholinergic activity in vivo in mice, by administering the compound intraperitoneally and observation of the salivation was made after 30 min1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID462834Inhibition of equine serum BChE by Ellman's method2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus.
AID1564164Inhibition of equine serum BuChE assessed as dissociation constant for enzyme-inhibitor complex using butyrylthiocholine iodide as substrate measured for 125 secs by Ellman's method2019European journal of medicinal chemistry, Nov-01, Volume: 181Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors.
AID1077146Selectivity ratio of IC50 for electric eel AChE to IC50 for equine serum BChE2014European journal of medicinal chemistry, Apr-09, Volume: 76Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents.
AID1498461Inhibition of horse serum BChE at 3.125 ug using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1498464Inhibition of horse serum BChE at 25 ug using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1524946Inhibition of BChE (unknown origin) using butyrylthiocholine iodide as substrate by spectrophotometry based Ellman's method2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.
AID175557Effect after an intraperitoneal dose of 0.3 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID1162589Inhibition of human recombinant AChE using acetylthiocholine iodide substrate incubated for 15 mins by spectrophotometry based Ellman's method2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors.
AID1593770Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by Ellman's method2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Dispiropyrrolidinyl-piperidone embedded indeno[1,2-b]quinoxaline heterocyclic hybrids: Synthesis, cholinesterase inhibitory activity and their molecular docking simulation.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1293781Inhibition of equine BChE using S-butyrylthiocholine chloride as substrate by Ellman's method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
2-Phenylbenzofuran derivatives as butyrylcholinesterase inhibitors: Synthesis, biological activity and molecular modeling.
AID1646342Inhibition of BChE (unknown origin)2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Design, synthesis and cholinesterase inhibitory activity of novel spiropyrrolidine tethered imidazole heterocyclic hybrids.
AID32110Inhibitory dose for anticholinesterase activity by ex vivo determination in rat salivary gland after intraperitoneal administration1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID437941Antioxidant activity in Wistar rat brain assessed as inhibition of lipid peroxidation2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1347777Inhibition of amyloid beta (25 to 35 residues) (unknown origin) aggregation at 50 ug/ml after 24 to 48 hrs by thioflavin T dye based confocal laser scanning microscopy
AID1678839Effect on locomotory activity in STZ-induced mouse model of Alzheimer's disease assessed as number of crossing 0.5 mg/kg, ip treated from 3 to 12 days by open field test (Rvb = 114.00 +/- 3.12 No_unit)2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.
AID746748Inhibition of equine serum BuChE using S-butyrylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition measured after 30 mins by Ellman's method2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
A facile chemo-, regio- and stereoselective synthesis and cholinesterase inhibitory activity of spirooxindole-pyrrolizine-piperidine hybrids.
AID1127083Inhibition of AChE (unknown origin) by Ellman colorimetric method2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis, acetylcholinesterase inhibition and larvicidal activity of girgensohnine analogs on Aedes aegypti, vector of dengue fever.
AID480456Inhibition of dexamethasone-induced human NR1-1a/NR2B receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L13-E6 cells assessed as LDH release at 25 uM after 30 mins2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents.
AID1491306Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured for 30 mins by Ellman's method2017European journal of medicinal chemistry, Sep-08, Volume: 137Isosteroidal alkaloids as potent dual-binding site inhibitors of both acetylcholinesterase and butyrylcholinesterase from the bulbs of Fritillaria walujewii.
AID1854475Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate pre-incubated for 5 mins followed by substrate addition and measured after 6 mins by Ellman's method2022European journal of medicinal chemistry, Nov-05, Volume: 241New naphtho/thienobenzo-triazoles with interconnected anti-inflammatory and cholinesterase inhibitory activity.
AID1564174Selectivity index, ratio of IC50 for human recombinant AChE expressed in HEK293 cells to IC50 for human serum BuChE2019European journal of medicinal chemistry, Nov-01, Volume: 181Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors.
AID688350Cytotoxicity against human G361 cells after 72 hrs by Calcein AM assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Apoptosis-inducing effects of distichamine and narciprimine, rare alkaloids of the plant family Amaryllidaceae.
AID600979Inhibition of human plasma AChE2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
AID1498448Inhibition of electric eel AChE at 6.25 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID550178Inhibition of AChE assessed as minimum drug level causing white zone of enzyme inhibition by TLC bioautography assay2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Phytochemical investigations of Stemona curtisii and synthetic studies on stemocurtisine alkaloids.
AID1315223Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE2016Journal of natural products, 05-27, Volume: 79, Issue:5
Alkaloids from Hippeastrum argentinum and Their Cholinesterase-Inhibitory Activities: An in Vitro and in Silico Study.
AID635416Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Benzenediol-berberine hybrids: multifunctional agents for Alzheimer's disease.
AID437957Antibacterial activity against Klebsiella pneumoniae at 2 mg/mL after 18 hrs by disc diffusion assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1443226Selectivity index, ratio of IC50 for acetylcholinesterase (unknown origin) to IC50 for butyrylcholinesterase (unknown origin)2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Green synthesis of novel spiro-indenoquinoxaline derivatives and their cholinesterases inhibition activity.
AID1054126Inhibition of human AChE2013Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
Divergent structure-activity relationships of structurally similar acetylcholinesterase inhibitors.
AID688349Cytotoxicity against human HeLa cells after 72 hrs by Calcein AM assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Apoptosis-inducing effects of distichamine and narciprimine, rare alkaloids of the plant family Amaryllidaceae.
AID271049Inhibition of horse serum BChE2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase.
AID1678840Effect on behavioral activity in STZ-induced mouse model of Alzheimer's disease assessed as rearing at 0.5 mg/kg, ip treated from 3 to 12 days by open field test (Rvb = 53.60 +/- 1.62 No_unit)2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1337747Inhibition of electric eel AChE pretreated for 20 mins followed by acetylthiocholine iodide substrate addition measured for 5 mins by Ellman's method2017European journal of medicinal chemistry, Jan-05, Volume: 125New azepino[4,3-b]indole derivatives as nanomolar selective inhibitors of human butyrylcholinesterase showing protective effects against NMDA-induced neurotoxicity.
AID1636643Inhibition of equine serum BuChE preincubated for 6 mins followed by addition of S-butyrylthiocholine iodide by Ellman's method2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Synthesis and evaluation of novel 1,2,3-triazole-based acetylcholinesterase inhibitors with neuroprotective activity.
AID726768Competitive inhibition of Electrophorus electricus AChE using acetylcholine as substrate by Lineweaver-Burk plot method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Acetylcholinesterase immobilized capillary reactors-tandem mass spectrometry: an on-flow tool for ligand screening.
AID1194501Inhibition of BchE in human plasma incubated for 30 mins using butyrylthiocholine substrate at 37 degC by DTNB dye based spectrophotometry2015Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
New septanoside and 20-hydroxyecdysone septanoside derivative from Atriplex portulacoides roots with preliminary biological activities.
AID1366158Antibacterial activity against Escherichia coli incubated overnight by two-fold serial dilution method2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Antibacterial constituents of the plant family Amaryllidaceae.
AID378483Inhibition of human AChE by Ellman's assay2006Journal of natural products, Sep, Volume: 69, Issue:9
Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana.
AID707053Displacement of [3H]MK-801 from NMDAR in Sprague-Dawley rat cerebral cortex homogenates after 2 hrs by liquid scintillation counting2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease.
AID73711In vitro reversal of vecuronium-induced neuromuscular block in guinea pig hemi-diaphragm.2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
AID707052Displacement of [3H]Ifenprodil from NMDAR-2B in Sprague-Dawley rat frontal cortex homogenates after 2 hrs by liquid scintillation counting2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease.
AID729524Inhibition of equine serum BuChE using S-butyrylthiocholine chloride substrate by Ellman's method based spectrophotometry2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and discovery of novel piperidone-grafted mono- and bis-spirooxindole-hexahydropyrrolizines as potent cholinesterase inhibitors.
AID688347Cytotoxicity against human K562 cells after 72 hrs by Calcein AM assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Apoptosis-inducing effects of distichamine and narciprimine, rare alkaloids of the plant family Amaryllidaceae.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1140467Selectivity index, ratio of IC50 for BuChE in equine serum to IC50 for electric eel AChE2014Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease.
AID1524945Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by spectrophotometry based Ellman's method2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.
AID378484Inhibition of horse serum BuChE by Ellman's method2006Journal of natural products, Sep, Volume: 69, Issue:9
Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana.
AID281638Increase in extracellular acetylcholine at 1 uM in urethane anesthetized Sprague-Dawley rat nucleus accumbens2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Acetylcholinesterase inhibitory activity of scopolin and scopoletin discovered by virtual screening of natural products.
AID1570261Inhibition of BuChE (unknown origin)2019European journal of medicinal chemistry, Oct-15, Volume: 180Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships.
AID1400271Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors.
AID1678843Antioxidant activity in STZ-induced mouse model of Alzheimer's disease assessed as increase in GSH level in brain at 0.5 mg/kg, ip treated from 3 to 12 days starting from 3 days post initial STZ stimulation and measured on day 17 by spectrophotometric met2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.
AID482856Inhibition of electric eel AChE by Ellman's method2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID486995Inhibition of equine serum BuChE by Ellman's method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase.
AID514203Inhibition of electric eel AChE by Ellman's method2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.
AID1167622Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins by spectrophotometric method2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID607923Inhibition of acetylcholinesterase by TLC bioautography2011Journal of natural products, Jan-28, Volume: 74, Issue:1
Phytochemical studies on Stemona aphylla: isolation of a new stemofoline alkaloid and six new stemofurans.
AID492427Antimalarial activity against Plasmodium falciparum K12009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
Antimalarials from nature.
AID569583Selectivity ratio of IC50 for electric eel AChE to IC50 for equine serum BChE2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Probing the mid-gorge of cholinesterases with spacer-modified bivalent quinazolinimines leads to highly potent and selective butyrylcholinesterase inhibitors.
AID501440Inhibition of AChE by Ellman's assay2010Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
Structure-activity studies on acetylcholinesterase inhibition in the lycorine series of Amaryllidaceae alkaloids.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1466563Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis
AID1077145Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method2014European journal of medicinal chemistry, Apr-09, Volume: 76Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents.
AID594821Inhibition of BChE2011Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
(+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase.
AID670570Inhibition of amyloid beta (1 to 40) fibril formation at 10 uM coincubated with amyloid beta (1 to 40) peptide after 72 hrs by transmission electron microscopic analysis2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.
AID1472442Inhibition of AChE (unknown origin)2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.
AID1126155Inhibition of AChE (unknown origin) assessed as minimum inhibitory concentration by bioautographic TLC assay2014Journal of natural products, Apr-25, Volume: 77, Issue:4
Marsupellins A-F, ent-longipinane-type sesquiterpenoids from the Chinese liverwort Marsupella alpine with acetylcholinesterase inhibitory activity.
AID480454Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release at 25 uM after 30 mins2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents.
AID656683Inhibition of electric eel AChE using acetylcholine iodide as substrate at 3.4 X 10'-4 M measured every 5 sec for 2 mins by Ellman's method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Prospective acetylcholinesterase inhibitory activity of indole and its analogs.
AID1854481Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate pre-incubated for 5 mins followed by substrate addition at 60 uM and measured after 6 mins by Ellman's method relative to control2022European journal of medicinal chemistry, Nov-05, Volume: 241New naphtho/thienobenzo-triazoles with interconnected anti-inflammatory and cholinesterase inhibitory activity.
AID1498445Inhibition of electric eel AChE at 0.781 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID479754Inhibition of Equine serum BChE after 2 mins by colorimetric Ellman assay2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Bivalent 5,8,9,13b-tetrahydro-6H-isoquino[1,2-a]isoquinolines and -isoquinolinium salts: novel heterocyclic templates for butyrylcholinesterase inhibitors.
AID747035Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Novel racemic tetrahydrocurcuminoid dihydropyrimidinone analogues as potent acetylcholinesterase inhibitors.
AID383199Inhibition of equine serum BuChE by Ellman's assay2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Design, synthesis and pharmacological evaluation of hybrid molecules out of quinazolinimines and lipoic acid lead to highly potent and selective butyrylcholinesterase inhibitors with antioxidant properties.
AID49086Change in response to vagal stimulation was detected in anaesthetised cats on administration of the compound; NT denotes not tested2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
AID1498450Inhibition of electric eel AChE at 25 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID749370Selectivity ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Microwave assisted synthesis, cholinesterase enzymes inhibitory activities and molecular docking studies of new pyridopyrimidine derivatives.
AID1328975Neurotoxicity in human SH-SY5Y cells assessed as decrease in cell viability at 1 uM after 24 hrs by XTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease.
AID1066954Inhibition of ICR mouse brain AChE using acetylthiocholine iodide as substrate at 100 uM incubated 10 mins prior to substrate addition measured after 10 mins by Ellman's method2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Synthesis of aminoalkyl-substituted coumarin derivatives as acetylcholinesterase inhibitors.
AID276346Inhibition of BChE2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID437943Inhibition of superoxide dismutase in Wistar rat brain2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1807566Inhibition of human BuChE using butyrylthiocholine chloride as substrate by Ellman's method2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID724167Inhibition of butyrylcholinesterase (unknown origin)2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.
AID44289In vitro inhibitory activity against Butyrylcholinesterase (BChE) in human serum2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and structure-activity relationships of open D-Ring galanthamine analogues.
AID1498453Inhibition of electric eel AChE at 0.024 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1389179Inhibition of electric eel AChE at 10 uM using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured for 45 mins by Ellmans microplate assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease.
AID486994Inhibition of electric eel AChE by Ellman's assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase.
AID754042Inhibition of equine serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins prior to substrate addition measured at 60 to 180 seconds by Ellman's method2013European journal of medicinal chemistry, Jun, Volume: 64Design, synthesis and evaluation of novel tacrine-coumarin hybrids as multifunctional cholinesterase inhibitors against Alzheimer's disease.
AID437951Antioxidant activity in Wistar rat brain assessed as lipid peroxidation2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1406252Inhibition of BChE (unknown origin)2018European journal of medicinal chemistry, Aug-05, Volume: 156Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities.
AID479753Inhibition of Electric eel AChE after 2 mins by colorimetric Ellman assay2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Bivalent 5,8,9,13b-tetrahydro-6H-isoquino[1,2-a]isoquinolines and -isoquinolinium salts: novel heterocyclic templates for butyrylcholinesterase inhibitors.
AID437956Antibacterial activity against Escherichia coli at 1 mg/mL after 18 hrs by disc diffusion assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1162591Selectivity index, ratio of IC50 for human recombinant BuChE to IC50 for human recombinant AChE2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors.
AID31968Inhibition against acetylcholinesterase (AChE)1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID1567161Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's spectrophotometric method2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
AID724168Inhibition of acetylcholinesterase (unknown origin)2013Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1
Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1271110Inhibition of BuChE (unknown origin) using butyrylthiocholine iodide as substrate at 80 ug/ml by Ellman spectrophotometric method2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and evaluation of bis-thiazole derivatives as new anticancer agents.
AID730446Lipophilicity, log P of the compound by HPLC analysis2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and in vitro evaluation of new derivatives of 2-substituted-6-fluorobenzo[d]thiazoles as cholinesterase inhibitors.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID260079Inhibitory activity against AChE from electric eel2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Isolation and cholinesterase-inhibition studies of sterols from Haloxylon recurvum.
AID1254737Inhibition of AChE (unknown origin)2015Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21
A computational view on the significance of E-ring in binding of (+)-arisugacin A to acetylcholinesterase.
AID1657594Inhibition of human AChE using acetylthiocholine iodide as substrate measured for 1 min by spectrophotometric based Ellman's method2020Journal of natural products, 05-22, Volume: 83, Issue:5
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.
AID1678838Anxiolytic-like activity in STZ-induced mouse model of Alzheimer's disease assessed as open arm frequency at 0.5 mg/kg, ip treated from 3 to 12 days starting from 3 days post initial STZ stimulation and measured on day 14 by elevated plus maze test (Rvb =2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID666575Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition measured every 1 min by Ellman's assay2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents.
AID345206Inhibition of human serum BChE by Ellman's assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
AID437958Antibacterial activity against Staphylococcus aureus at 2 mg/mL after 18 hrs by disc diffusion assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID694076Relative selectivity ratio, ratio of compound selectivity ratio to tacrine selectivity ratio for human recombinant BChE Ki to human recombinant AChE Ki2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aβ aggregation, and β-secretase.
AID1443223Inhibition of acetylcholinesterase (unknown origin) using acetylthiocholine as substrate preincubated for 20 mins followed by substrate addition by Ellmans method2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Green synthesis of novel spiro-indenoquinoxaline derivatives and their cholinesterases inhibition activity.
AID1331321Inhibition of BuChE (unknown origin) by spectrophotometric analysis based Ellman's assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID730447Inhibition of equine BChE using after 10 mins by Ellman's method2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and in vitro evaluation of new derivatives of 2-substituted-6-fluorobenzo[d]thiazoles as cholinesterase inhibitors.
AID1739259Inhibition of AChE (unknown origin) at 10 uM preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method relative to control2020European journal of medicinal chemistry, Aug-15, Volume: 200Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.
AID281636Inhibition of AChE by microplate assay2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Acetylcholinesterase inhibitory activity of scopolin and scopoletin discovered by virtual screening of natural products.
AID1312278Inhibition of BChE (unknown origin) pre-incubated for 15 mins before S-butyrylthiocholine chloride substrate addition and measured after 30 mins by colorimetric Ellman's method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Cholinesterase inhibitory activity of isoquinoline alkaloids from three Cryptocarya species (Lauraceae).
AID751999Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Design, synthesis and evaluation of flavonoid derivatives as potential multifunctional acetylcholinesterase inhibitors against Alzheimer's disease.
AID1443224Inhibition of butyrylcholinesterase (unknown origin) using acetylthiocholine as substrate preincubated for 20 mins followed by substrate addition by Ellmans method2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Green synthesis of novel spiro-indenoquinoxaline derivatives and their cholinesterases inhibition activity.
AID420064Inhibition of human CYP3A4 assessed as biotransformation of 7-benzyloxyquinoline2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Selective cytochrome P450 3A4 inhibitory activity of Amaryllidaceae alkaloids.
AID1493770Inhibition of BChE (unknown origin) using thiocholine as substrate preincubated for 15 mins followed by substrate addition measured after 5 mins by Ellman's method2018European journal of medicinal chemistry, Jan-01, Volume: 1432-Arylbenzofurans from Artocarpus lakoocha and methyl ether analogs with potent cholinesterase inhibitory activity.
AID32105Acetylcholinesterase inhibitory activity in rat striatal homogenates1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Synthesis and evaluation of 5-amino-5,6,7,8-tetrahydroquinolinones as potential agents for the treatment of Alzheimer's disease.
AID479755Selectivity ratio of IC50 for Electric eel AChE to IC50 for equine serum BChE2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Bivalent 5,8,9,13b-tetrahydro-6H-isoquino[1,2-a]isoquinolines and -isoquinolinium salts: novel heterocyclic templates for butyrylcholinesterase inhibitors.
AID1853195Inhibition of human acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
Pyrazolines as potential anti-Alzheimer's agents: DFT, molecular docking, enzyme inhibition and pharmacokinetic studies.
AID746378Inhibition of BuChE (unknown origin) by Ellman method2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease.
AID437946Antibacterial activity against Klebsiella pneumoniae after 18 hrs2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1301459Inhibition AChE (unknown origin) using ATCI as substrate assessed as hydrolysis of ATCI after 10 mins measured every 1 min for 10 times2016Journal of natural products, Feb-26, Volume: 79, Issue:2
Bioactive Constituents of Glycyrrhiza uralensis (Licorice): Discovery of the Effective Components of a Traditional Herbal Medicine.
AID1129236Selectivity ratio of IC50 for equine serum BChE to IC50 for electric eel AChE2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and discovery of highly functionalized mono- and bis-spiro-pyrrolidines as potent cholinesterase enzyme inhibitors.
AID1389178Inhibition of equine serum BChE at 10 uM using S-butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured for 45 mins by Ellmans microplate assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease.
AID776491Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition by Ellmans method2013European journal of medicinal chemistry, Nov, Volume: 69Multifunctional tacrine-flavonoid hybrids with cholinergic, β-amyloid-reducing, and metal chelating properties for the treatment of Alzheimer's disease.
AID1246442Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method2015European journal of medicinal chemistry, Sep-18, Volume: 102Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease.
AID175561Effect after an intraperitoneal dose of 3.0 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID1328976Neurotoxicity in human SH-SY5Y cells assessed as decrease in cell viability at 25 to 50 uM after 24 hrs by XTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease.
AID1594570Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID378485Inhibition of human AChE at 100 uM by Ellman's assay2006Journal of natural products, Sep, Volume: 69, Issue:9
Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana.
AID569582Inhibition of equine serum BChE by Ellman's method2011Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
Probing the mid-gorge of cholinesterases with spacer-modified bivalent quinazolinimines leads to highly potent and selective butyrylcholinesterase inhibitors.
AID1886770Cognitive enhancing effect in amyloid beta (1 to 42)-induced ICR mouse model assessed as reduction in latency at 1 mg/kg, icv measured on day 14 by Morris Water maze method
AID1634701Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 200 uM after 24 hrs by Griess assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Galanthamine, Plicamine, and Secoplicamine Alkaloids from Zephyranthes candida and Their Anti-acetylcholinesterase and Anti-inflammatory Activities.
AID307547Selectivity for electric eel AChE over equine serum BuChE2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors.
AID1646343Selectivity ratio of IC50 for BChE (unknown origin) to IC50 for AChE (unknown origin)2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Design, synthesis and cholinesterase inhibitory activity of novel spiropyrrolidine tethered imidazole heterocyclic hybrids.
AID1335318Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate by Ellman's method2016European journal of medicinal chemistry, Nov-29, Volume: 124New piperidine-hydrazone derivatives: Synthesis, biological evaluations and molecular docking studies as AChE and BChE inhibitors.
AID635417Inhibition of equine serum BuChE using acetylcholine as substrate preincubated for 15 mins by Ellman's method2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Benzenediol-berberine hybrids: multifunctional agents for Alzheimer's disease.
AID1593772Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BChE2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Dispiropyrrolidinyl-piperidone embedded indeno[1,2-b]quinoxaline heterocyclic hybrids: Synthesis, cholinesterase inhibitory activity and their molecular docking simulation.
AID603899Inhibition of electric eel AChE at 10'-4.3 M by colorimetric Ellman's assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Mycobacterium tuberculosis and cholinesterase inhibitors from Voacanga globosa.
AID670566Inhibition of BACE12012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.
AID1246443Inhibition of horse serum butyrylcholinesterase using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method2015European journal of medicinal chemistry, Sep-18, Volume: 102Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease.
AID1493747Inhibition of electric eel AChE at 3 uM using acetylthiocholine iodide as substrate measured for 0.5 to 1.5 mins post substrate addition by spectrophotometry based Ellman's method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents.
AID1466635Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric method2017Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13
Antioxidant and anticholinesterase potential of diterpenoid alkaloids from Aconitum heterophyllum.
AID1126156Inhibition of AChE (unknown origin) using acetylthiocholine as substrate at 5 uM preincubated for 15 mins measured after 30 mins by Ellman's method2014Journal of natural products, Apr-25, Volume: 77, Issue:4
Marsupellins A-F, ent-longipinane-type sesquiterpenoids from the Chinese liverwort Marsupella alpine with acetylcholinesterase inhibitory activity.
AID1736863Selectivity ratio of IC50 for human erythrocyte AChE to IC50 for human plasma BuChE2020European journal of medicinal chemistry, Apr-01, Volume: 191Design, synthesis and biological evaluation of 2,3-dihydro-5,6-dimethoxy-1H-inden-1-one and piperazinium salt hybrid derivatives as hAChE and hBuChE enzyme inhibitors.
AID1498458Inhibition of horse serum BChE at 0.391 ug using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID462836Selectivity ratio of IC50 for equine serum BChE to IC50 for bovine AChE2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus.
AID1524942Inhibition of BChE (unknown origin) at 100 ug/mL using butyrylthiocholine iodide as substrate by spectrophotometry based Ellman's method2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.
AID1167624Selectivity ratio of IC50 for equine serum BChE to IC50 for electric eel AChE2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1347778Disaggregation of amyloid beta (25 to 35 residues) (unknown origin) preformed fibrils at 50 ug/ml after 96 hrs to 9 days by thioflavin T dye based confocal laser scanning microscopy
AID1657596Inhibition of human BuChE using butyrylthiocholine iodide as substrate measured for 1 min by spectrophotometric based Ellman's method2020Journal of natural products, 05-22, Volume: 83, Issue:5
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.
AID480449Inhibition of equine serum BChE by modified Ellman's method2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents.
AID1597699Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method2019European journal of medicinal chemistry, Sep-01, Volume: 177Investigating 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole as scaffold of butyrylcholinesterase-selective inhibitors with additional neuroprotective activities for Alzheimer's disease.
AID1162590Inhibition of human recombinant BuChE using butyrylthiocholine iodide substrate incubated for 15 mins by spectrophotometry based Ellman's method2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors.
AID670565Selectivity ratio of IC50 for human AChE to IC50 for equine BuChE2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.
AID436266Inhibition of acetylcholinesterase2008Journal of natural products, Nov, Volume: 71, Issue:11
Synthesis and biological activities of thio-avarol derivatives.
AID1063991Inhibition of equine serum butyrylcholinesterase using S-butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured for 30 mins by Ellman's method2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Cholinesterase inhibitory activity versus aromatic core multiplicity: a facile green synthesis and molecular docking study of novel piperidone embedded thiazolopyrimidines.
AID1779364Inhibition of human serum BuChe using butyrylthiocholine iodide as substrate incubated for 25 mins by DTNB reagent based Ellman's method2021Bioorganic & medicinal chemistry, 07-15, Volume: 42"Clicking" fragment leads to novel dual-binding cholinesterase inhibitors.
AID482853Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives.
AID776489Inhibition of equine serum BuChE using S-butyrylcholinesterase iodide as substrate preincubated for 6 mins followed by substrate addition by Ellmans method2013European journal of medicinal chemistry, Nov, Volume: 69Multifunctional tacrine-flavonoid hybrids with cholinergic, β-amyloid-reducing, and metal chelating properties for the treatment of Alzheimer's disease.
AID482868Neuroprotective activity in human SH-SY5Y cells assessed as protection against okadaic acid-induced cell death at 1 uM after 24 hrs by MTT assay2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives.
AID48159Change in heart rate was detected in anaesthetised cats on administration of the compound; NT denotes not tested2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID30666Inhibitory activity against acetylcholinesterase (AChE) from Torpedo californica (Reversible type of inhibition)2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Synthesis, anticholinesterase activity and structure-activity relationships of m-Aminobenzoic acid derivatives.
AID262754Anticholinesterase activity against human erythrocyte AChE2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
AID1807565Inhibition of human BuChE at 100 uM using butyrylthiocholine chloride as substrate by Ellman's method2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID1807567Selectivity index, ratio of IC50 for human AChE to IC50 for human BuChe2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID362528Inhibition of butyrylcholinesterase2008Journal of natural products, Aug, Volume: 71, Issue:8
Bioactive 5alpha-pregnane-type steroidal alkaloids from Sarcococca hookeriana.
AID1347783Inhibition of amyloid beta (25 to 35 residues) (unknown origin) aggregation at 50 ug/ml after 24 to 48 hrs by FTIR spectroscopy
AID1322224Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 15 secs for 5 to 10 mins by Ellman's method2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Synthesis and evaluation of dihydropyrimidinone-derived selenoesters as multi-targeted directed compounds against Alzheimer's disease.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1636644Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Synthesis and evaluation of novel 1,2,3-triazole-based acetylcholinesterase inhibitors with neuroprotective activity.
AID1176926Inhibition of AChE (unknown origin) assessed as reduction in acetylthiocholine iodide hydrolysis after 15 mins by Ellman method2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Sulfonamides as multifunctional agents for Alzheimer's disease.
AID1498900Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition 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.
AID1076771Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 100 nM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 22014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1076770Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 1 uM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 24 2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1271108Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 80 ug/ml by Ellman spectrophotometric method2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and evaluation of bis-thiazole derivatives as new anticancer agents.
AID1176928Inhibition of BuChE (unknown origin) assessed as reduction in S-butyrylthiocholine chloride hydrolysis at 10 uM after 15 mins by Ellman method2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Sulfonamides as multifunctional agents for Alzheimer's disease.
AID1493748Inhibition of horse serum BuChE at 3 uM using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured after 10 mins by spectrophotometry based-Ellman's method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents.
AID1886774Cognitive enhancing effect in amyloid beta (1 to 42)-induced ICR mouse model assessed as reduction in amyloid beta (1 to 42) peptide level in brain at 2.5 mg/kg, icv measured on day 14 by ELISA
AID694075Selectivity ratio of Ki for human recombinant BChE to Ki for human recombinant AChE2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aβ aggregation, and β-secretase.
AID1498446Inhibition of electric eel AChE at 1.563 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID594820Inhibition of AChE-induced amyloid beta aggregation2011Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
(+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase.
AID746749Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins by Ellman's method2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
A facile chemo-, regio- and stereoselective synthesis and cholinesterase inhibitory activity of spirooxindole-pyrrolizine-piperidine hybrids.
AID1075992Inhibition of electric eel acetylcholinesterase type VI-S using acetylthiocholine iodide as substrate measured every 30s for 5 mins by Ellman's spectrophotometric method2014European journal of medicinal chemistry, Mar-21, Volume: 75Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1537271Selectivity index, ratio of IC50 for human BuChE to IC50 for human AChE2019Journal of natural products, 02-22, Volume: 82, Issue:2
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.
AID1636642Inhibition of electric eel AChE preincubated for 6 mins followed by addition of acetylthiocholine iodide by Ellman's method2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Synthesis and evaluation of novel 1,2,3-triazole-based acetylcholinesterase inhibitors with neuroprotective activity.
AID707700Inhibition of human recombinant GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
AID1331323Inhibition of electric eel AChE at 2 uM by spectrophotometric analysis based Ellman's assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents.
AID1578093Antitrypanosomal activity against Trypanosoma cruzi2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID1339190Inhibition of horse serum BuChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method2017Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4
Synthesis, anticholinesterase activity and molecular modeling study of novel carbamate-substituted thymol/carvacrol derivatives.
AID1328971Neuroprotective activity against oligomycine/rotenone-induced oxidative stress-mediated cell death in human SH-SY5Y cells assessed as increase in cell viability after 24 hrs by XTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease.
AID1498462Inhibition of horse serum BChE at 6.25 ug using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID298279Inhibition of human recombinant butyrylcholinesterase2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
AID437955Antibacterial activity against Bacillus subtilis at 1 mg/mL after 18 hrs by disc diffusion assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1267381Inhibition of horse serum butyrylcholinesterase using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents.
AID1267382Selectivity ratio of IC50 for horse serum BuChE to IC50 for electric eel AChE2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents.
AID437945Antibacterial activity against Staphylococcus aureus after 18 hrs2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID526489Inhibition of electric eel AChE by Ellman's method2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Indole alkaloids from Ervatamia hainanensis with potent acetylcholinesterase inhibition activities.
AID378482Inhibition of electric eel AChE by Ellman's assay2006Journal of natural products, Sep, Volume: 69, Issue:9
Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana.
AID752001Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman's method2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Design, synthesis and evaluation of flavonoid derivatives as potential multifunctional acetylcholinesterase inhibitors against Alzheimer's disease.
AID482854Inhibition of equine serum BuChE by Ellman's method2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives.
AID437948Antibacterial activity against Escherichia coli after 18 hrs2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID298281Inhibition of self-induced amyloid beta (1-40) aggregation at 10 uM by thioflavin T based fluorometric assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
AID1472441Inhibition of BChE (unknown origin)2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.
AID1389181Inhibition of equine serum BuChE using S-butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured for 45 mins by Ellmans microplate assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease.
AID1271109Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at by Ellman spectrophotometric method2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and evaluation of bis-thiazole derivatives as new anticancer agents.
AID1347788Disaggregation of amyloid beta (25 to 35 residues) (unknown origin) preformed fibrils at 50 ug/ml after 96 hrs to 9 days by ThT-based fluorescence spectroscopic method
AID1678842Antioxidant activity in STZ-induced mouse model of Alzheimer's disease assessed as reduction in TBARS level in brain at 0.5 mg/kg, ip treated from 3 to 12 days starting from 3 days post initial STZ stimulation and measured on day 17 by spectrophotometric 2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.
AID1545271Inhibition of human acetylcholinesterase2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID1063990Selectivity ratio of IC50 for equine serum butyrylcholinesterase to IC50 for Electrophorus electricus acetylcholinesterase2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Cholinesterase inhibitory activity versus aromatic core multiplicity: a facile green synthesis and molecular docking study of novel piperidone embedded thiazolopyrimidines.
AID635415Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Benzenediol-berberine hybrids: multifunctional agents for Alzheimer's disease.
AID437949Antioxidant activity in Wistar rat brain assessed as superoxide dismutase content2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1076769Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 10 uM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 242014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1507310Inhibition of human AChE2017European journal of medicinal chemistry, Aug-18, Volume: 136Discorhabdin alkaloids from Antarctic Latrunculia spp. sponges as a new class of cholinesterase inhibitors.
AID670563Inhibition of human AChE using acetylthiocholine iodide as substrate after 5 mins by DTNB method2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.
AID311339Inhibition of AChE by Ellman method2007Journal of natural products, Sep, Volume: 70, Issue:9
Benzylphenethylamine alkaloids from Hosta plantaginea with inhibitory activity against tobacco mosaic virus and acetylcholinesterase.
AID707054Inhibition of AChE in Wistar rat brain homogenates using acetylthiocholine iodide and DTNB as substrate after 10 mins by Ellman method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease.
AID281639Increase in extracellular acetylcholine at 2 uM in urethane anesthetized Sprague-Dawley rat nucleus accumbens2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Acetylcholinesterase inhibitory activity of scopolin and scopoletin discovered by virtual screening of natural products.
AID688351Cytotoxicity against human BJ cells after 72 hrs by Calcein AM assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Apoptosis-inducing effects of distichamine and narciprimine, rare alkaloids of the plant family Amaryllidaceae.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1076768Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 10 nM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rela2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1593771Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Dispiropyrrolidinyl-piperidone embedded indeno[1,2-b]quinoxaline heterocyclic hybrids: Synthesis, cholinesterase inhibitory activity and their molecular docking simulation.
AID1854488Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pre-incubated for 5 mins followed by substrate addition at 4.5 uM and measured after 6 mins by Ellman's method relative to control2022European journal of medicinal chemistry, Nov-05, Volume: 241New naphtho/thienobenzo-triazoles with interconnected anti-inflammatory and cholinesterase inhibitory activity.
AID1736860Inhibition of human plasma BuChE using butyrylthiocholine as substrate measured after 5 mins by Ellman's method2020European journal of medicinal chemistry, Apr-01, Volume: 191Design, synthesis and biological evaluation of 2,3-dihydro-5,6-dimethoxy-1H-inden-1-one and piperazinium salt hybrid derivatives as hAChE and hBuChE enzyme inhibitors.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1129234Inhibition of equine serum BChE using S-butyrylthiocholine chloride as substrate preincubated for 15 mins by spectrophotometer analysis2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and discovery of highly functionalized mono- and bis-spiro-pyrrolidines as potent cholinesterase enzyme inhibitors.
AID765550Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by Ellman's microplate assay2013European journal of medicinal chemistry, Sep, Volume: 67An expedient, ionic liquid mediated multi-component synthesis of novel piperidone grafted cholinesterase enzymes inhibitors and their molecular modeling study.
AID1872732Inhibition of AChE (unknown origin) incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Apr-05, Volume: 233Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy.
AID1066951Memory enhancing effect in ICR mouse assessed as reversal of scopolamine-induced amnesia by measuring step-through latencies at 1 mg/kg, po administered 1 hr prior to acquisition trial measured after 24 hrs by passive avoidance test relative to control2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Synthesis of aminoalkyl-substituted coumarin derivatives as acetylcholinesterase inhibitors.
AID1356515Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate pretreated for 15 mins followed by substrate addition and measured by DTNB reagent based assay2018Journal of natural products, 08-24, Volume: 81, Issue:8
A Bioactive Resveratrol Trimer from the Stem Bark of the Sri Lankan Endemic Plant Vateria copallifera.
AID666573Inhibition of electric eel acetylcholine esterase using acetylcholine chloride as substrate incubated for 15 mins prior to substrate addition measured every 1 min by Ellman's assay2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents.
AID1179994Inhibition of BuChE (unknown origin)2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Coumarin hybrids as novel therapeutic agents.
AID670564Inhibition of equine BuChE using butyrylthiocholine iodide as substrate after 5 mins by DTNB method2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.
AID1328983Neuroprotective activity against NMDA-induced excitotoxicity in Sprague-Dawley rat primary cortical neurons assessed as increase in cell viability after 3 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease.
AID670569Inhibition of self-induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by thioflavin T-based fluorescence analysis2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.
AID1780622Inhibition of electric eel AChE using acetylcholine iodide as a substrate measured for 125 secs by DNTB reagent based Ellman's method2021ACS medicinal chemistry letters, Nov-11, Volume: 12, Issue:11
Ugi Reaction Synthesis of Oxindole-Lactam Hybrids as Selective Butyrylcholinesterase Inhibitors.
AID1142530Inhibition of yeast alpha-glucosidase type 3 using p-nitrophenyl-alpha-D-glucopyranoside as substrate preincubated with substrate for 5 mins prior to enzyme challenge for 30 mins by absorbance analysis2014European journal of medicinal chemistry, Jun-10, Volume: 80Dual inhibition of the α-glucosidase and butyrylcholinesterase studied by molecular field topology analysis.
AID1315225Inhibition of electric eel AChE using ATCI as substrate preincubated for 30 mins followed by substrate addition measured after 5 mins by DTNB-based spectrophotometric analysis2016Journal of natural products, 05-27, Volume: 79, Issue:5
Alkaloids from Hippeastrum argentinum and Their Cholinesterase-Inhibitory Activities: An in Vitro and in Silico Study.
AID600978Inhibition of human erythrocytes AChE2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
AID263610Inhibition of AChE activity2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Isoquinoline derivatives as potential acetylcholinesterase inhibitors.
AID365698Inhibition of AchE2008Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines.
AID1678841Antialzheimer activity in streptozotocin-induced mouse model of memory impairment assessed as median time of avoidance latency descent at 0.5 mg/kg, ip treated from 3 to 12 days starting from 3 days post initial STZ stimulation and measured on day 16 by a2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.
AID1331322Inhibition of BuChE (unknown origin) at 10 uM by spectrophotometric analysis based Ellman's assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents.
AID437942Antioxidant activity in Wistar rat brain assessed as reduction in glutathione content2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID404434Inhibition of Torpedo californica AChE2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
AID1678837Anxiolytic-like activity in STZ-induced mouse model of Alzheimer's disease assessed as open arm time permanency at 0.5 mg/kg, ip treated from 3 to 12 days starting from 3 days post initial STZ stimulation and measured on day 14 by elevated plus maze test 2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.
AID1075991Inhibition of BuChE in human serum using butyrylthiocholine iodide as substrate measured every 30s for 5 mins by Ellman's spectrophotometric method2014European journal of medicinal chemistry, Mar-21, Volume: 75Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1070089Inhibition of equine serum BChE using S-butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Ionic liquid mediated synthesis of mono- and bis-spirooxindole-hexahydropyrrolidines as cholinesterase inhibitors and their molecular docking studies.
AID480455Inhibition of dexamethasone-induced human NR1-1a/NR2B receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L13-E6 cells assessed as LDH release after 30 mins2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents.
AID776490Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2013European journal of medicinal chemistry, Nov, Volume: 69Multifunctional tacrine-flavonoid hybrids with cholinergic, β-amyloid-reducing, and metal chelating properties for the treatment of Alzheimer's disease.
AID1075979Selectivity index, ratio of IC50 for human serum BuChE to IC50 for electric eel acetylcholinesterase type VI-S2014European journal of medicinal chemistry, Mar-21, Volume: 75Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1498444Selectivity ratio of IC50 for horse serum BChE to IC50 for electric eel AChE2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID730448Inhibition of Electrophorus electricus AChE using acetylthiocholine as substrate after 10 mins by Ellman's method2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and in vitro evaluation of new derivatives of 2-substituted-6-fluorobenzo[d]thiazoles as cholinesterase inhibitors.
AID1237656Inhibition of human acetylcholinesterase using ATCI/DTNB as substrate preincubated for 30 mins followed by substrate addition measured for 60 mins by Ellman method2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
In vitro evaluation and in silico screening of synthetic acetylcholinesterase inhibitors bearing functionalized piperidine pharmacophores.
AID707698Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
AID437952Antioxidant activity in Wistar rat brain assessed as glutathione content2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID462833Inhibition of bovine AChE by Elman's method2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus.
AID1779363Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate incubated for 25 mins by DTNB reagent based Ellman's method2021Bioorganic & medicinal chemistry, 07-15, Volume: 42"Clicking" fragment leads to novel dual-binding cholinesterase inhibitors.
AID1899571Inhibition of electric eel AChE at 10 uM using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 45 mins by Ellman's method2022European journal of medicinal chemistry, Jan-15, Volume: 228Imidazolylacetophenone oxime-based multifunctional neuroprotective agents: Discovery and structure-activity relationships.
AID1564162Inhibition of electric eel AChE assessed as dissociation constant for enzyme-inhibitor complex using acetylthiocholine iodide as substrate measured for 125 secs by Ellman's method2019European journal of medicinal chemistry, Nov-01, Volume: 181Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors.
AID486996Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase.
AID1498447Inhibition of electric eel AChE at 3.125 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1780623Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as a substrate measured for 125 secs by DNTB reagent based Ellman's method2021ACS medicinal chemistry letters, Nov-11, Volume: 12, Issue:11
Ugi Reaction Synthesis of Oxindole-Lactam Hybrids as Selective Butyrylcholinesterase Inhibitors.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1167623Inhibition of equine serum BChE using S-butyrylthiocholine chloride as substrate incubated for 6 mins by spectrophotometric method2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Design, synthesis and evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1865084Inhibition of human recombinant AChe using acetylthiocholine iodide as substrate incubated for 10 mins by DTNB reagent based Ellman's method
AID480450Selectivity ratio of IC50 for equine serum BChE to IC50 for electric eel AChE2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents.
AID1063989Selectivity ratio of IC50 for Electrophorus electricus acetylcholinesterase to IC50 for equine serum butyrylcholinesterase2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Cholinesterase inhibitory activity versus aromatic core multiplicity: a facile green synthesis and molecular docking study of novel piperidone embedded thiazolopyrimidines.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID383200Selectivity ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Design, synthesis and pharmacological evaluation of hybrid molecules out of quinazolinimines and lipoic acid lead to highly potent and selective butyrylcholinesterase inhibitors with antioxidant properties.
AID456907Selectivity for electric eel AChE over horse serum BChE2010Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3
Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors.
AID1557015Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate by Ellman's method2019European journal of medicinal chemistry, Oct-01, Volume: 179Novel N-benzylpiperidine carboxamide derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease.
AID1567163Inhibition of human recombinant BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's spectrophotometric method2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
AID1389180Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured for 45 mins by Ellmans microplate assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
In silico studies, synthesis and pharmacological evaluation to explore multi-targeted approach for imidazole analogues as potential cholinesterase inhibitors with neuroprotective role for Alzheimer's disease.
AID262756Selectivity for AChE over BChE2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
AID1498459Inhibition of horse serum BChE at 0.781 ug using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID276347Selectivity for AChE over BChE2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
AID694073Inhibition of human recombinant AChE using acetylthiocholine as substrate2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aβ aggregation, and β-secretase.
AID1175427Inhibition of ICR mouse brain AChE using acetylthiocholine iodide as substrate preincubated for 10 mins before substrate addition by modified Ellman's method2015Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1
Synthesis of aminoalkyl-substituted aurone derivatives as acetylcholinesterase inhibitors.
AID752000Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman's method2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Design, synthesis and evaluation of flavonoid derivatives as potential multifunctional acetylcholinesterase inhibitors against Alzheimer's disease.
AID383158Inhibition of acetylcholinesterase at 10 uM by Ellman's method2008Journal of natural products, May, Volume: 71, Issue:5
Xanthones from Gentianella amarella ssp. acuta with acetylcholinesterase and monoamine oxidase inhibitory activities.
AID1066955Inhibition of ICR mouse brain AChE using acetylthiocholine iodide as substrate incubated 10 mins prior to substrate addition measured after 10 mins by Ellman's method2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Synthesis of aminoalkyl-substituted coumarin derivatives as acetylcholinesterase inhibitors.
AID294502Inhibition of BuChE in horse serum2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives: a new class of acetylcholinesterase inhibitors.
AID456906Inhibition of horse serum BChE by Ellman's method2010Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3
Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors.
AID593739Inhibition of equine serum Butyrylcholinesterase2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors.
AID707048Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease.
AID1597702Inhibition of equine serum BChE using butyrylthiocholine as substrate preincubated for 20 mins followed by substrate addition and measured upto 5 mins by Ellman's method2019European journal of medicinal chemistry, Sep-01, Volume: 177Investigating 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole as scaffold of butyrylcholinesterase-selective inhibitors with additional neuroprotective activities for Alzheimer's disease.
AID307545Inhibition of electric eel AChE2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors.
AID1426027Inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured every minute for fifteen minutes by Ellman's method2017European journal of medicinal chemistry, Feb-15, Volume: 127Amaryllidaceae alkaloids with new framework types from Zephyranthes candida as potent acetylcholinesterase inhibitors.
AID114804Compound was evaluated for the cholinergic activity in vivo in mice by administering the compound intraperitoneally and observation of the tremors was made after 30 min1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID482855Inhibition of AChE in human erythrocytes by Ellman's method2010Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14
Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives.
AID262755Anticholinesterase activity against human plasma BChE2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1077143Antialzheimer activity in Wistar rat scopolamine-induced cognition impairment model assessed as decrease in amount of errors plus baits not found during exploration at 1 umol/100 g body weight, ip treated for 5 mins prior to scopolamine-challenge measured2014European journal of medicinal chemistry, Apr-09, Volume: 76Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents.
AID765547Selectivity ratio of IC50 for electric eel AChE to IC50 for horse serum BChE2013European journal of medicinal chemistry, Sep, Volume: 67An expedient, ionic liquid mediated multi-component synthesis of novel piperidone grafted cholinesterase enzymes inhibitors and their molecular modeling study.
AID593738Inhibition of electric eel Acetylcholinesterase2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors.
AID754043Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins prior to substrate addition measured at 60 to 180 seconds by Ellman's method2013European journal of medicinal chemistry, Jun, Volume: 64Design, synthesis and evaluation of novel tacrine-coumarin hybrids as multifunctional cholinesterase inhibitors against Alzheimer's disease.
AID1317853Inhibition of equine serum BuChE preincubated for 5 mins followed by addition of butyrylthiocholine iodide as substrate measured after 2 mins by Ellman's method2016European journal of medicinal chemistry, Aug-25, Volume: 119Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies.
AID345205Inhibition of human recombinant AChE by Ellman's assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID260080Inhibitory activity against BuChE from horse serum2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Isolation and cholinesterase-inhibition studies of sterols from Haloxylon recurvum.
AID1736859Inhibition of human erythrocyte AChE using acetylthiocholine as substrate measured after 5 mins by Ellman's method2020European journal of medicinal chemistry, Apr-01, Volume: 191Design, synthesis and biological evaluation of 2,3-dihydro-5,6-dimethoxy-1H-inden-1-one and piperazinium salt hybrid derivatives as hAChE and hBuChE enzyme inhibitors.
AID1347784Disaggregation of amyloid beta (25 to 35 residues) (unknown origin) preformed fibrils at 50 ug/ml after 96 hrs to 9 days by FTIR spectroscopy
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID294503Selectivity for Torpedo californica AChE over horse BuChE2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives: a new class of acetylcholinesterase inhibitors.
AID1230202Inhibition of electric eel AChE using acetylthiocholine as substrate assessed as concentration of 5-thio-2-nitrobenzoic acid ion formed by spectrophotometric/Ellman's method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
In Vitro Inhibitory Effects of 8-O-Demethylmaritidine and Undulatine on Acetylcholinesterase and Their Predicted Penetration across the Blood-Brain Barrier.
AID1594569Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment.
AID1807564Selectivity index, ratio of IC50 for human BuChe to IC50 for human AChE2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Derivatives of montanine-type alkaloids and their implication for the treatment of Alzheimer's disease: Synthesis, biological activity and in silico study.
AID343772Inhibition of Torpedo californica AchE activity by Ellman's assay2008Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13
Petrosamine, a potent anticholinesterase pyridoacridine alkaloid from a Thai marine sponge Petrosia n. sp.
AID456905Inhibition of electric eel AChE by modified Ellman method2010Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3
Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors.
AID116900Compound was evaluated for the cholinergic activity by the induction of amnesia at high toxic doses and lethal dose was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID381366Inhibition of AChE by microplate assay2000Journal of natural products, Jun, Volume: 63, Issue:6
The application of HPLC with on-line coupled UV/MS-biochemical detection for isolation of an acetylcholinesterase inhibitor from narcissus 'Sir Winston Churchill'.
AID1443225Selectivity index, ratio of IC50 for butyrylcholinesterase (unknown origin) to IC50 for acetylcholinesterase (unknown origin)2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Green synthesis of novel spiro-indenoquinoxaline derivatives and their cholinesterases inhibition activity.
AID1427875Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method2017European journal of medicinal chemistry, Feb-15, Volume: 127Targeting Alzheimer's disease by investigating previously unexplored chemical space surrounding the cholinesterase inhibitor donepezil.
AID765549Inhibition of horse serum BChE using S-butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by Ellman's microplate assay2013European journal of medicinal chemistry, Sep, Volume: 67An expedient, ionic liquid mediated multi-component synthesis of novel piperidone grafted cholinesterase enzymes inhibitors and their molecular modeling study.
AID1273007Inhibition of equine BChE using BTC as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by Ellman's assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Ferulic acid-carbazole hybrid compounds: Combination of cholinesterase inhibition, antioxidant and neuroprotection as multifunctional anti-Alzheimer agents.
AID1186580Selectivity ratio of Ki for human BChE to Ki for human AChE2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase.
AID1498454Inhibition of electric eel AChE at 0.049 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1537270Inhibition of human BuChE using butyrylthiocholine iodide as substrate measured for 1 min by Ellman's method2019Journal of natural products, 02-22, Volume: 82, Issue:2
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.
AID746379Inhibition of AChE (unknown origin) by Ellman method2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1076767Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 100 nM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rel2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1491305Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured for 30 mins by Ellman's method2017European journal of medicinal chemistry, Sep-08, Volume: 137Isosteroidal alkaloids as potent dual-binding site inhibitors of both acetylcholinesterase and butyrylcholinesterase from the bulbs of Fritillaria walujewii.
AID1176927Inhibition of AChE (unknown origin) assessed as reduction in acetylthiocholine iodide hydrolysis at 2 uM after 15 mins by Ellman method2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Sulfonamides as multifunctional agents for Alzheimer's disease.
AID600981Inhibition of human plasma BChE2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
AID1335319Inhibition of horse serum butyrylcholinesterase by Ellman's method2016European journal of medicinal chemistry, Nov-29, Volume: 124New piperidine-hydrazone derivatives: Synthesis, biological evaluations and molecular docking studies as AChE and BChE inhibitors.
AID31036In vitro inhibition of human recombinant AChE.2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
AID345208Inhibition of self-induced amyloid beta (1-40) aggregation at 10 uM by thioflavin T formation assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
AID1524944Inhibition of BChE (unknown origin) at 20 ug/mL using butyrylthiocholine iodide as substrate by spectrophotometry based Ellman's method2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.
AID437953Antibacterial activity against Klebsiella pneumoniae at 1 mg/mL after 18 hrs by disc diffusion assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1739255Selectivity index, ratio of IC50 for BuChE (unknown origin) to IC50 for AChE (unknown origin)2020European journal of medicinal chemistry, Aug-15, Volume: 200Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.
AID1491307Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE2017European journal of medicinal chemistry, Sep-08, Volume: 137Isosteroidal alkaloids as potent dual-binding site inhibitors of both acetylcholinesterase and butyrylcholinesterase from the bulbs of Fritillaria walujewii.
AID749372Inhibition of equine serum BuChE using S-butyrylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition measured after 30 mins by Ellman's method2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Microwave assisted synthesis, cholinesterase enzymes inhibitory activities and molecular docking studies of new pyridopyrimidine derivatives.
AID656680Inhibition of electric eel AChE using acetylcholine iodide as substrate measured every 5 sec for 2 mins by Ellman's method2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Prospective acetylcholinesterase inhibitory activity of indole and its analogs.
AID1593769Inhibition of equine serum BChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by Ellman's method2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Dispiropyrrolidinyl-piperidone embedded indeno[1,2-b]quinoxaline heterocyclic hybrids: Synthesis, cholinesterase inhibitory activity and their molecular docking simulation.
AID1466564Inhibition of equine serum BuChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis
AID1400272Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors.
AID1317854Selectivity ratio, ratio of IC50 for equine serum BuChE to electric eel AChE2016European journal of medicinal chemistry, Aug-25, Volume: 119Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies.
AID298280Inhibition of human AChE-induced amyloid beta (1-40) aggregation at 100 uM2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
AID421515Inhibition of equine serum BuChE by Ellman's method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Synthesis, biological evaluation and molecular modeling of oxoisoaporphine and oxoaporphine derivatives as new dual inhibitors of acetylcholinesterase/butyrylcholinesterase.
AID568572Inhibition of human erythrocytes acetylcholinesterase after 15 mins2011Journal of natural products, Jan-28, Volume: 74, Issue:1
Biotransformation of turmerones by Aspergillus niger.
AID603787Inhibition of electric eel AChE by colorimetric Ellman's assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Mycobacterium tuberculosis and cholinesterase inhibitors from Voacanga globosa.
AID1077144Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method2014European journal of medicinal chemistry, Apr-09, Volume: 76Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents.
AID30544In vitro inhibitory activity against acetylcholinesterase (AChE) in Electrophorus electricus2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and structure-activity relationships of open D-Ring galanthamine analogues.
AID1678836Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by Ellman's method2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.
AID670568Inhibition of human AChE-induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by thioflavin T-based fluorescence analysis2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.
AID44285Ex vivo inhibition of human plasma Butyrylcholinesterase.2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
AID1739253Inhibition of AChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method2020European journal of medicinal chemistry, Aug-15, Volume: 200Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.
AID345207Inhibition of human recombinant AChE-induced amyloid beta (1-40) aggregation at 100 uM by thioflavin T formation assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
AID1328951Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate incubated for 15 mins followed by substrate addition by Ellman's method2016European journal of medicinal chemistry, Oct-21, Volume: 122Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease.
AID333566Inhibition of rat brain acetylcholinesterase by colorimetric method2004Journal of natural products, Nov, Volume: 67, Issue:11
Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors.
AID416453Inhibition of AChE from rat cortex homogenate by Ellmans method2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.
AID1556704Inhibition of BuChE in human serum using S-butyrylthiocholine iodide as substrate at 100 uM preincubated with enzyme for 10 mins followed by substrate addition measured for 15 mins by Ellman's method relative to control2019European journal of medicinal chemistry, Oct-01, Volume: 179Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.
AID1524943Inhibition of AChE (unknown origin) at 20 ug/mL using acetylthiocholine iodide as substrate by spectrophotometry based Ellman's method2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.
AID1328972Neuroprotective activity against okadaic acid-induced tau phosphorylation-mediated cell death in human SH-SY5Y cells assessed as increase in cell viability after 24 hrs by XTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease.
AID1556711Inhibition of BuChE in human serum using S-butyrylthiocholine iodide as substrate preincubated with enzyme for 10 mins followed by substrate addition measured for 15 mins by Ellman's method2019European journal of medicinal chemistry, Oct-01, Volume: 179Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.
AID707699Inhibition of human recombinant GST-tagged DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
AID1872733Inhibition of BChE (unknown origin) incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Apr-05, Volume: 233Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy.
AID1076765Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 10 uM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rela2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1186578Inhibition of human AChE assessed as acetylthiocholine hydrolysis2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase.
AID1498460Inhibition of horse serum BChE at 1.563 ug using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1466565Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE
AID765548Selectivity ratio of IC50 for horse serum BChE to IC50 for electric eel AChE2013European journal of medicinal chemistry, Sep, Volume: 67An expedient, ionic liquid mediated multi-component synthesis of novel piperidone grafted cholinesterase enzymes inhibitors and their molecular modeling study.
AID1524941Inhibition of AChE (unknown origin) at 100 ug/mL using acetylthiocholine iodide as substrate by spectrophotometry based Ellman's method2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Bioactivity-guided identification of flavonoids with cholinesterase and β-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.
AID566361Inhibition of AChE by Ellman's method2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Triterpenoidal alkaloids from Buxus natalensis and their acetylcholinesterase inhibitory activity.
AID336177Inhibition of acetylcholinesterase-mediated hydrolysis of acetylcholine at 0.16 mg/mL relative to galanthamine2002Journal of natural products, Oct, Volume: 65, Issue:10
Bioactive constituents from Iryanthera megistophylla.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID416454Inhibition of BChE from rat serum by Ellmans method2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.
AID688344Cytotoxicity against human CEM cells after 72 hrs by Calcein AM assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Apoptosis-inducing effects of distichamine and narciprimine, rare alkaloids of the plant family Amaryllidaceae.
AID1570262Inhibition of AChE (unknown origin)2019European journal of medicinal chemistry, Oct-15, Volume: 180Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID422295Inhibition of AChE by spectrophotometry2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antioxidant and anticholinesterase activity evaluation of ent-kaurane diterpenoids from Sideritis arguta.
AID566384Inhibition of horse serum BChE after 2 mins by Ellman's reaction2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Citrusosides A-D and furanocoumarins with cholinesterase inhibitory activity from the fruit peels of Citrus hystrix.
AID1498463Inhibition of horse serum BChE at 12.5 ug using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID437954Antibacterial activity against Staphylococcus aureus at 1 mg/mL after 18 hrs by disc diffusion assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID365699Inhibition of BchE2008Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines.
AID47967Effective dose required for the reversal of vecuronium-induced neuromuscular block in-vivo in Chloaralose anaesthetised cats; NT denotes not tested2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
AID407780Inhibition of human AChE2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
AID422296Inhibition of BChE by spectrophotometry2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antioxidant and anticholinesterase activity evaluation of ent-kaurane diterpenoids from Sideritis arguta.
AID1594568Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment.
AID1076764Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 100 uM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rel2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1339189Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method2017Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4
Synthesis, anticholinesterase activity and molecular modeling study of novel carbamate-substituted thymol/carvacrol derivatives.
AID1498457Inhibition of electric eel AChE at 0.391 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1129233Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins by spectrophotometer analysis2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and discovery of highly functionalized mono- and bis-spiro-pyrrolidines as potent cholinesterase enzyme inhibitors.
AID32109Inhibitory dose for anticholinesterase activity by ex vivo determination in rat forebrain after intraperitoneal administration1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID1400273Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors.
AID754041Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE2013European journal of medicinal chemistry, Jun, Volume: 64Design, synthesis and evaluation of novel tacrine-coumarin hybrids as multifunctional cholinesterase inhibitors against Alzheimer's disease.
AID241692Inhibitory concentration against human erythrocyte Acetylcholinesterase2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
AID315115Inhibition of electric eel acetylcholinesterase2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
N-Alkylated galanthamine derivatives: Potent acetylcholinesterase inhibitors from Leucojum aestivum.
AID1332254Inhibition of acetylcholinesterase (unknown origin) assessed as reduction in formation of 5-thio-2-nitrobenzoate from acetylthiocholine iodide preincubated for 15 mins followed by substrate addition measured after 30 mins by Ellman's method2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Design and synthesis of new piperidone grafted acetylcholinesterase inhibitors.
AID1317852Inhibition of electric eel AChE preincubated for 5 mins followed by addition of acetylthiocholine iodide as substrate measured after 2 mins by Ellman's method2016European journal of medicinal chemistry, Aug-25, Volume: 119Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies.
AID175558Effect after an intraperitoneal dose of 1.0 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
AID480453Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release after 30 mins2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents.
AID688348Cytotoxicity against human MCF7 cells after 72 hrs by Calcein AM assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Apoptosis-inducing effects of distichamine and narciprimine, rare alkaloids of the plant family Amaryllidaceae.
AID421516Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Synthesis, biological evaluation and molecular modeling of oxoisoaporphine and oxoaporphine derivatives as new dual inhibitors of acetylcholinesterase/butyrylcholinesterase.
AID1231568Inhibition of acetylcholinesterase (unknown origin) assessed as AChI hydrolysis using AChI and DTNB as substrate by Ellman's method2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Discovery of potent carbonic anhydrase and acetylcholine esterase inhibitors: novel sulfamoylcarbamates and sulfamides derived from acetophenones.
AID1861405Inhibition of Equine serum BuChE using S-butyrylthiocholine iodide as a substrate and measured for 125 sec by DTNB based Ellman's method2022Bioorganic & medicinal chemistry, 08-15, Volume: 68Evaluation of chromane derivatives: Promising privileged scaffolds for lead discovery within Alzheimer's disease.
AID729525Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for AChE (unknown origin)2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and discovery of novel piperidone-grafted mono- and bis-spirooxindole-hexahydropyrrolizines as potent cholinesterase inhibitors.
AID1739254Inhibition of BuChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method2020European journal of medicinal chemistry, Aug-15, Volume: 200Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.
AID1567162Inhibition of human recombinant BuChE at 25 uM using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's spectrophotometric method relative to control2019European journal of medicinal chemistry, Sep-15, Volume: 178Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.
AID294501Inhibition of AChE2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives: a new class of acetylcholinesterase inhibitors.
AID302143Inhibition of Electrophorus electricus AChE by Ellman's method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.
AID421514Inhibition of electric eel AChE by Ellman's method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Synthesis, biological evaluation and molecular modeling of oxoisoaporphine and oxoaporphine derivatives as new dual inhibitors of acetylcholinesterase/butyrylcholinesterase.
AID635414Inhibition of electric eel AChE using acetylcholine chloride as substrate preincubated for 15 mins by Ellman's method2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Benzenediol-berberine hybrids: multifunctional agents for Alzheimer's disease.
AID1070087Selectivity ratio of IC50 for equine serum BChE to IC50 for AChE (unknown origin)2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Ionic liquid mediated synthesis of mono- and bis-spirooxindole-hexahydropyrrolidines as cholinesterase inhibitors and their molecular docking studies.
AID1861404Inhibition of electric eel AChE using acetylcholine iodide as a substrate and measured for 125 sec by DTNB based Ellman's method2022Bioorganic & medicinal chemistry, 08-15, Volume: 68Evaluation of chromane derivatives: Promising privileged scaffolds for lead discovery within Alzheimer's disease.
AID298278Inhibition of human recombinant acetylcholinesterase2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
AID437960Antibacterial activity against Escherichia coli at 2 mg/mL after 18 hrs by disc diffusion assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID1657598Effective permeability of the compound at pH 7.4 at 100 uM measured after 3 to 6 hrs by PAMPA assay2020Journal of natural products, 05-22, Volume: 83, Issue:5
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.
AID1070088Selectivity index, ratio of IC50 for AChE (unknown origin) to IC50 for equine serum BChE2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Ionic liquid mediated synthesis of mono- and bis-spirooxindole-hexahydropyrrolidines as cholinesterase inhibitors and their molecular docking studies.
AID437959Antibacterial activity against Bacillus subtilis at 2 mg/mL after 18 hrs by disc diffusion assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis, spectral characterization and biological evaluation of phosphorylated derivatives of galanthamine.
AID749373Inhibition of electric eel AChE using acetylcholine iodide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins by Ellman's method2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Microwave assisted synthesis, cholinesterase enzymes inhibitory activities and molecular docking studies of new pyridopyrimidine derivatives.
AID694074Inhibition of human recombinant BChE using acetylthiocholine as substrate2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aβ aggregation, and β-secretase.
AID31964In vitro inhibitory effect on rat Acetylcholinesterase1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation.
AID446351Inhibition of human recombinant AChE2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Probing Torpedo californica acetylcholinesterase catalytic gorge with two novel bis-functional galanthamine derivatives.
AID30543Compound was assessed for in vitro inhibition of Acetylcholinesterase isolated from Electrophorus electricus2000Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7
Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts.
AID1631831Selectivity ratio of IC50 for human plasma BuChE to IC50 for human erythrocyte AChE2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
Discovery and Structure-Activity Relationships of a Highly Selective Butyrylcholinesterase Inhibitor by Structure-Based Virtual Screening.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1356517Inhibition of BChE (unknown origin) using butyrylthiocholine iodide as substrate pretreated for 15 mins followed by substrate addition and measured by DTNB reagent based assay relative to control2018Journal of natural products, 08-24, Volume: 81, Issue:8
A Bioactive Resveratrol Trimer from the Stem Bark of the Sri Lankan Endemic Plant Vateria copallifera.
AID1073062Inhibition of Electric eel AChE assessed as amount of thiocholine released using acetylthiocholine iodide as substrate after 6 mins by Ellman's method2014Journal of natural products, Mar-28, Volume: 77, Issue:3
Chemical composition of the bark of Tetrapterys mucronata and identification of acetylcholinesterase inhibitory constituents.
AID1556710Inhibition of AChE in human erythrocytes using acetylthiocholine iodide as substrate preincubated with enzyme for 10 mins followed by substrate addition measured for 15 mins by Ellman's method2019European journal of medicinal chemistry, Oct-01, Volume: 179Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.
AID1886771Cognitive enhancing effect in amyloid beta (1 to 42)-induced ICR mouse model assessed as reduction in latency at 2.5 mg/kg, icv measured on day 14 by Morris Water maze method
AID1657597Selectivity index, ratio of IC50 for inhibition of human AChE using acetylthiocholine iodide as substrate to inhibition of human BuChE using butyrylthiocholine iodide as substrate2020Journal of natural products, 05-22, Volume: 83, Issue:5
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1865085Inhibition of human recombinant BuChe using butyrylthiocholine iodide as substrate incubated for 10 mins by DTNB reagent based Ellman's method
AID1076775Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 100 uM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 22014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1537274Inhibition of POP (unknown origin) using (Z)-Gly-Pro-p-nitroanilide as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by spectrophotometric method2019Journal of natural products, 02-22, Volume: 82, Issue:2
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.
AID1366160Antibacterial activity against Staphylococcus aureus incubated overnight by two-fold serial dilution method2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Antibacterial constituents of the plant family Amaryllidaceae.
AID1498456Inhibition of electric eel AChE at 0.195 ug using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured every 5 mins for 15 mins by spectrophotometric method relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
A cascade synthesis, in vitro cholinesterases inhibitory activity and docking studies of novel Tacrine-pyranopyrazole derivatives.
AID1634699Inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured every 13 secs by Ellman's method2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Galanthamine, Plicamine, and Secoplicamine Alkaloids from Zephyranthes candida and Their Anti-acetylcholinesterase and Anti-inflammatory Activities.
AID284418Inhibition of eel AChE2007Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
Preparation of secolycorines against acetylcholinesterase.
AID241560Inhibitory concentration against human plasma Butyrylcholinesterase2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
AID746380Inhibition of AChE (unknown origin) at 2 uM by Ellman method2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease.
AID1537276Inhibition of GSK3B (unknown origin) at 10 uM relative to control2019Journal of natural products, 02-22, Volume: 82, Issue:2
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.
AID407781Inhibition of human BuChE2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
AID234643Selectivity at AChE and BChE2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
AID1186579Inhibition of human BChE assessed as acetylthiocholine hydrolysis2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase.
AID1063992Inhibition of Electrophorus electricus acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured for 30 mins by Ellman's method2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Cholinesterase inhibitory activity versus aromatic core multiplicity: a facile green synthesis and molecular docking study of novel piperidone embedded thiazolopyrimidines.
AID271050Selectivity for horse serum BChE over electric eel AChE2006Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase.
AID1682145Inhibition of acetylcholinesterase (unknown origin)2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1140465Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 6 mins followed by substrate addition by Ellman's method2014Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease.
AID482723Inhibition of AChE assessed as minimum drug level causing white zone of enzyme inhibition by TLC bioautography2010Journal of natural products, May-28, Volume: 73, Issue:5
Semisynthesis and acetylcholinesterase inhibitory activity of stemofoline alkaloids and analogues.
AID1273004Inhibition of electric eel AChE using ATC as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by Ellman's assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Ferulic acid-carbazole hybrid compounds: Combination of cholinesterase inhibition, antioxidant and neuroprotection as multifunctional anti-Alzheimer agents.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1811Experimentally measured binding affinity data derived from PDB2001Proteins, Feb-01, Volume: 42, Issue:2
Three-dimensional structure of a complex of galanthamine (Nivalin) with acetylcholinesterase from Torpedo californica: implications for the design of new anti-Alzheimer drugs.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2001Proteins, Feb-01, Volume: 42, Issue:2
Three-dimensional structure of a complex of galanthamine (Nivalin) with acetylcholinesterase from Torpedo californica: implications for the design of new anti-Alzheimer drugs.
AID1802055In vitro AChE and BChE Assay from Article 10.1016/j.bioorg.2016.10.002: \\Rational design and synthesis of dihydropyrimidine based dual binding site acetylcholinesterase inhibitors.\\2016Bioorganic chemistry, 12, Volume: 69Rational design and synthesis of dihydropyrimidine based dual binding site acetylcholinesterase inhibitors.
AID1799735Cholinesterase Inhibition Assay from Article 10.1080/14756360802236393: \\Butyrylcholinesterase inhibitory activity of testosterone and some of its metabolites.\\2009Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 24, Issue:2
Butyrylcholinesterase inhibitory activity of testosterone and some of its metabolites.
AID1802058Cholinesterase Inhibition Assay from Article 10.1111/cbdd.12773: \\Novel N-allyl/propargyl tetrahydroquinolines: Synthesis via Three-component Cationic Imino Diels-Alder Reaction, Binding Prediction, and Evaluation as Cholinesterase Inhibitors.\\2016Chemical biology & drug design, 10, Volume: 88, Issue:4
Novel N-allyl/propargyl tetrahydroquinolines: Synthesis via Three-component Cationic Imino Diels-Alder Reaction, Binding Prediction, and Evaluation as Cholinesterase Inhibitors.
AID1802597Cholinesterase Inhibition Assay from Article 10.1016/j.bioorg.2017.02.010: \\Synthesis of readily available fluorophenylalanine derivatives and investigation of their biological activity.\\2017Bioorganic chemistry, 04, Volume: 71Synthesis of readily available fluorophenylalanine derivatives and investigation of their biological activity.
AID1799683Enzyme Inhibition Assay from Article 10.1080/14756360600889708: \\New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids.\\2006Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 21, Issue:6
New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids.
AID1802939Acetylcholinesterase Inhibition Assay from Article 10.3109/14756360903213481: \\Nostotrebin 6, a bis(cyclopentenedione) with cholinesterase inhibitory activity isolated from Nostoc sp. str. Lukesovu00E1 27/97.\\2010Journal of enzyme inhibition and medicinal chemistry, Jun, Volume: 25, Issue:3
Nostotrebin 6, a bis(cyclopentenedione) with cholinesterase inhibitory activity isolated from Nostoc sp. str. Lukesová 27/97.
AID1797821In vitro BuChE Inhibition Assay from Article 10.1021/jm070536w: \\New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.\\2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.
AID1796450Enzyme Inhibition Assay from Article 10.1021/ja0466154: \\The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design.\\2004Journal of the American Chemical Society, Dec-01, Volume: 126, Issue:47
The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design.
AID1796451Enzyme Inhibition Assay from Article 10.1016/s0968-0896(98)00133-3: \\Potent acetylcholinesterase inhibitors: design, synthesis, and structure-activity relationships of bis-interacting ligands in the galanthamine series.\\1998Bioorganic & medicinal chemistry, Oct, Volume: 6, Issue:10
Potent acetylcholinesterase inhibitors: design, synthesis, and structure-activity relationships of bis-interacting ligands in the galanthamine series.
AID1800998Ellman's Method from Article 10.1016/j.bioorg.2014.11.005: \\Salicylanilide diethyl phosphates as cholinesterases inhibitors.\\2015Bioorganic chemistry, Feb, Volume: 58Salicylanilide diethyl phosphates as cholinesterases inhibitors.
AID1801810AChE Inhibitory Assay from Article 10.1111/cbdd.12732: \\Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.2016Chemical biology & drug design, 07, Volume: 88, Issue:1
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.
AID1802080Cholinesterase Inhibition Assay from Article 10.1111/cbdd.12800: \\Structure-activity relationship studies of benzyl-, phenethyl-, and pyridyl-substituted tetrahydroacridin-9-amines as multitargeting agents to treat Alzheimer's disease.\\2016Chemical biology & drug design, 11, Volume: 88, Issue:5
Structure-activity relationship studies of benzyl-, phenethyl-, and pyridyl-substituted tetrahydroacridin-9-amines as multitargeting agents to treat Alzheimer's disease.
AID1796482Cholinesterase Inhibition Assay from Article 10.1021/jm050578p: \\Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.\\2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
AID1796572Cholinesterase Inhibition Assay from Article 10.1021/jm010491d: \\Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.\\2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
AID1802583AChE/BChE Inhibition Assay from Article 10.1016/j.bioorg.2017.01.004: \\Synthesis, biological evaluation and docking studies of 2,3-dihydroquinazolin-4(1H)-one derivatives as inhibitors of cholinesterases.\\2017Bioorganic chemistry, 02, Volume: 70Synthesis, biological evaluation and docking studies of 2,3-dihydroquinazolin-4(1H)-one derivatives as inhibitors of cholinesterases.
AID1801040Anticholinesterase Activity Assays from Article 10.1016/j.bioorg.2015.02.002: \\Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives.\\2015Bioorganic chemistry, Apr, Volume: 59Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives.
AID1801888EqBuChE Inhibition Assay from Article 10.1016/j.bioorg.2016.05.004: \\New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives.\\2016Bioorganic chemistry, 08, Volume: 67New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives.
AID1797820In Vitro AChE Inhibition Assay from Article 10.1021/jm070536w: \\New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.\\2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.
AID1801887EeAChE Inhibition Assay from Article 10.1016/j.bioorg.2016.05.004: \\New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives.\\2016Bioorganic chemistry, 08, Volume: 67New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives.
AID1802975Enzyme Inhibition Assay from Article 10.3109/14756361003671078: \\Nantenine as an acetylcholinesterase inhibitor: SAR, enzyme kinetics and molecular modeling investigations.\\2011Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 26, Issue:1
Nantenine as an acetylcholinesterase inhibitor: SAR, enzyme kinetics and molecular modeling investigations.
AID1811Experimentally measured binding affinity data derived from PDB1999FEBS letters, Dec-17, Volume: 463, Issue:3
Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB1999FEBS letters, Dec-17, Volume: 463, Issue:3
Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution.
AID1345946Human acetylcholinesterase (Cartwright blood group) (Hydrolases)2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,711)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990248 (14.49)18.7374
1990's49 (2.86)18.2507
2000's625 (36.53)29.6817
2010's624 (36.47)24.3611
2020's165 (9.64)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 95.79

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index95.79 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.30 (4.65)
Search Engine Demand Index166.63 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (95.79)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials209 (11.15%)5.53%
Reviews0 (0.00%)6.00%
Reviews266 (14.19%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies47 (2.51%)4.05%
Observational0 (0.00%)0.25%
Observational10 (0.53%)0.25%
Other7 (100.00%)84.16%
Other1,342 (71.61%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (95)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Comparative, Randomized, Single-Dose, 2-way Crossover Bioavailability Study of Dr.Reddy's Laboratories, Ltd. and Janssen Pharmaceutical Products, l.P. (Reminyl®)4 mg Galantamine HBr Tablets in Healthy Adult Male Volunteers Under Fed Conditions [NCT01372306]Phase 124 participants (Actual)Interventional2004-10-31Completed
Evaluation of Three Potential CNS Pretreatments for Soman Exposure - Huperzine A, Donepezil, and Galantamine - on Human Performance [NCT01194336]84 participants (Actual)Observational2012-02-29Completed
Randomized, 2-Way Crossover, Bioequivalence Study of Galantamine 4 mg Tablet and Reminyl Following a 4 mg Dose in Healthy Subjects Under Fasting Conditions [NCT01190748]Phase 124 participants (Actual)Interventional2004-11-30Completed
Galantamine Treatment for Nonfluent Aphasia in Stroke Patients [NCT01129479]8 participants (Actual)Interventional2004-10-31Completed
An Open-Label Investigation of the Adjuvant Therapeutic Effects of Galantamine in Patients With Chronic Schizophrenia and Persistent Deficit Symptoms [NCT00161044]20 participants Interventional2004-09-30Completed
Oxytocin or Galantamine vs. Placebo for the Treatment of Negative Symptoms and Cognitive Impairments in Schizophrenia [NCT01012167]Phase 286 participants (Actual)Interventional2010-02-28Completed
A Discontinuation of Cholinesterase Inhibitors for the Treatment of Severe Alzheimer's Disease in Long Term Care Setting [NCT02035982]Phase 340 participants (Actual)Interventional2010-07-31Completed
Enhancing Parasympathetic Activity to Improve Endothelial Dysfunction, Vascular Oxidative Stress in African Americans [NCT04769206]Phase 1/Phase 288 participants (Anticipated)Interventional2021-12-20Recruiting
Symptomatic Treatment of Vascular Cognitive Impairment [NCT02098824]Phase 2/Phase 330 participants (Anticipated)Interventional2014-02-28Recruiting
Effects of Cholinergic Stimulation on Visceral Fat, Oxidative Stress and Inflammatory Markers in Patients With Metabolic Syndrome: a Randomized Clinical Trial [NCT02283242]Phase 460 participants (Actual)Interventional2014-03-31Completed
Comparative, Randomized, Single-Dose, 2-way Crossover Bioavailability Study of Dr. Reddy's Laboratories, Ltd. and Janssen Pharmaceutical Products, l.P. (Reminyl®)4 mg Galantamine HBr Tablets in Healthy Adult Male Volunteers Under Fasting Conditions [NCT01372280]Phase 128 participants (Actual)Interventional2004-10-31Completed
Randomized, 2-Way Crossover, Bioequivalence Study of Galantamine 4 mg Tablet and Reminyl Following a 4 mg Dose in Healthy Subjects Under Fed Conditions [NCT01190761]Phase 124 participants (Actual)Interventional2004-12-31Completed
Galantamine Effects on Nicotine Responses in Smokers [NCT01417429]Phase 112 participants (Actual)Interventional2010-03-31Completed
Effects of Galantamine and Donépézil on the Amount and the Quality oh the Sleep in Patients Suffering From Alzheimer Disease. [NCT00750529]Phase 115 participants (Actual)Interventional2008-11-30Completed
The Efficacy and Safety of Galantamine for Dysfunction in Bipolar Disorder [NCT00741598]Phase 472 participants (Actual)Interventional2008-09-30Completed
A Randomized, Double-Blind, Placebo-controlled Trial of Long-term (2-year) Treatment of Galantamine in Mild to Moderately-Severe Alzheimer's Disease [NCT00679627]Phase 32,051 participants (Actual)Interventional2008-06-30Terminated(stopped due to Due to a pre-specified imbalance of deaths between treatment groups, the DSMB recommended early termination of the trial)
Interventions to Test the Alpha7 Nicotinic Receptor Model in Schizophrenia [NCT00509067]Phase 243 participants (Actual)Interventional2007-11-30Completed
Galantamine Effects on Cognitive Function in Marijuana Users [NCT00969696]Phase 129 participants (Actual)Interventional2009-08-31Completed
A Bioequivalent Study to Compare Galantamine Oral Solution With Marketed Galantamine Capsule After Single Oral Administration of 10 mg. [NCT00645554]Phase 12 participants (Actual)InterventionalCompleted
Non-interventional Study on Long-term Application of Galantamine and Nootropics in Patients With Alzheimer's Disease [NCT01009476]1,134 participants (Actual)Observational2006-03-31Completed
The Use of Galantamine HBr (Reminyl) in Electroconvulsive Therapy: Impact on Mood and Cognitive Functioning [NCT00566735]Phase 339 participants (Actual)Interventional2004-07-31Completed
Characteristics of Treatment Responders to Galantamine Administration in the Patients With Alzheimer's Disease [NCT01029132]66 participants (Actual)Interventional2007-04-30Completed
A Prospective, Open-labeled, Multicenter Study of Galantamine on the Attention and Frontal Function of the Patients With Dementia of Alzheimer Type [NCT00216515]Phase 4102 participants (Actual)Interventional2004-03-31Completed
Galantamine to Enhance Cognitive Behavioral Therapy for Cocaine Abuse With Methadone Maintained Individuals [NCT00809835]Phase 2120 participants (Actual)Interventional2007-12-31Completed
The Use of Galantamine (Reminyl ER) in Patients With MIXed Dementia: Effects on Cognition and Quality of Life [NCT00814658]Phase 422 participants (Actual)Interventional2008-06-30Completed
Phase IV Study for the Assessment of Modulating Effect of Galantamine (Reminyl PRC) on Circadian Rhythm in Patients With Moderate Alzheimer's Disease [NCT01181921]Phase 41 participants (Actual)Interventional2011-05-31Terminated(stopped due to The recruitment rate was very low (one screening failure and one early withdrawal patient))
A Randomized, Double Blind, Active Control, Flexible Dose, Multicenter Study to Evaluate Galantamine HBr in the Treatment of Alzheimer's Disease:Safety and Effectiveness of an Immediate-release Table Formulation. [NCT00645190]Phase 3215 participants (Actual)Interventional2004-03-31Completed
Evaluation of Efficacy and Safety of Galantamine in Subjects With Dementia of Alzheimer's Type Who Failed to Benefit From Donepezil [NCT01478633]Phase 4102 participants (Actual)Interventional2011-09-30Completed
Galantamine Augmentation of Escitalopram for Treatment of Depression Associated Cognitive Impairment in Outpatients - A Randomized Single Blind Clinical Trial [NCT00423969]Phase 420 participants Interventional2003-11-30Terminated
Galantamine Effects on Cognitive Function in Abstinent Cocaine Users [NCT00606801]34 participants (Actual)Interventional2007-06-30Completed
Vagal Stimulation in POTS - The Autonomic Inflammatory Reflex (Pilot 3) [NCT03124355]Phase 111 participants (Actual)Interventional2017-09-30Active, not recruiting
"Competence Network - Dementia (BMBF) Pharmacological and Psychosocial Treatment (Modul E.2) Part II: The Efficacy of a Combination Regimen in Patients With Mild to Moderate Probable Alzheimer's Disease" [NCT01921972]Phase 4232 participants (Actual)Interventional2004-11-30Completed
Placebo Controlled Evaluation of Galantamine in the Treatment of Alzheimer's Disease: Safety and Efficacy Under a Slow-Titration Regimen [NCT00000172]Phase 30 participants InterventionalCompleted
Diffusion Tensor Weighted MRI in Alzheimer's Disease: Prediction and Mapping of Symptomatic and Disease Modifying Treatment Effects of Galantamine (Reminyl®) [NCT00523666]Phase 420 participants (Anticipated)Interventional2006-09-30Recruiting
A Study of the Effect of Concomitant Administration of Multiple Doses of BMS-708163 on the Pharmacokinetics of Galantamine in Healthy Subjects [NCT01039194]Phase 118 participants (Actual)Interventional2010-01-31Completed
A Phase 4 Double-Blind, Placebo-Controlled Study of Galantamine to Improve Cognitive Dysfunction in Bipolar Disorder [NCT00195845]Phase 430 participants (Anticipated)Interventional2003-04-30Completed
Comparison of Therapeutic Strategies With Cholinesterase Inhibitors: Stop or Still (SOS) Trial [NCT03454646]Phase 41,205 participants (Anticipated)Interventional2024-06-01Not yet recruiting
Pilot Examination of Galantamine in the Management of Tic Disorders [NCT00226824]Phase 41 participants (Actual)Interventional2005-09-30Terminated(stopped due to Unable to recruit subjects into the trial.)
An Open Label 24-Week, Flexible Dose Trial to Assess the Safety and Efficacy of Galantamine in Patients With Dementia With Lewy Bodies [NCT00230997]Phase 350 participants Interventional2002-12-31Completed
A Double-blind, Randomized Pilot Study to Evaluate the Effects of Galantamine and Donepezil on Sleep and Attention and Gastrointestinal (GI) Tolerance in Patients With Mild to Moderate Alzheimer's Disease (AD) [NCT00035204]Phase 463 participants (Actual)InterventionalCompleted
Lewy Body Spectrum Disorders: Investigating Neuropsychiatric Benefit and Adverse Effects in Response to Cholinesterase Inhibitors Using Genetics and Brain SPECT [NCT01944436]57 participants (Actual)Observational2006-09-30Completed
Effects of Galantamine on Cognition [NCT01100775]Phase 212 participants (Actual)Interventional2010-05-31Completed
Galantamine in the Preventive Treatment of Chronic Post-Traumatic Headache [NCT00219869]Phase 430 participants Interventional2005-07-31Recruiting
Galantamine Versus Placebo in Childhood Autism [NCT00252603]Phase 320 participants Interventional2004-04-30Completed
Efficacy, Tolerability and Safety of Galantamine in the Treatment of Alzheimer's Disease [NCT00253188]Phase 3653 participants (Actual)Interventional1997-02-28Completed
Galantamine in the Treatment of Alzheimer's Disease: Flexible Dose Range Trial [NCT00253227]Phase 3387 participants (Actual)Interventional1997-07-31Completed
Placebo-Controlled Evaluation of Galantamine in the Treatment of Alzheimer's Disease: A Cardiac Safety Study. [NCT00309725]Phase 3139 participants (Actual)InterventionalCompleted
Placebo-controlled Confirmatory Study of Galantamine (R113675) for Alzheimer's Type Dementia [NCT00814801]Phase 3580 participants (Actual)Interventional2007-02-28Completed
Continuous Arterial Spin Labeling (CASL) MRI for Monitoring and Prediction of Drug Therapy in Alzheimers Disease (AD) [NCT00637442]30 participants (Anticipated)Interventional2008-02-29Active, not recruiting
Phase IV Study of General Clinical Research Center Of the Jinan Mental Hospital(TAIWAN) [NCT00626613]Phase 40 participants InterventionalActive, not recruiting
A Randomized 26-Week, Double-Blind, Placebo Controlled Trial to Evaluate the Safety and Efficacy of Galantamine in the Treatment of Vascular Dementia [NCT00035191]Phase 3254 participants (Actual)Interventional2001-10-31Completed
Randomized Controlled Trial of Galantamine, Methylphenidate, and Placebo for the Treatment of Cognitive Symptoms in Patients With Traumatic Brain Injury (TBI) and/or Posttraumatic Stress Disorder (PTSD) [NCT01416948]Phase 232 participants (Actual)Interventional2011-08-31Terminated(stopped due to The funding agency, DoD, determined that the study could not meet its enrollment numbers by the end of the grant.)
A Double-Blind Comparison of Galantamine HBr and Placebo in Adults With Attention Deficit Hyperactivity Disorder [NCT00181675]Phase 440 participants Interventional2002-12-31Completed
A European Multi-Center Study to Determine the Safety and Efficacy of Galanthamine Hydrobromide 40mg/Day (32 mg /Day GAL Base, Tid Dose Regimen) in Patients Diagnosed With Alzheimer-Type Dementia [NCT00338117]Phase 3554 participants (Actual)Interventional1995-08-31Completed
Targeting the Cholinergic Pathway in HIV-associated Inflammation and Cognitive Dysfunction [NCT03384784]Phase 2114 participants (Actual)Interventional2017-10-30Completed
An Open Pilot Study to Evaluate the Safety and Efficacy of Galantamine in the Treatment of Pick's Disease/Frontotemporal Dementia /Pick Complex [NCT00416169]Phase 241 participants (Actual)Interventional2003-05-31Completed
A Randomized Double-Blind Placebo-Controlled Trial to Evaluate the Efficacy and Safety of Galantamine in Patients With Mild Cognitive Impairment (MCI) Clinically at Risk for Development of Clinically Probable Alzheimer's Disease [NCT00236431]Phase 31,063 participants (Actual)Interventional2001-05-31Completed
Efficacy, Tolerability and Safety of Galantamine in the Treatment of Alzheimer's Disease [NCT00253201]Phase 3636 participants (Actual)InterventionalCompleted
Galantamine for Cognitive Deficits in Schizophrenia [NCT00463879]Phase 2/Phase 321 participants (Actual)Interventional2005-09-30Completed
The Efficacy of Galantamine Treatment on Attention in Patients With Alzheimer's Disease [NCT01054976]Phase 499 participants (Actual)Interventional2006-10-31Completed
Investigator Initiated Study: Galantamine CR Potential Enhancement of Attentional and Executive Function in Non-Demented Patients With Parkinson's Disease [NCT00211588]90 participants (Anticipated)Interventional2004-06-30Active, not recruiting
Long Term Treatment With Galantamine In Dementia [NCT00216502]Phase 3254 participants (Actual)Interventional2001-08-31Completed
A Study of Galantamine HBr as an Adjunctive Treatment to Atypical Antipsychotic Medications in Outpatients With Schizophrenia and Associated Cognitive Deficits. [NCT00077727]Phase 3107 participants (Actual)Interventional2003-03-31Completed
Galantamine ER Open Label Rapid Dose Escalation Trial in Alzheimer's Disease [NCT00082602]Phase 383 participants (Actual)Interventional2004-05-31Completed
Treatment of Tardive Dyskinesia With Galantamine [NCT00164242]Phase 436 participants Interventional2002-01-31Completed
[NCT00181636]25 participants InterventionalCompleted
Pilot Study of Galantamine and CBT4CBT to Reduce Post-taper Relapse for MAT [NCT03547622]Early Phase 16 participants (Actual)Interventional2018-05-01Completed
A Randomized Double Blind Placebo-Controlled Trial to Evaluate the Efficacy and Safety of Galantamine in Patients With Mild Cognitive Impairment (MCI) Clinically at Risk for Development of Clinically Probable Alzheimer's Disease. [NCT00236574]Phase 3974 participants (Actual)Interventional2001-05-31Completed
An Open-Label Trial of Adjunctive Galantamine Maintenance Therapy to Treat Functional Impairments in Chronic Outpatients With Schizophrenia [NCT00232349]Phase 421 participants (Actual)Interventional2005-02-28Terminated(stopped due to Study terminated due to no apparent benefit.)
The Safety and Efficacy of Galantamine in the Treatment of Vascular and Mixed Dementia [NCT00261573]Phase 3593 participants (Actual)Interventional1998-12-31Completed
An Open-Label Extension Study to Assess the Long-Term Safety and Tolerability of Galantamine HBr in the Treatment of Mild Cognitive Impairment [NCT00240695]Phase 3724 participants (Actual)Interventional2003-05-31Completed
Placebo-Controlled Evaluation of Galantamine in the Treatment of Alzheimer's Disease: Safety and Efficacy of a Controlled-Release Formulation [NCT00253214]Phase 3973 participants (Actual)Interventional2001-03-31Completed
An Observational Study of Clinical Outcomes and Safety Profile of Galantamine in the Treatment of Patients With Alzheimer's Disease Over an 18-month Period [NCT00299676]61 participants (Actual)Observational2005-05-31Completed
Effect of Nicotine Agonist Galantamine Added to High Potency Medications for Cognitive Function in Patients With Schizophrenia and Schizoaffective Disorder [NCT00320736]Phase 420 participants Interventional2004-01-31Completed
Long Term Safety and Efficacy of Galantamine in Alzheimer's Disease (Extension INT-8) [NCT00304629]Phase 3241 participants (Actual)Interventional2000-03-31Completed
Open Observational Study of Galantamine Hydrobromide Administration for the Treatment of Patients With Mild to Moderate Dementia of the Alzheimer Type [NCT00297362]344 participants (Actual)Observational2004-06-30Completed
Placebo-Controlled, Double-Blind Study of Galantamine (R113675) in the Treatment of Alzheimer's Disease. [NCT00301574]Phase 3398 participants (Actual)Interventional2001-04-30Completed
Evaluation de l'efficacité de la Galantamine Versus Placebo associée à Une Revalidation Neuropsychologique Chez Des Patients présentant un Trouble Cognitif après un Premier Infarctus cérébral : étude en Neuroimagerie Fonctionnelle [NCT01508494]Phase 247 participants (Actual)Interventional2011-06-29Completed
Treatment of Severe Alzheimer's Disease in a Residential Home, Nursing Home, or Geriatric Residential Setting: Evaluation of Efficacy and Safety of Galantamine Hydrobromide in a Randomised, Doubleblind, Placebo-Controlled Study. [NCT00216593]Phase 3415 participants (Actual)Interventional2003-12-31Completed
Comparative Effectiveness Research Trial of Alzheimer's Disease Drugs [NCT01362686]200 participants (Actual)Interventional2011-04-30Terminated(stopped due to Low study accrual caused the study to be ended early.)
Functional Neuroimaging (fMRI) Biomarker of Allosteric Nicotinic Receptor Modulation in Mild Alzheimer's Disease Patients: A Razadyne vs. Aricept Dose Escalation Trial [NCT00369603]Phase 44 participants (Actual)Interventional2006-10-31Terminated(stopped due to Reduced access to AchEI medication-naive mild AD patients.)
Cholinergic Enhancement as a Treatment for Nicotine Addiction [NCT01880099]60 participants (Actual)Interventional2013-12-31Completed
A Pilot Parallel Double-Blind, Randomized Trial of Galantamine for Subarachnoid Hemorrhage [NCT02872857]Phase 1/Phase 260 participants (Actual)Interventional2016-09-30Completed
Repurposing Cholinesterase Inhibitors for Smoking Cessation. [NCT01669538]Phase 298 participants (Actual)Interventional2012-08-31Completed
Racial Differences in Vagal Control of Glucose Homeostasis, Chronic Study [NCT03014323]Phase 10 participants (Actual)Interventional2017-01-31Withdrawn(stopped due to No fundings)
Adjunctive Galantamine for Treatment of Cognitive Impairments in Patients With Schizophrenia [NCT00176423]Phase 4117 participants (Actual)Interventional2002-05-31Completed
Donepezil/ Galantamine in the Treatment of Post-stroke Cognitively Impaired Rehabilitating Elderly [NCT00227994]Phase 440 participants (Actual)Interventional2003-04-30Completed
Racial Differences in Vagal Control of Glucose Homeostasis [NCT02365285]Phase 1/Phase 223 participants (Actual)Interventional2015-03-31Completed
The Use of Low-Dose Galantamine to Potentiate the Attention-Enhancing Effects of Low-Dose Nicotine [NCT02420327]43 participants (Actual)Interventional2014-09-30Completed
Cognitive Enhancement as a Target for Cocaine Pharmacotherapy [NCT01531153]93 participants (Actual)Interventional2011-09-30Completed
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
The Effect of the Acetylcholinesterase Inhibitor, Galantamine, on Short-term Abstinence [NCT01548638]Phase 213 participants (Actual)Interventional2012-02-29Completed
A Phase II, Multicenter, Randomized, Double-Blind, Parallel-Group, Placebo-Controlled Study to Investigate the Efficacy and Safety of RO4602522 Added to Background Alzheimer's Disease Therapy in Patients With Moderate Severity Alzheimer's Disease [NCT01677754]Phase 2542 participants (Actual)Interventional2012-10-24Completed
A Proof-of Concept Trial of Galantamine and Memantine for Cognitive Impairments in Schizophrenia: Is the Combination Effective? [NCT02234752]Phase 23 participants (Actual)Interventional2014-09-30Terminated(stopped due to Funding no longer available and PI no longer working at the institution)
An Observational, Multi-Center Study to Demonstrate That the Change of Attention Measure is Correlated With the Changes of Caregiver's Burden After Treatment With Galantamine in Patients With Alzheimer's Disease [NCT01734395]1,882 participants (Actual)Observational2007-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00176423 (4) [back to overview]Overall Cognitive Improvement Z-score
NCT00176423 (4) [back to overview]ECG Changes From Baseline to 12 Weeks.
NCT00176423 (4) [back to overview]Abnormal Involuntary Movement Scale (AIMS)
NCT00176423 (4) [back to overview]Simpson Angus Scale (SAS) Total Score
NCT00227994 (2) [back to overview]Physical Function (Measured by the FIM-motor)
NCT00227994 (2) [back to overview]Medication Tolerability
NCT00509067 (3) [back to overview]Clinical Global Impression
NCT00509067 (3) [back to overview]MATRICS Verbal Learning and Memory
NCT00509067 (3) [back to overview]Negative Symptoms Measured on Positive and Negative Syndrome Scale (PANSS)
NCT00566735 (3) [back to overview]Cognitive Functioning
NCT00566735 (3) [back to overview]Baseline Depressive Symptoms
NCT00566735 (3) [back to overview]Number of Side Effects
NCT00606801 (15) [back to overview]Performance on the Sustained Attention to Response Task (SART)- Mean Reaction Time for Correct Press on Go Trial
NCT00606801 (15) [back to overview]Performance on the Sustained Attention to Response Task (SART)- Number of Errors on Go Trials
NCT00606801 (15) [back to overview]Performance on the Modified Stroop Task (Cocaine-Stroop)- Stroop Effect
NCT00606801 (15) [back to overview]Paired Associate Learning (PAL) - Mean Errors
NCT00606801 (15) [back to overview]Paired Associate Learning (PAL) - Stages Complete
NCT00606801 (15) [back to overview]Pattern Recognition Memory (PRM) - Number Correct Answers
NCT00606801 (15) [back to overview]Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP A' (Sensitivity to Target Sequences)
NCT00606801 (15) [back to overview]Pattern Recognition Memory (PRM) - Response Time for Correct Answers
NCT00606801 (15) [back to overview]Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP B' (Strength to Detect to Target Sequences)
NCT00606801 (15) [back to overview]Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP Reaction Time
NCT00606801 (15) [back to overview]Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP Total Correct Rejections
NCT00606801 (15) [back to overview]Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP Total Hits
NCT00606801 (15) [back to overview]Performance on the Modified Stroop Task (Cocaine-Stroop)- Carry-over Effect
NCT00606801 (15) [back to overview]Performance on the Modified Stroop Task (Cocaine-Stroop)- Reaction Time
NCT00606801 (15) [back to overview]Performance on the Sustained Attention to Response Task (SART) - Number of Errors on NoGo Trials
NCT00679627 (9) [back to overview]Change From Baseline in Caregiver Time Spent With the Patient Measured Using the Assessment of Subject Accommodation Status and Caregiver Burden (APAS-CarB)
NCT00679627 (9) [back to overview]Change From Baseline in Disability Assessment in Dementia (DAD) Scores
NCT00679627 (9) [back to overview]Change From Baseline in the Mini-Mental State Examination (MMSE) Score
NCT00679627 (9) [back to overview]Change From Baseline in the Mini-Mental State Examination (MMSE) Score
NCT00679627 (9) [back to overview]The Number of Deaths Reported in Participants
NCT00679627 (9) [back to overview]Change From Baseline in Institutional Status
NCT00679627 (9) [back to overview]Change From Baseline in Patient Accommodation Measured Using the Assessment of Subject Accommodation Status and Caregiver Burden (APAS-CarB)
NCT00679627 (9) [back to overview]Change From Baseline in the Mini-Mental State Examination (MMSE) Subscales (Orientation, Registration, Attention and Calculation, Recall, and Language)
NCT00679627 (9) [back to overview]Change From Baseline in the Disability Assessment in Dementia (DAD) Subscales (Initiation, Planning and Organization, Effective Performance, Basic, Instrumental, and Leisure)
NCT00741598 (5) [back to overview]Quality of Life Satisfaction Questionnaire (Q-LES-Q)
NCT00741598 (5) [back to overview]Scores on the California Verbal Learning Test (CVLT-II) at Screening and Week 16
NCT00741598 (5) [back to overview]The Conners' Continuous Performance Test (CPT) at Baseline, Weeks 4, 8, 12, and 16
NCT00741598 (5) [back to overview]The Range of Impaired Functioning Tool (LIFE-RIFT)
NCT00741598 (5) [back to overview]Scores on the Wisconsin Card Sorting Test (WCST) at Screening and Week 16
NCT00809835 (3) [back to overview]Cocaine Use
NCT00809835 (3) [back to overview]Cognitive Function
NCT00809835 (3) [back to overview]Cocaine Abstinence
NCT00814658 (10) [back to overview]Reaction Time for Face Recognition Test at Baseline, Week 8, and Week 24
NCT00814658 (10) [back to overview]Reaction Time for Two-choice Reaction Time Test at Baseline, Week 8, and Week 24
NCT00814658 (10) [back to overview]Reaction Time for Simple Reaction Time Test at Baseline, Week 8, and Week 24
NCT00814658 (10) [back to overview]The Clinical Global Impression (CGI) at Week 4, Week 8, Week 16, and Week 24
NCT00814658 (10) [back to overview]The Neuropsychiatric Inventory (NPI) at Baseline, Week 8, and Week 24
NCT00814658 (10) [back to overview]The Quality of Life Assessment for Caregivers of Patients With Alzheimer's Disease (QoL- AD) Total Scores at Baseline, Week 8, Week 24
NCT00814658 (10) [back to overview]The Quality of Life Assessment for Patients With Alzheimer's Disease (QoL- AD) Total Scores at Baseline, Week 8, Week 24
NCT00814658 (10) [back to overview]The Quality of Life Assessment for Patients With Alzheimer's Disease (QoL- AD) Total Scores, Based on the Caregiver's Opinion, at Baseline, Week 8, Week 24
NCT00814658 (10) [back to overview]The Alzheimer's Disease Assessment Scale - Cognitive Subscale (ADAS-Cog) at Baseline, Week 8, and Week 24
NCT00814658 (10) [back to overview]Reaction Time for Word Recognition and Learning Test at Baseline, Week 8, and Week 24
NCT00814801 (5) [back to overview]Change From Baseline in the Alzheimer's Disease Assessment Scale - Japan Cognitive Subscale (ADAS-J Cog)
NCT00814801 (5) [back to overview]Change From Baseline in the Behavioral Pathology in Alzheimer's Disease Rating Scale (Behave-AD)
NCT00814801 (5) [back to overview]Change From Baseline in the Disability Assessment for Dementia (DAD)
NCT00814801 (5) [back to overview]Distribution of Clinician's Interview-Based Impression of Change Plus - Japan (CIBIC Plus-J)
NCT00814801 (5) [back to overview]Change From Baseline in the Mental Function Impairment Scale (MENFIS)
NCT01012167 (83) [back to overview]Arizona Sexual Experience Questionnaire (ASEX) Male
NCT01012167 (83) [back to overview]Barnes Akathisia Scale (BAS) - Global Score
NCT01012167 (83) [back to overview]Blood Oxytocin Levels
NCT01012167 (83) [back to overview]Brief Psychiatric Rating Scale (BPRS) - Psychosis Score
NCT01012167 (83) [back to overview]Brief Psychiatric Rating Scale (BPRS) - Total Score
NCT01012167 (83) [back to overview]Calgary Depression Scale (CDS) - Total Score
NCT01012167 (83) [back to overview]Electrocardiogram (EKG)
NCT01012167 (83) [back to overview]Laboratory Measures - A/G Ratio
NCT01012167 (83) [back to overview]Laboratory Measures - Albumin
NCT01012167 (83) [back to overview]Laboratory Measures - Alkaline Phosphatase
NCT01012167 (83) [back to overview]Laboratory Measures - ALT/SGPT
NCT01012167 (83) [back to overview]Laboratory Measures - AST/SGOT
NCT01012167 (83) [back to overview]Laboratory Measures - Bilirubin
NCT01012167 (83) [back to overview]Laboratory Measures - BUN
NCT01012167 (83) [back to overview]Laboratory Measures - Calcium
NCT01012167 (83) [back to overview]Laboratory Measures - Chloride
NCT01012167 (83) [back to overview]Laboratory Measures - Cholesterol
NCT01012167 (83) [back to overview]Laboratory Measures - CO2
NCT01012167 (83) [back to overview]Laboratory Measures - Globulin
NCT01012167 (83) [back to overview]Laboratory Measures - Glucose
NCT01012167 (83) [back to overview]Laboratory Measures - HDL
NCT01012167 (83) [back to overview]Laboratory Measures - LDL
NCT01012167 (83) [back to overview]Laboratory Measures - Potassium
NCT01012167 (83) [back to overview]Laboratory Measures - Protein
NCT01012167 (83) [back to overview]Laboratory Measures - Sodium
NCT01012167 (83) [back to overview]Laboratory Measures - Triglycerides
NCT01012167 (83) [back to overview]Laboratory Measures - VLDL
NCT01012167 (83) [back to overview]Mean Z-Scores for Composite Cognitive Primary Outcome* by Treatment Group and Week
NCT01012167 (83) [back to overview]Neurocognitive Assessment Battery (MCCB) - Attention Vigilance
NCT01012167 (83) [back to overview]Neurocognitive Assessment Battery (MCCB) - Composite Score
NCT01012167 (83) [back to overview]Neurocognitive Assessment Battery (MCCB) - Processing Speed
NCT01012167 (83) [back to overview]Neurocognitive Assessment Battery (MCCB) - Reasoning/Problem Solving
NCT01012167 (83) [back to overview]Neurocognitive Assessment Battery (MCCB) - Social Cognition
NCT01012167 (83) [back to overview]Neurocognitive Assessment Battery (MCCB) - Verbal Learning
NCT01012167 (83) [back to overview]Neurocognitive Assessment Battery (MCCB) - Visual Learning
NCT01012167 (83) [back to overview]Neurocognitive Assessment Battery (MCCB) - Working Memory
NCT01012167 (83) [back to overview]Positive and Negative Affect Schedule (PANAS) - Negative
NCT01012167 (83) [back to overview]Positive and Negative Affect Schedule (PANAS) - Positive
NCT01012167 (83) [back to overview]Reactions to Partner
NCT01012167 (83) [back to overview]Scale for the Assessment of Negative Symptoms (SANS) - Alogia
NCT01012167 (83) [back to overview]Scale for the Assessment of Negative Symptoms (SANS) - Anhedonia
NCT01012167 (83) [back to overview]Scale for the Assessment of Negative Symptoms (SANS) - Avolition
NCT01012167 (83) [back to overview]Scale for the Assessment of Negative Symptoms (SANS) - Blunted Affect
NCT01012167 (83) [back to overview]Scale for the Assessment of Negative Symptoms (SANS) Total Score
NCT01012167 (83) [back to overview]Simpson-Angus Scale (SAS)
NCT01012167 (83) [back to overview]Vital Signs - Diastolic Blood Pressure
NCT01012167 (83) [back to overview]Vital Signs - Pulse
NCT01012167 (83) [back to overview]Vital Signs - Systolic Blood Pressure
NCT01012167 (83) [back to overview]Willingness to Interact
NCT01012167 (83) [back to overview]Vital Signs - Weight
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Abdominal Pain
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Anorexia
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Bruising Easily
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Constipation
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Diarrhea
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Dizziness
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Dry Eye
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Dry Mouth
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Enuresis
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Excessive Tearing of the Eye
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Fever
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Headache
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Hyperhydrosis
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Hypersalivation
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Insomnia
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Malaise
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Mucosal Ulceration
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Nasal Irritation
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Nausea
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Rash
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Restlessness
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Sedation
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Sore Throat
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Stiffness
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Tinnitus
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Tremor
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Urticaria
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Uterine Contractions
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Vomiting
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Weight Loss
NCT01012167 (83) [back to overview]Side Effect Checklist (SEC) - Wheezing
NCT01012167 (83) [back to overview]Abnormal Involuntary Movement Scale (AIMS)
NCT01012167 (83) [back to overview]Arizona Sexual Experience Questionnaire (ASEX) Female
NCT01054976 (5) [back to overview]Change From Baseline in Choice Reaction Time
NCT01054976 (5) [back to overview]Change From Baseline in Alzheimer's Disease Assessment Scale - Cognitive Subscale (ADAS-Cog)
NCT01054976 (5) [back to overview]Change From Baseline in Korean Version of Disability Assessment for Demential Scale (DAD-K)
NCT01054976 (5) [back to overview]Change From Baseline in Seoul-Instrumental Activities of Daily Livings (S-IADL)
NCT01054976 (5) [back to overview]Change From Baseline in Simple Reaction Time
NCT01100775 (9) [back to overview]Trust Game (Dollar Amount Earned)
NCT01100775 (9) [back to overview]Facial Affect Recognition Score (Number of Responses)
NCT01100775 (9) [back to overview]The Brief Smell Identification Test (B-SIT) Score (Number of Correct Responses)
NCT01100775 (9) [back to overview]RVIP Target Hit and False Alarm (Number of Responses)
NCT01100775 (9) [back to overview]Hopkins Verbal Learning Test (HVLT) Score
NCT01100775 (9) [back to overview]RVIP Reaction Times (ms)
NCT01100775 (9) [back to overview]Reading the Mind in the Eyes Score (Number of Correct Responses)
NCT01100775 (9) [back to overview]Brief Assessment of Cognition for Schizophrenia (BACS) Score
NCT01100775 (9) [back to overview]Social Affiliation Measured by Social Affiliative Role Play (Rating Scale Score)
NCT01362686 (3) [back to overview]Discontinuation Rates
NCT01362686 (3) [back to overview]Healthy Aging Brain Care (HABC)-Monitor
NCT01362686 (3) [back to overview]Neuropsychiatric Inventory (NPI)
NCT01531153 (17) [back to overview]Heart Rate
NCT01531153 (17) [back to overview]Stroop- RT Correct Neutral
NCT01531153 (17) [back to overview]Digit Span- LDSF
NCT01531153 (17) [back to overview]Digit Span- LDSB
NCT01531153 (17) [back to overview]Digit Span- DSF
NCT01531153 (17) [back to overview]Digit Span- DSB
NCT01531153 (17) [back to overview]CANTAB SST- SD Correct
NCT01531153 (17) [back to overview]CANTAB SST- SSRT
NCT01531153 (17) [back to overview]CANTAB SST- Median Correct
NCT01531153 (17) [back to overview]CANTAB RVIP Measure: RVP FALSE ALARM
NCT01531153 (17) [back to overview]CANTAB RVIP Measure: RVP B
NCT01531153 (17) [back to overview]CANTAB RVIP Measure: RVP A
NCT01531153 (17) [back to overview]Blood Pressure- Systolic
NCT01531153 (17) [back to overview]Blood Pressure- Diastolic
NCT01531153 (17) [back to overview]Urine Toxicology
NCT01531153 (17) [back to overview]Stroop- Effect Drug Neutral Mean Correct
NCT01531153 (17) [back to overview]Stroop- RT Correct Drug
NCT01548638 (7) [back to overview]Number of Days of Abstinence During a 7-day Quit Attempt
NCT01548638 (7) [back to overview]Cognitive Performance: Working Memory Accuracy
NCT01548638 (7) [back to overview]Cognitive Performance: Working Memory Reaction Time
NCT01548638 (7) [back to overview]Side Effects of Galantamine
NCT01548638 (7) [back to overview]Subjective Symptoms (Negative Affect)
NCT01548638 (7) [back to overview]Subjective Symptoms (Nicotine Withdrawal)
NCT01548638 (7) [back to overview]Subjective Symptoms (Smoking Urges)
NCT01669538 (4) [back to overview]Subjective Symptoms
NCT01669538 (4) [back to overview]Common Side Effects of Galantamine Check List
NCT01669538 (4) [back to overview]Cognitive Performance
NCT01669538 (4) [back to overview]Total Number of Smoke-free Days (Biochemically Verified) During a 7-day Quit Attempt.
NCT01734395 (3) [back to overview]Change From Screening at Week 16 in Mini Mental State Exam Scores (MMSE)
NCT01734395 (3) [back to overview]Change From Baseline at Week 16 in Attention Questionnaire Scores (AQS)
NCT01734395 (3) [back to overview]Change From Baseline at Week 16 in Burden Interview (BI) Scores
NCT01880099 (1) [back to overview]Smoking Choice Procedure
NCT02234752 (8) [back to overview]KYN/TRP
NCT02234752 (8) [back to overview]KYNA/KYN
NCT02234752 (8) [back to overview]Kynurenic Acid (KYNA)
NCT02234752 (8) [back to overview]Kynurenine (KYN)
NCT02234752 (8) [back to overview]PIC/KYN
NCT02234752 (8) [back to overview]Picolinic Acid (PIC)
NCT02234752 (8) [back to overview]Free Tryptophan (TRP)
NCT02234752 (8) [back to overview]Change in Level of Cognition
NCT02365285 (2) [back to overview]Change in Oxidative Stress: Baseline to 4 Hours
NCT02365285 (2) [back to overview]Change in Oxidative Stress: Baseline to 2 Hours
NCT02420327 (7) [back to overview]Change Detection Task Reaction Time
NCT02420327 (7) [back to overview]Change Detection Task Accuracy
NCT02420327 (7) [back to overview]Spatial Attentional Resource Allocation Task (SARAT) Non-predictive Trial Reaction Time
NCT02420327 (7) [back to overview]Spatial Attentional Resource Allocation Task Predictive Trials Reaction Time
NCT02420327 (7) [back to overview]Rapid Visual Information Processing Task Reaction Time
NCT02420327 (7) [back to overview]Rapid Visual Information Processing Task Hit Rate
NCT02420327 (7) [back to overview]Profile of Mood Scale - Total Mood Disturbance
NCT02872857 (5) [back to overview]Montreal Cognitive Assessment (MoCA)
NCT02872857 (5) [back to overview]Mortality
NCT02872857 (5) [back to overview]Montreal Cognitive Assessment (MoCA)
NCT02872857 (5) [back to overview]EuroQOL Score as Assessed by a Visual Analogue Scale (VAS)
NCT02872857 (5) [back to overview]Tolerability as Assessed by the Number of Participants Who Stop Study Medication Due to Adverse Event Possibly Associated With Study Drug
NCT03547622 (3) [back to overview]Substance Use Calendar
NCT03547622 (3) [back to overview]Clinical Opioid Withdrawal Scale (COWS)
NCT03547622 (3) [back to overview]Change in Methadone/Buprenorphine Dose to 0 mg for Successful Completion of Taper

Overall Cognitive Improvement Z-score

Participants were administered an eight-test neuropsychological test battery at baseline and end-of-study. The battery included the following tests: working memory: WAIS-III Letter-Number Sequencing and Brief Assessment of Cognition in Schizophrenia Number Sequencing; verbal memory: California Verbal Learning Test (CVLT); visual memory: Brief Visuospatial Memory Test (BVMT); motor speed: Grooved Pegboard; processing speed: WAIS-III Digit Symbol and WAIS-III Symbol Search; and the Gordon Diagnostic System CPT. Alternate forms of the CVLT and BVMT were used for the two test occasions. For each neuropsychological test, participant scores were converted to z-scores: z = (score - baseline mean)/baseline SD. For the primary outcome measure, an overall composite z-score was computed from the average of the individual test z-scores. A positive z-score would reflect better performance compared to baseline; a negative z-score would reflect worse performance compared to baseline. (NCT00176423)
Timeframe: 12 weeks

,
Interventionz-score (Mean)
Week 0Week 12
Galantamine0.030.15
Placebo-0.030.61

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ECG Changes From Baseline to 12 Weeks.

Three measures were examined: PR interval, QRS interval, and QTc interval. The three measures were derived from a standard 12-lead ECG recording. (NCT00176423)
Timeframe: 12 weeks

,
Interventionmsec (Mean)
PR intervalQRS intervalQTc interval
Galantamine25.711.43.03
Placebo3.0-1.63.03

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Abnormal Involuntary Movement Scale (AIMS)

"Change in AIMS Total Score: Frequencies of Maximum Within-Participant Increases (worsening) from Baseline by Treatment Group. Total score calculated by adding scores from scales #1-#10. Each scale ranges from 0=None to 4=Severe. The minimum total AIMS score is 0 and the maximum score is 40. Higher scores indicate a more severe abnormal involuntary movement rating." (NCT00176423)
Timeframe: 12 weeks (Week 12 - Week 0)

,
Interventionscore on a scale (Mean)
Week 0Week 12
Galantamine2.02.1
Placebo2.11.6

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Simpson Angus Scale (SAS) Total Score

"The SAS total were calculated by adding scores from scales #1-#11. Each scale ranges from 0=None/Normal to 4=Extreme/Severe. The minimum total score is 0 and the maximum score is 44. Higher scores indicate a more severe extrapyramidal side effect rating." (NCT00176423)
Timeframe: 12 weeks (Week 12 - Week 0)

,
Interventionscore on a scale (Mean)
Week 0Week 12
Galantamine1.41.1
Placebo1.61.6

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Physical Function (Measured by the FIM-motor)

Score on Functional Independence Measure (FIM) motor score, where 7 indicates total assistance/complete dependence and 91 is complete independence (NCT00227994)
Timeframe: Measured at weeks 0 and 12

,
Interventionunits on a scale (Mean)
Baseline FIMWeek 12 FIM
Donepezil49.487.4
Galantamine47.173.1

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Medication Tolerability

Number of participants who withdrew due to side effects. (NCT00227994)
Timeframe: Measured throughout the study

Interventionparticipants (Number)
Galantamine5
Donepezil5

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Clinical Global Impression

The score for each subject was the mean rating on the severity item. The score of the item ranged from 1 (normal) to 7 (among most severely ill). (NCT00509067)
Timeframe: Measured at Baseline and Weeks 4, 8, 12, and 16

,
Interventionunits on a scale (Mean)
BaselineWeek 4Week 8Week 12Week 16
Galantamine and CDP-choline Group4.3243.673.873.8
Placebo Group4.383.924.0443.68

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MATRICS Verbal Learning and Memory

The measure of verbal learning and memory is the Hopkins Verbal Learning Test. The score for each subject is the sum of the total number of words recalled correctly for Trials 1, 2, and 3. The measure is the mean of these scores at baseline, Week 8, and Week 16. (NCT00509067)
Timeframe: Measured at Baseline and Weeks 8 and 16

,
Interventionraw scores (Mean)
BaselineWeek 8Week 16
Galantamine and CDP-choline Group20.521.823.0
Placebo Group20.621.220.4

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Negative Symptoms Measured on Positive and Negative Syndrome Scale (PANSS)

The score for each subject was the sum of the ratings for five items on the negative-symptom subscale of the PANSS: 1) blunted affect, 2) emotional withdrawal, 3) poor rapport, 4) passive/apathetic social withdrawal, and 5) lack of spontaneity and flow of conversation. Each item (symptom) is rated on a scale from 1 = absence of negative symptom to 7 = extreme negative symptom. The sum of the ratings for the five items range from 5 to 35, with higher scores indicating more severe symptoms. The primary outcome measure is the mean of the sum of these ratings across subjects. (NCT00509067)
Timeframe: Measured at Baseline and Weeks 4, 8, 12, and 16

,
Interventionunits on a scale (Mean)
BaselineWeek 4Week 8Week 12Week 16
Galantamine/CDP Choline17.6317.0613.9314.9313.93
Placebos for Galantamine/CDP Choline18.2917.0817.2617.3216.05

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Cognitive Functioning

This measure refers to participants' scores on the Delayed Memory Index (DMI) compared from baseline (before first ECT) to discharge (after last ECT). The score can range from 40 to 137. The higher the score, the better, in terms of cognitive functioning. (NCT00566735)
Timeframe: Participants were questioned at baseline and after their last electroconvulsive therapy treatment

,
InterventionScore on the DMI (Mean)
Pre-ECTPost-ECT
Galantamine88.7588.17
Placebo80.3368.50

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Baseline Depressive Symptoms

This measure refers to the Hamilton Rating Scale for Depression-17 scores (HAM-D-17) which can range from 0 to 50, with <7 referring to mild-to-no depression, and >23 referring to severe depression. (NCT00566735)
Timeframe: Participants were questioned at baseline

InterventionScore on the HAM-D-17 (Mean)
Placebo24.53
Galantamine27.33

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Number of Side Effects

This measure refers to the number of reported side effects experienced by participants during the study. The side effects were nausea, headache, dizziness, diarrhea, and vomiting. (NCT00566735)
Timeframe: Participants were followed for the duration of hospital stay, an average of 3 weeks

InterventionNumber of reported side effects (Number)
Placebo19
Galantamine13

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Performance on the Sustained Attention to Response Task (SART)- Mean Reaction Time for Correct Press on Go Trial

"The SART is a Go / NoGo task measuring the ability to activate or inhibit responses. In this 4.5 minute task, 225 single digits (25 × 9 digits) were presented on a computer monitor. Each digit was presented for 250 ms, and was immediately followed by a mask for 900 ms. The mask consists of a ring with a diagonal cross in the center. Subjects were instructed to press a spacebar to every digit except the 3, and to give equal importance to speed and accuracy. Responses were allowed during the presentation of both the digit and mask. The digits were presented in a different random order for each subject. There were 18 practice trials, containing 2 no-response targets (3s).~For the Go trial, the reaction time reflected the response activation function, faster reaction time indicating greater response activation.~Complete data for 3 subjects in the Placebo group, and for 1 subject in the galantamine group were not capture do to experimenter and computer errors." (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionmilliseconds (Mean)
BaselineDay 5Day 10
Galantamine375.3382.6357.8
Placebo399.7405.4411.1

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Performance on the Sustained Attention to Response Task (SART)- Number of Errors on Go Trials

"The SART is a Go / NoGo task measuring the ability to activate or inhibit responses. In this 4.5 minute task, 225 single digits (25 × 9 digits) were presented on a computer monitor. Each digit was presented for 250 ms, and was immediately followed by a mask for 900 ms. The mask consists of a ring with a diagonal cross in the center. Subjects were instructed to press a spacebar to every digit except the 3, and to give equal importance to speed and accuracy. Responses were allowed during the presentation of both the digit and mask. The digits were presented in a different random order for each subject. There were 18 practice trials, containing 2 no-response targets (3s). The number of errors on Go trials reflected the response activation function, with fewer errors indicating greater response activation.~Complete data for 3 subjects in the Placebo group, and for 1 subject in the galantamine group were not capture do to experimenter and computer errors." (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionthe number of errors (Mean)
BaselineDay 5Day 10
Galantamine7.23.85.1
Placebo14.612.010.6

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Performance on the Modified Stroop Task (Cocaine-Stroop)- Stroop Effect

The Cocaine-Stroop task measures attention capture (attentional bias) secondary to cocaine cues; (Stroop effect - calculated as the difference between mean RT on cocaine words and mean RT on control words). Subjects completed 2 counterbalanced blocks (150 trials per block). One block contained 15 cocaine words and neutral words in a mixed order. The other block contained 15 control words matched in length and frequency to cocaine words, and a different set of neutral words. Subjects were required to indicate the colors in which the words were written as quickly and accurately as possible. Reaction times for identification of word color was measured. In addition, the difference in RT to words following cocaine and control words were measured (carry-over effect). Complete data for 3 participants (2 placebo and 1 galantamine) were not capture due to experimenter and computer errors. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionmilliseconds (Mean)
BaselineDay 5Day 10
Galantamine-13.119.6-33.7
Placebo10.5-19.7-61.5

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Paired Associate Learning (PAL) - Mean Errors

Rapid Visual Processing test (RVIP) is a measure of sustained attention with a small working memory component that is sensitive to cholinergic enhancers. In the Paired Associate Learning (PAL) task, boxes are displayed on the screen and are opened in a random order. One or more of the boxes will contain a pattern. After the subjects have seen the patterns behind each box, the patterns are then displayed in the middle of the screen, one at a time, and the subject must touch the box where the pattern was originally located. An error will cause the test to open the boxes again to remind the subject of their locations. The number of boxes with patterns increases throughout the test. The stages completed and number of errors are measures of interest. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionerrors (Mean)
BaselineDay 5Day 10
Galantamine25.618.116.8
Placebo31.123.617.7

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Paired Associate Learning (PAL) - Stages Complete

Rapid Visual Processing test (RVIP) is a measure of sustained attention with a small working memory component that is sensitive to cholinergic enhancers. In the Paired Associate Learning (PAL) task, boxes are displayed on the screen and are opened in a random order. One or more of the boxes will contain a pattern. After the subjects have seen the patterns behind each box, the patterns are then displayed in the middle of the screen, one at a time, and the subject must touch the box where the pattern was originally located. An error will cause the test to open the boxes again to remind the subject of their locations. The number of boxes with patterns increases throughout the test. The stages completed and number of errors are measures of interest. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventioncompleted stages (Mean)
BaselineDay 5Day 10
Galantamine4.94.94.9
Placebo4.84.94.9

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Pattern Recognition Memory (PRM) - Number Correct Answers

Pattern Recognition Memory (PRM) tests visual pattern recognition memory in a two choice forced discrimination paradigm. 12 visual patterns are presented, then the subject must choose between each of these patterns and a novel pattern. The number of correct responses are measured. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionnumber correct answers (Mean)
BaselineDay 5Day 10
Galantamine20.220.620.7
Placebo20.814.921.0

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Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP A' (Sensitivity to Target Sequences)

Rapid Visual Processing test (RVIP) is a measure of sustained attention with a small working memory component that is sensitive to cholinergic enhancers. In the RVIP, subjects must detect either odd or even 3 digit sequences appearing in a box in a pseudo-random order at 100 digits per minute. A' is a measure of sensitivity to target sequences and it reflects probabilities of hits and false alarms to provide a score of sensitivity to the target regardless of response tendency. The scores range from 0 (bad) to 1 (good). (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionsensitivity index (Mean)
BaselineDay 5Day 10
Galantamine0.870.900.92
Placebo0.890.900.90

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Pattern Recognition Memory (PRM) - Response Time for Correct Answers

In the PRM, the subject is presented with a series of 12 visual patterns, one at a time, in the center of the screen. These patterns are designed so that they cannot easily be given verbal labels. In the recognition phase, the subject is required to choose between a pattern they have already seen and a novel pattern. The time to correct answer was measured. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionmilliseconds (Mean)
BaselineDay 5Day 10
Galantamine243920921889
Placebo235720921995

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Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP B' (Strength to Detect to Target Sequences)

Rapid Visual Processing test (RVIP) is a measure of sustained attention with a small working memory component that is sensitive to cholinergic enhancers. In the RVIP, subjects must detect either odd or even 3 digit sequences appearing in a box in a pseudo-random order at 100 digits per minute. B reflects the probability of hits and false alarms to provide a measure of the participants tendency to respond regardless of whether the target sequence is presented. The scores range from -1 to +1 with scores near +1 indicative of a subject that gave few false alarms. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionspecificity index (Mean)
BaselineDay 5Day 10
Galantamine.88.91.88
Placebo.88.82.85

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Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP Reaction Time

Rapid Visual Processing test (RVIP) is a measure of sustained attention with a small working memory component that is sensitive to cholinergic enhancers. In the RVIP, subjects must detect either odd or even 3 digit sequences appearing in a box in a pseudo-random order at 100 digits per minute. Reaction time (RT) to correct answers was measured. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionmilliseconds (Mean)
BaselineDay 5Day 10
Galantamine476.8379.2386.9
Placebo407.7427.4433.3

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Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP Total Correct Rejections

Rapid Visual Processing test (RVIP) is a measure of sustained attention with a small working memory component that is sensitive to cholinergic enhancers. In the RVIP, subjects must detect either odd or even 3 digit sequences appearing in a box in a pseudo-random order at 100 digits per minute. The number of correct rejections was measured. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventioncorrect rejections (Mean)
BaselineDay 5Day 10
Galantamine242.4247.9253.9
Placebo247.2217.6248.2

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Performance on the Cambridge Neuropsychological Test Automated Battery (CANTAB) - RVIP Total Hits

Rapid Visual Processing test (RVIP) is a measure of sustained attention with a small working memory component that is sensitive to cholinergic enhancers. In the RVIP, subjects must detect either odd or even 3 digit sequences appearing in a box in a pseudo-random order at 100 digits per minute. The total hits were measured (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionhits (Mean)
BaselineDay 5Day 10
Galantamine14.816.919.7
Placebo16.718.018.0

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Performance on the Modified Stroop Task (Cocaine-Stroop)- Carry-over Effect

The Cocaine-Stroop task measures attention capture (attentional bias) secondary to cocaine cues; (Stroop effect - calculated as the difference between mean RT on cocaine words and mean RT on control words). Subjects completed 2 counterbalanced blocks (150 trials per block). One block contained 15 cocaine words and neutral words in a mixed order. The other block contained 15 control words matched in length and frequency to cocaine words, and a different set of neutral words. Subjects were required to indicate the colors in which the words were written as quickly and accurately as possible. Reaction times for identification of word color was measured. In addition, the difference in RT to words following cocaine and control words were measured (carry-over effect). Complete data for 3 participants (2 placebo and 1 galantamine) were not capture due to experimenter and computer errors. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionmilliseconds (Mean)
BaselineDay 5Day 10
Galantamine13.432.118.6
Placebo32.443.5-29.8

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Performance on the Modified Stroop Task (Cocaine-Stroop)- Reaction Time

The Cocaine-Stroop task measures attention capture (attentional bias) secondary to cocaine cues; (Stroop effect - calculated as the difference between mean RT on cocaine words and mean RT on control words). Subjects completed 2 counterbalanced blocks (150 trials per block). One block contained 15 cocaine words and neutral words in a mixed order. The other block contained 15 control words matched in length and frequency to cocaine words, and a different set of neutral words. Subjects were required to indicate the colors in which the words were written as quickly and accurately as possible. Reaction times for identification of word color was measured. In addition, the difference in RT to words following cocaine and control words were measured (carry-over effect). Complete data for 3 participants (2 placebo and 1 galantamine) were not capture due to experimenter and computer errors. (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionmilliseconds (Mean)
BaselineDay 5Day 10
Galantamine771742698
Placebo722734748

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Performance on the Sustained Attention to Response Task (SART) - Number of Errors on NoGo Trials

"The SART is a Go / NoGo task measuring the ability to activate or inhibit responses. In this 4.5 minute task, 225 single digits (25 × 9 digits) were presented on a computer monitor. Each digit was presented for 250 ms, and was immediately followed by a mask for 900 ms. The mask consists of a ring with a diagonal cross in the center. Subjects were instructed to press a spacebar to every digit except the 3, and to give equal importance to speed and accuracy. Responses were allowed during the presentation of both the digit and mask. The digits were presented in a different random order for each subject. There were 18 practice trials, containing 2 no-response targets (3s). For the Go/NoGo task, response inhibition was measured as the number of errors on the no- Go trials, with low errors indicating better response inhibition.~Complete data for 3 subjects in the Placebo group, and for 1 subject in the galantamine group were not capture do to experimenter and computer errors." (NCT00606801)
Timeframe: Baseline, Day 5 and Day 10

,
Interventionnumber of errors (Mean)
BaselineDay 5Day 10
Galantamine13.110.212.2
Placebo12.810.711.8

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Change From Baseline in Caregiver Time Spent With the Patient Measured Using the Assessment of Subject Accommodation Status and Caregiver Burden (APAS-CarB)

The table below presents the number of days that caregiving activities were provided during the past week. (NCT00679627)
Timeframe: Baseline, Months 12 and 24

,
InterventionDays (Mean)
Provided caregiving during past week - BaselineProvided caregiving during past week - Month 12Provided caregiving during past week - Month 24
Galantamine5.776.076.20
Placebo5.916.066.13

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Change From Baseline in Disability Assessment in Dementia (DAD) Scores

The DAD assesses physical activities of daily living and instrumental-activities of daily livings of participants with Alzheimer disease. This measure is a validated, disability assessment scale that collects information regarding the ability of a participant to initiate, plan, organize, and perform activities of daily living, as based on a structured interview with the caregiver. The maximum scores were 13 for initiation, 10 for planning and organizing, and 17 for effective performance in order to yield a total maximum score of 40. These scores were normalized to a scale of 100 for analysis.A higher score, or percentage of items that can be performed represents fewer disabilities in carrying out activities of daily living while a lower percentage indicates an increase in disabilities. (NCT00679627)
Timeframe: Baseline, Month 24

InterventionScores on scale (Mean)
Placebo-10.81
Galantamine-8.16

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Change From Baseline in the Mini-Mental State Examination (MMSE) Score

The MMSE is a brief 30-point questionnaire test that is used or the assessment of dementia patients' cognitive impairment. Evaluation of points are as follows: 24 to 30 = no cognitive impairment, 18 to 23 = mild cognitive impairment, 0 to 17 = severe cognitive impairment. Lower scores indicate worsening. (NCT00679627)
Timeframe: Baseline, Month 24

InterventionScores on scale (Mean)
Placebo-2.14
Galantamine-1.41

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Change From Baseline in the Mini-Mental State Examination (MMSE) Score

The MMSE is a brief 30-point questionnaire test that is used or the assessment of dementia patients' cognitive impairment. Evaluation of points are as follows: 24 to 30 = no cognitive impairment, 18 to 23 = mild cognitive impairment, 0 to 17 = severe cognitive impairment. Lower scores indicate worsening. (NCT00679627)
Timeframe: Baseline, Month 6

InterventionScores on scale (Mean)
Placebo-0.28
Galantamine0.15

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The Number of Deaths Reported in Participants

An external Data Safety Monitoring Board (DSMB) was assigned for this study to monitor the progress of the study and to ensure that the safety of participants was not compromised. (NCT00679627)
Timeframe: Up to 2 years

InterventionNumber of Participants (Number)
Placebo56
Galantamine33

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Change From Baseline in Institutional Status

This table describes the number of participants who were reported as institutionalized at baseline and Month 24. (NCT00679627)
Timeframe: Baseline, Month 24

,
InterventionNumber of Participants (Number)
BaselineMonth 24
Galantamine06
Placebo15

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Change From Baseline in Patient Accommodation Measured Using the Assessment of Subject Accommodation Status and Caregiver Burden (APAS-CarB)

"The APAS-CarB is a measure used to evaluate participant status and caregiver burden. The table below presents Patient Accommodation assessed as the percentage of participants home with friend or relative using the APAS-CarB." (NCT00679627)
Timeframe: Baseline, Months 12 and 24

,
InterventionPercentage of participants (Number)
Home with friend or relative - BaselineHome with friend or relative - Month 12Home with friend or relative - Month 24
Galantamine62.861.860.1
Placebo62.161.455.3

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Change From Baseline in the Mini-Mental State Examination (MMSE) Subscales (Orientation, Registration, Attention and Calculation, Recall, and Language)

The MMSE, is a validated, brief examination that rates subjects on orientation (total score, 10), registration (total score, 3), attention (total score, 5), calculation (total score, 5), recall (total score, 3), and language (total score, 9). The maximum score is 30 (only the higher of the two scores for attention and calculation [each with a maximum score of 5] was used). A higher score compared with baseline indicates less impairment. (NCT00679627)
Timeframe: Baseline, Month 24

,
InterventionScores on scale (Mean)
OrientationRegistrationAttention and CalculationRecallLanguage
Galantamine-0.76-0.16-0.160.10-0.68
Placebo-0.96-0.20-0.460.00-0.93

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Change From Baseline in the Disability Assessment in Dementia (DAD) Subscales (Initiation, Planning and Organization, Effective Performance, Basic, Instrumental, and Leisure)

The DAD assesses physical activities of daily living and instrumental-activities of daily livings of participants with Alzheimer disease. This measure is a validated, disability assessment scale that collects information regarding the ability of a participant to initiate, plan, organize, and perform activities of daily living, as based on a structured interview with the caregiver. The maximum scores were 13 for initiation, 10 for planning and organizing, and 17 for effective performance in order to yield a total maximum score of 40. These scores were normalized to a scale of 100 for analysis.A higher score, or percentage of items that can be performed represents fewer disabilities in carrying out activities of daily living while a lower percentage indicates an increase in disabilities. (NCT00679627)
Timeframe: Baseline, Month 24

,
InterventionScores on scale (Mean)
InitiationPlanning and OrganizationEffective PerformanceBasicInstrumentalLeisure
Galantamine-9.60-9.96-10.82-9.84-10.72-10.46
Placebo-13.53-13.14-13.82-14.24-13.52-13.02

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Quality of Life Satisfaction Questionnaire (Q-LES-Q)

"The Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) is a self-report instrument designed to measure the degree of enjoyment and satisfaction experienced by subjects in various areas of daily functioning. There are 16 areas of functioning, each scored from 1 (very poor) to 5 (very good). The range of scores is 16-80, with lower scores representing lower functioning and satisfaction.~The outcome measures presented are Q-LES-Q Total score = Sum of all scores from all 16 areas of functioning" (NCT00741598)
Timeframe: Screening

,
Interventionunits on a scale (Mean)
Q-LES-Q Total, BaselineQ-LES-Q Total, Week 4Q-LES-Q Total, Week 8Q-LES-Q Total, Week 12Q-LES-Q Total, Week 16
Galantamine-ER62.366.0362.6266.9664.75
Placebo63.0364.7565.2866.5261.31

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Scores on the California Verbal Learning Test (CVLT-II) at Screening and Week 16

"CVLT is a test measuring verbal learning and verbal memory. Subjects are expected to remember a list of words. They are asked to repeat the words remembered 5 times (5 trials). Each of the words correctly remembered, in each trial, is marked as 1 point. The outcome measures presented are:~CVLT Total Trials 1-5, Baseline = Number of total words remembered, sum of trials 1-5, at baseline CVLT Total Trials 1-5, Week 16 = Number of total words remembered, sum of trials 1-5, at week 16." (NCT00741598)
Timeframe: Measured at screening and Week 16

,
Interventionnumber of total words remembered (Mean)
CVLT Total Trials 1-5, BaselineCVLT Total Trials 1-5, Week 16
Galantamine-ER50.1558.88
Placebo47.2152.90

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The Conners' Continuous Performance Test (CPT) at Baseline, Weeks 4, 8, 12, and 16

"Conner's CPT (Conner's Continuous Performance Task) is a neuropsychological test that measures a person's sustained and selective attention. Subjects are instructed to click the space bar when they are presented with any letter except the letter X. The person must refrain from clicking if they see the letter X presented. Clicking to the letter X is a commission error, not clicking to other letters are omission errors.~The outcome measures presented are Total number of errors = Total number of omission + commission errors This outcome measure is presented at each study visit (baseline, week 4, week 8, week 12, and week 16)" (NCT00741598)
Timeframe: Measured at screening; baseline; and Weeks 4, 8, 12, and 16

,
Interventiontotal number of errors (Mean)
CPT Total omission + commission errors, BaselineCPT Total omission + commission errors, Week 4CPT Total omission + commission errors, Week 8CPT Total omission + commission errors, Week 12CPT Total omission + commission errors, Week 16
Galantamine-ER22.1621.8715.619.9114.23
Placebo19.4019.2416.3916.4115.18

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The Range of Impaired Functioning Tool (LIFE-RIFT)

The LIFE-RIFT is a brief measure of functional impairment. The total scale score is a sum of four items with range of scale from 0 to 26 (from no impairment to severe impairment). (NCT00741598)
Timeframe: Baseline, Weeks 4, 8, 12, and 16

,
Interventionunits on a scale (Mean)
LIFE-RIFT total score, BaselineLIFE-RIFT total score, Week 4LIFE-RIFT total score, Week 8LIFE-RIFT total score, Week 12LIFE-RIFT total score, Week 16
Galantamine-ER10.399.669.078.248.88
Placebo9.419.038.538.038.20

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Scores on the Wisconsin Card Sorting Test (WCST) at Screening and Week 16

"WCST (Wisconsin Card Sorting Test) is a neuropsychological test measuring the ability to display flexibility in the face of changing schedules of reinforcement. Subjects are presented with cards and requested to match them. Unbeknownst to the subject, the matching rules change while the test is delivered. The test measures subjects' ability to understand the new rules.~The outcome measures presented are Total correct baseline = total correct card choices at baseline Total errors baseline = total erroneous card choices at baseline Total correct week 16 = total correct card choices at week 16 Total errors baseline = total erroneous card choices at week 16" (NCT00741598)
Timeframe: Measured at screening and Week 16

,
Interventionnumber of card choices made (Mean)
Total Correct BaselineTotal Errors BaselineTotal Correct Week 16Total Errors Week 16
Galantamine-ER45.8729.7051.9427.75
Placebo44.1129.7944.2829.61

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Cocaine Use

Reduction in cocaine use, operationalized as the frequency of cocaine use by month using timeline followback. (NCT00809835)
Timeframe: 12 weeks

,,,
InterventionDays (Mean)
Baseline12 Weeks
Galantamine14.816.32
Galantamine and CBT18.828.60
Placebo and CBT15.687.65
Placebo Only14.8510.25

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Cognitive Function

"A composite using a carefully selected neuropsychological battery that includes measures of executive cognitive functioning frequently affected among cocaine users, likely to be important moderators of CBT4CBT, and sensitive to galantamine effects. These will include measures of multiple aspects of attention, cognitive inhibition, sustained attention (CANTAB), decision making (BART), and memory (digit span).~Scores ranged from -1.77 to 1.42 with a higher score indicating higher cognitive functioning." (NCT00809835)
Timeframe: 12 weeks

Interventionscores on a scale (Mean)
Galantamine and CBT-.12
Galantamine.11
Placebo and CBT-.06
Placebo Only.03

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Cocaine Abstinence

operationalized by percentage of drug-free urine specimens submitted (We will use the Branan ToxCup Drug Screen Cup onsite TESTCUP system for detection of cocaine, methamphetamine, THC, benzodiazepine, and opioids) at 12 Weeks (NCT00809835)
Timeframe: 12 weeks

Interventionpercentage of negative urines (Mean)
Galantamine and CBT22.45
Galantamine31.13
Placebo and CBT20.49
Placebo Only14.78

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Reaction Time for Face Recognition Test at Baseline, Week 8, and Week 24

The face recognition test is a computerized attention test in which ten unfamiliar faces were presented simultaneously on the computer screen for ten seconds to be remembered. After that, a single face was shown and the patient had to press the button one if he/she remembered or, otherwise, button five. It consisted of a random presentation of ten pre-exposed faces and ten new faces as distracters. The reaction time, assessed per patient, was averaged at each time point for each patient e.g., at baseline, Weeks 8 and 24. This test is part of the Computerized Neuropsychological Test Battery. (NCT00814658)
Timeframe: Baseline, Week 8, Week 24

Interventionmilliseconds (Mean)
Galantamine + Nimodipine (Baseline)3124.00
Galantamine + Placebo (Baseline)2684.45
Galantamine + Nimodipine (Week 8)2262.50
Galantamine + Placebo (Week 8)2734.25
Galantamine + Nimodipine (Week 24)2357.80
Galantamine + Placebo (Week 24)3099.38

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Reaction Time for Two-choice Reaction Time Test at Baseline, Week 8, and Week 24

The Two-choice reaction time test is a computerized attention test in which the numbers one or five were presented in the center of the computer screen in a random order. The patient had to press the correspondent button in the response box as quickly as possible. The patient's right finger was put over the button five and the left finger over button one before the test begun. The reaction time, assessed 100 times per patient, was averaged at each time point for each patient e.g., at baseline, Week 8 and Week 24.This test is part of the Computerized Neuropsychological Test Battery (CNTB). (NCT00814658)
Timeframe: Baseline, Week 8, Week 24

Interventionmilliseconds (Mean)
Galantamine + Nimodipine (Baseline)1919.72
Galantamine + Placebo (Baseline)1096.75
Galantamine + Nimodipine (Week 8)852.70
Galantamine + Placebo (Week 8)1187.78
Galantamine + Nimodipine (Week 24)727.60
Galantamine + Placebo (Week 24)1116.25

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Reaction Time for Simple Reaction Time Test at Baseline, Week 8, and Week 24

The Simple Reaction Time is a computerized attention test that evaluates the patient's reaction time. The number one was presented in the center of the computer screen and the patient had to press this number in the response box as quickly as possible. The reaction time, assessed 100 times per patient, was averaged at each time point for each patient e.g., at baseline, Week 8 and Week 24. The patient's finger was put over button one before the test begun. This test is part of the Computerized Neuropsychological Test Battery (CNTB). (NCT00814658)
Timeframe: Baseline, Week 8, Week 24

Interventionmilliseconds (Mean)
Galantamine + Nimodipine (Baseline)1024.06
Galantamine + Placebo (Baseline)729.18
Galantamine + Nimodipine (Week 8)466.60
Galantamine + Placebo (Week 8)671.33
Galantamine + Nimodipine (Week 24)467.60
Galantamine + Placebo (Week 24)584.44

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The Clinical Global Impression (CGI) at Week 4, Week 8, Week 16, and Week 24

The Clinical Global Impression (CGI) is a scale to assess treatment response in patients with mental disorders. The Clinical Global Impression Improvement scale (CGI-I) requires the clinician to rate how much the patient's illness has improved or worsened relative to a baseline state. A patient's illness is compared to change over time and rated as: very much improved, much improved, minimally improved, no change, minimally worse, much worse, or very much worse. (NCT00814658)
Timeframe: Week 4, Week 8, Week 16, Week 24

,,,,,,,
Interventionparticipants (Number)
Very much improvedMuch improvedMinimally improvedNo changeMinimally worseMuch worseVery much worse
Galantamine + Nimodipine (Week 16)0121100
Galantamine + Nimodipine (Week 24)0131000
Galantamine + Nimodipine (Week 4)0114100
Galantamine + Nimodipine (Week 8)0022100
Galantamine + Placebo (Week 16)0035000
Galantamine + Placebo (Week 24)0241100
Galantamine + Placebo (Week 4)0154000
Galantamine + Placebo (Week 8)0162000

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The Neuropsychiatric Inventory (NPI) at Baseline, Week 8, and Week 24

The NPI evaluates 12 neuropsychiatric domains: delusions, hallucinations, dysphoria, anxiety, aggression, euphoria, dis-inhibition, irritability/lability, apathy, aberrant motor activity, eating disorders, and night-time behavior disturbances. For present domains, the severity and frequency of the behavior are determined. Frequency is rated 1 (rarely) to 4 (very often) and Severity is scored 1 (mild) to 3 (severe). The product scores vary from 1 (mild and rarely) to 12 (very often and severe). Total scores vary from 0 (no present domain) to 144 (all domains are present, are often and severe). (NCT00814658)
Timeframe: Baseline, Week 8, Week 24

Interventionscores on a scale (Mean)
Galantamine + Nimodipine (Baseline)24.0
Galantamine + Placebo (Baseline)26.92
Galantamine + Nimodipine (Week 8)20.20
Galantamine + Placebo (Week 8)22.11
Galantamine + Nimodipine (Week 24)15.00
Galantamine + Placebo (Week 24)19.75

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The Quality of Life Assessment for Caregivers of Patients With Alzheimer's Disease (QoL- AD) Total Scores at Baseline, Week 8, Week 24

The Quality of Life assessment scale for caregivers of patients with Alzheimer's disease (QoL-AD) is a 13-item scale with four possible scores for each question (score 1: poor and score 4: excellent). It evaluates the caregivers own perceived quality of life. Total score ranges from 13 to 52. Higher scores represent a better outcome. (NCT00814658)
Timeframe: Baseline, Week 8, Week 24

Interventionscores on a scale (Mean)
Galantamine + Nimodipine (Baseline)34.00
Galantamine + Placebo (Baseline)36.50
Galantamine + Nimodipine (Week 8)32.00
Galantamine + Placebo (Week 8)33.56
Galantamine + Nimodipine (Week 24)36.60
Galantamine + Placebo (Week 24)34.88

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The Quality of Life Assessment for Patients With Alzheimer's Disease (QoL- AD) Total Scores at Baseline, Week 8, Week 24

The Quality of Life assessment scale for patients with Alzheimer's disease (QoL-AD) is a 13-item scale with four possible scores for each question (score 1: poor and score 4: excellent). Total score ranges from 13 to 52. Higher scores represent a better outcome. (NCT00814658)
Timeframe: Baseline, Week 8, Week 24

Interventionscores on a scale (Mean)
Galantamine + Nimodipine (Baseline)33.56
Galantamine + Placebo (Baseline)32.67
Galantamine + Nimodipine (Week 8)35.60
Galantamine + Placebo (Week 8)33.11
Galantamine + Nimodipine (Week 24)36.60
Galantamine + Placebo (Week 24)33.86

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The Quality of Life Assessment for Patients With Alzheimer's Disease (QoL- AD) Total Scores, Based on the Caregiver's Opinion, at Baseline, Week 8, Week 24

The Quality of Life assessment scale for patients with Alzheimer's disease (QoL-AD), according to the opinion of the caregiver is a 13-item scale with four possible scores for each question (score 1: poor and score 4: excellent). It evaluates the opinion of the caregiver about the patient's quality of life. Total score ranges from 13 to 52. Higher scores represent a better outcome. (NCT00814658)
Timeframe: Baseline, Week 8, Week 24

Interventionscores on a scale (Mean)
Galantamine + Nimodipine (Baseline)28.33
Galantamine + Placebo (Baseline)29.33
Galantamine + Nimodipine (Week 8)27.80
Galantamine + Placebo (Week 8)29.78
Galantamine + Nimodipine (Week 24)29.80
Galantamine + Placebo (Week 24)29.13

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The Alzheimer's Disease Assessment Scale - Cognitive Subscale (ADAS-Cog) at Baseline, Week 8, and Week 24

The ADAS-Cog is a psychometric instrument that evaluates memory, attention, reasoning, language, orientation and praxis using an 11-point Assessment Scale. It has a minimum score of 0 and a maximum severity score of 70, and a higher score indicates more impairment. (NCT00814658)
Timeframe: Baseline, Week 8, Week 24

Interventionscores on a scale (Mean)
Galantamine + Nimodipine (Baseline)30.40
Galantamine + Placebo (Baseline)28.20
Galantamine + Nimodipine (Week 8)25.10
Galantamine + Placebo (Week 8)31.03
Galantamine + Nimodipine (Week 24)25.02
Galantamine + Placebo (Week 24)27.70

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Reaction Time for Word Recognition and Learning Test at Baseline, Week 8, and Week 24

The reaction time for word recognition and learning test is a computerized attention test that evaluates the patient's reaction time. This test is similar to the Face Recognition test procedure using Words. The recognition procedure was repeated three times to evaluate a learning effect. The reaction time, assessed per patient, was averaged at each time point for each patient e.g., at baseline, Week 8 and Week 24. This test is part of the Computerized Neuropsychological Test Battery (CNTB). (NCT00814658)
Timeframe: Baseline, Week 8, Week 24

Interventionmilliseconds (Mean)
Galantamine + Nimodipine (Baseline)2022.17
Galantamine + Placebo (Baseline)2978.77
Galantamine + Nimodipine (Week 8)1966.40
Galantamine + Placebo (Week 8)2379.83
Galantamine + Nimodipine (Week 24)1722.00
Galantamine + Placebo (Week 24)3038.81

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Change From Baseline in the Alzheimer's Disease Assessment Scale - Japan Cognitive Subscale (ADAS-J Cog)

ADAS-J cog is the Japanese version of the cognitive function subscale of the Alzheimer's disease assessment scale (ADAS). This scale is used to detect changes in cognitive function in individuals with Alzheimer disease on the basis of three domains: memory, language and behavior. The minimum score is zero (0) and means well cognitive function. The maximum total score is 70 points, and the larger the score, the more severe the degree of impairment. (NCT00814801)
Timeframe: Baseline and 24 weeks

InterventionScores on a scale (Mean)
Placebo Group0.90
Galantamine Group 1-0.58
Galantamine Group 2-1.66

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Change From Baseline in the Behavioral Pathology in Alzheimer's Disease Rating Scale (Behave-AD)

Behave-AD is a CIBIC plus-J subscale that rates the patient's severity of psychotic symptoms. This four-point scale varies from 0 (=none) to 3 (= serious). (NCT00814801)
Timeframe: Baseline and 24 weeks

InterventionScores on a scale (Mean)
Placebo Group0.0
Galantamine Group 1-0.2
Galantamine Group 2-0.3

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Change From Baseline in the Disability Assessment for Dementia (DAD)

Each of the 40 item of the DAD is scored as 1 point= Yes, 0 point= No, or non applicable= N/A. A total score (minimum=0; maximum=40) is the sum of points for each questions converted out 100. Items rated as Not Applicable (N/A) are not considered for the total score. The final score is a percentage that gives an appreciation of global function in activity of daily life (ADL). Higher scores represent less disability in ADL while lower scores indicate more dysfunction. (NCT00814801)
Timeframe: Baseline and 24 weeks

InterventionScores on a scale (Mean)
Placebo Group-2.8
Galantamine Group 1-1.0
Galantamine Group 2-2.2

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Distribution of Clinician's Interview-Based Impression of Change Plus - Japan (CIBIC Plus-J)

"CIBIC plus-J is the Japanese version of the Clinician's Interview-based Impression of Change plus the caregiver's input (CIBIC plus). It is a seven-point categorical assessment scale for evaluating the efficacy of antidementia drugs, ranging from markedly improved to markedly worse." (NCT00814801)
Timeframe: 24 weeks

,,
Interventionpatients (Number)
Markedly improvedModerately improvedMinimally improvedNo changeMinimally worseModerately worseMarkedly worse
Galantamine Group 1012396064160
Galantamine Group 214327361201
Placebo Group07366462220

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Change From Baseline in the Mental Function Impairment Scale (MENFIS)

MENFIS is a Clinician's Interview-Based Impression of Change (CIBIC) plus-Japan subscale that rates the patient's severity for mental function impairment. This seven-point scale varies from 0 (= absolutely no impairment) to 6 (=complete impairment). (NCT00814801)
Timeframe: Baseline and 24 weeks

InterventionScores on a scale (Mean)
Placebo Group2.2
Galantamine Group 11.6
Galantamine Group 21.9

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Arizona Sexual Experience Questionnaire (ASEX) Male

"Mean ASEX total scores by treatment and week for male participants. Total scores are calculated by adding scores for scales #1-#5. Total scores are calculated by adding scores for scales #1-#5. Each scale ranges from 1=Easily/Extremely to 6=Never/None. The minimum total ASEX score is 5 and the maximum score is 30. Lower scores indicate more positive sexual experiences." (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin/Placebo-galantamine16.517.11.5
2: Galantamine/Placebo-oxytocin18.120.21.6
3: Placebo-galantamine /Placebo-oxytocin20.821.70.8

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Barnes Akathisia Scale (BAS) - Global Score

"For each subject, the largest increase from baseline in the global akathisia score at any visit during follow-up was calculated. The global akathisia score ranges from 0=Absent to 5=Severe Akathisia. Higher scores indicate a more severe global rating of akathisia." (NCT01012167)
Timeframe: Treatment Week 0 and Week 6

,,
Interventionpercentage of participants (Number)
No worsening (0)Worsening of 1
1: Oxytocin/Placebo-galantamine93.336.67
2: Galantamine/Placebo-oxytocin1000
3: Placebo-galantamine /Placebo-oxytocin94.125.88

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Blood Oxytocin Levels

Blood Oxytocin Levels by Treatment and Visit (NCT01012167)
Timeframe: Treatment Week 0 and Week 6

,,
Interventionpg/mL (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin/Placebo-galantamine18.2217.22-1.88
2: Galantamine/Placebo-oxytocin13.7610.11-2.99
3: Placebo-galantamine /Placebo-oxytocin14.6913.21-1.73

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Brief Psychiatric Rating Scale (BPRS) - Psychosis Score

"The psychosis score is calculated by adding the scores for scales #4 Conceptual Disorganization, #11 Suspiciousness, #12 Hallucinatory Behavior, and #15 Unusual Thought Content. Each scale ranges from 1=Not Present to 7=Very Severe. The minimum psychosis score is 4 and the maximum psychosis score is 28. A higher score indicates a more severe psychosis rating." (NCT01012167)
Timeframe: Every other week for 6 weeks

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 2Treatment Week 4Treatment Week 6
1: Oxytocin9.349.409.879.67
2: Galantamine7.307.217.006.78
3: Placebo8.187.908.067.59

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Brief Psychiatric Rating Scale (BPRS) - Total Score

"The total BPRS score is calculated by adding the scores for scales #1-#18. Each scale ranges from 1=Not Present to 7=Very Severe. Total scores range from a minimum score of 18 to a maximum score of 126. A higher total score indicates a more severe psychiatric symptom rating." (NCT01012167)
Timeframe: Every other week for 6 weeks

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 2Treatment Week 4Treatment Week 6
1: Oxytocin/Placebo-galantamine34.1634.0034.0734.33
2: Galantamine/Placebo-oxytocin30.3528.9527.8327.67
3: Placebo-galantamine /Placebo-oxytocin32.6531.7531.7232.18

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Calgary Depression Scale (CDS) - Total Score

"Total score calculated by adding scores for scales #1-#9. Each scale ranges from 0=Absent to 3=Severe. The minimum total CDS score is 0 and the maximum total CDS score is 27. A higher score indicates a more severe depression rating." (NCT01012167)
Timeframe: Every other week for 6 weeks

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 2Treatment Week 4Treatment Week 6
1: Oxytocin/Placebo-galantamine2.372.202.131.67
2: Galantamine/Placebo-oxytocin0.841.050.670.50
3: Placebo-galantamine /Placebo-oxytocin1.591.000.941.29

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Electrocardiogram (EKG)

Mean corrected QT interval (QTc) by study week and treatment. (NCT01012167)
Timeframe: Once during Evaluation and once at Treatment Week 6

,,
InterventionQTc (Mean)
Evaluation Week 0Treatment Week 6Change
1: Oxytocin/Placebo-galantamine416.5415.7-2.9
2: Galantamine/Placebo-oxytocin419.0408.1-10.2
3: Placebo-galantamine /Placebo-oxytocin422.6423.80.9

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Laboratory Measures - A/G Ratio

Albumin to Globulin (A/G) ratio in the blood by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventiong/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin1.651.710.04
2: Galantamine1.581.620.05
3: Placebo1.571.600.07

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Laboratory Measures - Albumin

Albumin blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventiong/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin4.394.380.04
2: Galantamine4.274.23-0.03
3: Placebo4.354.370.03

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Laboratory Measures - Alkaline Phosphatase

Alkaline phosphatase blood level by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
InterventionU/L (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin/Placebo-galantamine83.4778.73-4.77
2: Galantamine/Placebo-oxytocin83.4282.500.88
3: Placebo-galantamine /Placebo-oxytocin86.4088.951.19

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Laboratory Measures - ALT/SGPT

Alanine transaminase/serum glutamic-pyruvic transaminase (ALT/SGPT) blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
InterventionU/L (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin/Placebo-galantamine22.8720.67-2.15
2: Galantamine/Placebo-oxytocin31.2628.90-2.65
3: Placebo-galantamine /Placebo-oxytocin27.4027.740.31

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Laboratory Measures - AST/SGOT

Aspartate aminotransferase/serum glutamic oxaloacetic transaminase (AST/SGOT) blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
InterventionU/L (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin/Placebo-galantamine19.8720.27-1.46
2: Galantamine/Placebo-oxytocin22.6821.45-1.53
3: Placebo-galantamine /Placebo-oxytocin22.5023.581.00

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Laboratory Measures - Bilirubin

Bilirubin blood level by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionmg/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin0.450.490.03
2: Galantamine0.350.390.05
3: Placebo0.400.380.03

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Laboratory Measures - BUN

BUN blood level by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionmg/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin12.8012.730.15
2: Galantamine10.7411.551.06
3: Placebo11.9512.00-0.06

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Laboratory Measures - Calcium

Calcium blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionmg/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin9.539.570.12
2: Galantamine9.369.23-0.16
3: Placebo9.589.54-0.03

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Laboratory Measures - Chloride

Chloride blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
InterventionmE/qL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin100.60101.530.62
2: Galantamine102.79102.90-0.06
3: Placebo100.15100.470.56

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Laboratory Measures - Cholesterol

Total cholesterol blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionmg/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin159.18156.931.50
2: Galantamine166.07162.93-2.40
3: Placebo179.60177.33-11.44

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Laboratory Measures - CO2

Carbon Dioxide (CO2) blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
InterventionmE/qL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin23.4723.27-0.31
2: Galantamine22.4222.50-0.06
3: Placebo23.4022.83-0.20

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Laboratory Measures - Globulin

Globulin blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventiong/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin2.722.58-0.15
2: Galantamine2.812.66-0.18
3: Placebo2.822.78-0.09

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Laboratory Measures - Glucose

Glucose blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionmg/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin108.0799.67-9.23
2: Galantamine98.61102.132.00
3: Placebo103.00112.319.77

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Laboratory Measures - HDL

High-density lipoprotein (HDL) blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionmg/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin44.0944.31-0.70
2: Galantamine45.5043.642.11
3: Placebo41.1441.42-1.67

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Laboratory Measures - LDL

Low-density lipoprotein (LDL) blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionmg/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin90.3685.92-0.60
2: Galantamine91.2592.29-1.38
3: Placebo105.79103.73-13.00

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Laboratory Measures - Potassium

Potassium blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
InterventionmE/qL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin4.204.07-0.12
2: Galantamine4.144.01-0.15
3: Placebo4.174.160.00

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Laboratory Measures - Protein

Protein blood level by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventiong/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin7.107.140.07
2: Galantamine7.076.92-0.13
3: Placebo7.177.15-0.04

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Laboratory Measures - Sodium

Sodium blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
InterventionmE/qL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin138.53138.530.15
2: Galantamine139.53139.15-0.53
3: Placebo137.30137.470.31

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Laboratory Measures - Triglycerides

Triglyceride blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionmg/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin124.55124.7914.00
2: Galantamine155.20142.29-39.30
3: Placebo163.47162.171.22

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Laboratory Measures - VLDL

Very low density lipoprotein (VLDL) blood levels by treatment group and visit. (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionmg/dL (Mean)
EvaluationTreatment Week 6Change
1: Oxytocin24.7326.752.80
2: Galantamine22.0023.62-3.13
3: Placebo33.1728.00-0.43

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Mean Z-Scores for Composite Cognitive Primary Outcome* by Treatment Group and Week

* Composite Cognitive Primary Outcome = mean of z-scores from the Brief Assessment of Cognition in Schizophrenia (BACS) Symbol Digit test, the Hopkins Verbal Learning Test (HVLT), and the Rapid Visual Information Processing test (RVIP). Z-scores for each test were calculated as Z = (individual patient score - pooled baseline mean)/(pooled baseline standard deviation). Higher values of the composite score represent a better outcome. (NCT01012167)
Timeframe: Treatment Week 0 and Week 6

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin/Placebo-galantamine0.230.330.1
2: Galantamine/Placebo-oxytocin-0.22-0.050.17
3: Placebo-galantamine /Placebo-oxytocin0.210.180.03

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Neurocognitive Assessment Battery (MCCB) - Attention Vigilance

"MCCB Attention Vigilance domain score by week calculated from the Continuous Performance Test, Identical Pairs version. The domain score scale is 20-80, with higher scores indicating a better outcome.~." (NCT01012167)
Timeframe: Once at Treatment Week 0 (baseline) and again at Treatment Week 6 (end of treatment).

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin36.939.52.6
2: Galantamine33.534.51.1
3: Placebo37.235.1-2.1

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Neurocognitive Assessment Battery (MCCB) - Composite Score

MCCB Composite Score by Week ranging from -10-100 with a higher score indicating a better outcome. (NCT01012167)
Timeframe: Once at Treatment Week 0 (baseline) and again at Treatment Week 6 (end of treatment).

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin/Placebo-galantamine25.928.22.3
2: Galantamine/Placebo-oxytocin24.526.21.7
3: Placebo-galantamine /Placebo-oxytocin28.228.90.7

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Neurocognitive Assessment Battery (MCCB) - Processing Speed

MCCB Processing Speed domain score by week calculated from the Trail Making Test- Part A, Brief Assessment of Cognition in Schizophrenia- symbol coding subtest, and the Category fluency test- animal naming. The domain score scale is 20-80, with higher scores indicating a better outcome. (NCT01012167)
Timeframe: Once at Treatment Week 0 (baseline) and again at Treatment Week 6 (end of treatment).

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin33.534.20.7
2: Galantamine31.935.43.5
3: Placebo34.035.61.6

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Neurocognitive Assessment Battery (MCCB) - Reasoning/Problem Solving

MCCB Reasoning/Problem Solving domain score by week calculated from the Neuropsychological Assessment Battery- mazes subtest. The domain score scale is 20-80, with higher scores indicating a better outcome. (NCT01012167)
Timeframe: Once at Treatment Week 0 (baseline) and again at Treatment Week 6 (end of treatment).

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin39.740.71.0
2: Galantamine39.342.93.7
3: Placebo41.441.70.3

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Neurocognitive Assessment Battery (MCCB) - Social Cognition

MCCB Social Cognition domain score by week calculated from the Mayer-Salovey-Caruso Emotional Intelligence Test- managing emotions branch. The domain score scale is 20-80, with higher scores indicating a better outcome. (NCT01012167)
Timeframe: Once at Treatment Week 0 (baseline) and again at Treatment Week 6 (end of treatment).

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin31.732.50.8
2: Galantamine32.829.6-3.2
3: Placebo30.432.82.4

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Neurocognitive Assessment Battery (MCCB) - Verbal Learning

MCCB Verbal Learning domain score by week calculated from the Hopkins Verbal Learning Test-Revised, immediate recall (three learning trials only). The domain score scale is 20-80, with higher scores indicating a better outcome. (NCT01012167)
Timeframe: Once at Treatment Week 0 (baseline) and again at Treatment Week 6 (end of treatment).

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin36.338.72.5
2: Galantamine33.435.82.4
3: Placebo36.536.4-0.1

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Neurocognitive Assessment Battery (MCCB) - Visual Learning

MCCB Visual Learning domain score by week calculated from the Brief Visuospatial Memory Test-Revised. The domain score scale is 20-80, with higher scores indicating a better outcome. (NCT01012167)
Timeframe: Once at Treatment Week 0 (baseline) and again at Treatment Week 6 (end of treatment).

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin33.836.22.4
2: Galantamine37.233.7-3.4
3: Placebo35.134.2-0.9

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Neurocognitive Assessment Battery (MCCB) - Working Memory

MCCB Working Memory domain score by week calculated from the Wechsler Memory Scale, 3rd ed., spatial span subtest. The domain score scale is 20-80, with higher scores indicating a better outcome. (NCT01012167)
Timeframe: Once at Treatment Week 0 (baseline) and again at Treatment Week 6 (end of treatment).

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin34.734.80.1
2: Galantamine33.734.70.9
3: Placebo35.338.12.8

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Positive and Negative Affect Schedule (PANAS) - Negative

"Participant reported responses after Brief Role Play rating how they felt during the role plays. Participants rated 12 negative affect items on a scale of 1-5, with 1 being very slightly or not at all and 5 being extremely. The minimum score for this measure is 12 and the maximum score is 60. Higher scores indicate a higher rate of negative affect during the role plays." (NCT01012167)
Timeframe: Treatment Week 0 and Week 6

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change from Week 0 at Week 6
1: Oxytocin20.518.8-1.7
2: Galantamine18.218.0-0.2
3: Placebo20.218.9-1.3

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Positive and Negative Affect Schedule (PANAS) - Positive

"Participant reported responses after Brief Role Play rating how they felt during the role plays. Participants rated 12 positive affect items on a scale of 1-5, with 1 being very slightly or not at all and 5 being extremely. The minimum score for this measure is 12 and the maximum score is 60. Higher scores indicate a higher rate of positive affect during the role plays." (NCT01012167)
Timeframe: Treatment Week 0 and Week 6

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change from Week 0 at Week 6
1: Oxytocin38.138.50.4
2: Galantamine37.039.52.5
3: Placebo42.540.8-1.6

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Reactions to Partner

"Participant reported responses after Brief Role Play. The Reactions to Partner item was calculated by totaling responses to 7 scales. Each scale score ranges from 1-5, which 1 being completely agree and 5 being completely disagree. The minimum score for this measure is 7 and the maximum score is 35. Higher responses indicate a more negative reaction to their role play partner." (NCT01012167)
Timeframe: Treatment Week 0 and Week 6

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change from Week 0 at Week 6
1: Oxytocin13.713.70.0
2: Galantamine14.413.9-0.4
3: Placebo12.512.50.0

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Scale for the Assessment of Negative Symptoms (SANS) - Alogia

Mean score by treatment and week. Scores range from 0-5, with higher scores indicating a worse outcome. (NCT01012167)
Timeframe: Every other week for 6 weeks

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 2Treatment Week 4Treatment Week 6Change from Week 0 at Week 2Change from Week 0 at Week 4Change from Week 0 at Week 6
1: Oxytocin/Placebo-galantamine0.600.440.560.56-0.16-0.04-0.04
2: Galantamine/Placebo-oxytocin0.950.890.850.78-0.05-0.03-0.10
3: Placebo-galantamine /Placebo-oxytocin0.990.890.800.69-0.10-0.17-0.19

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Scale for the Assessment of Negative Symptoms (SANS) - Anhedonia

Mean score by treatment and week. Scores range from 0-5, with higher scores indicating a worse outcome. (NCT01012167)
Timeframe: Every other week for 6 weeks

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 2Treatment Week 4Treatment Week 6Change from Week 0 at Week 2Change from Week 0 at Week 4Change from Week 0 at Week 6
1: Oxytocin/Placebo-galantamine2.422.422.272.330.00-0.15-0.09
2: Galantamine/Placebo-oxytocin2.602.592.462.43-0.01-0.11-0.14
3: Placebo-galantamine /Placebo-oxytocin2.662.582.602.66-0.080.010.12

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Scale for the Assessment of Negative Symptoms (SANS) - Avolition

Mean score by treatment and week. Scores range from 0-5, with higher scores indicating a worse outcome. (NCT01012167)
Timeframe: Every other week for 6 weeks

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 2Treatment Week 4Treatment Week 6Change from Week 0 at Week 2Change from Week 0 at Week 4Change from Week 0 at Week 6
1: Oxytocin/Placebo-galantamine2.942.782.852.88-0.15-0.09-0.05
2: Galantamine/Placebo-oxytocin2.912.732.742.74-0.18-0.16-0.16
3: Placebo-galantamine /Placebo-oxytocin2.442.432.442.41-0.010.040.05

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Scale for the Assessment of Negative Symptoms (SANS) - Blunted Affect

Mean score by treatment and week. Scores range from 0-5, with higher scores indicating a worse outcome. (NCT01012167)
Timeframe: Every other week for 6 weeks

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 2Treatment Week 4Treatment Week 6Change from Week 0 at Week 2Change from Week 0 at Week 4Change from Week 0 at Week 6
1: Oxytocin/Placebo-galantamine1.671.321.521.48-0.35-0.15-0.19
2: Galantamine/Placebo-oxytocin1.961.891.791.70-0.07-0.09-0.17
3: Placebo-galantamine /Placebo-oxytocin2.212.051.941.85-0.16-0.19-0.19

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Scale for the Assessment of Negative Symptoms (SANS) Total Score

Mean SANS Total Score by Treatment and Week. SANS total score range = 0-85. Higher scores indicate more severe negative symptoms. (NCT01012167)
Timeframe: Every other week for 6 weeks

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 2Treatment Week 4Treatment Week 6Change from Week 0 at Week 2Change from Week 0 at Week 4Change from Week 0 at Week 6
1: Oxytocin/Placebo-galantamine33.2330.0731.2731.40-3.17-1.97-1.83
2: Galantamine/Placebo-oxytocin36.6335.2234.0633.22-1.41-1.69-2.53
3: Placebo-galantamine /Placebo-oxytocin36.6335.0534.2233.47-1.58-1.47-1.00

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Simpson-Angus Scale (SAS)

"SAS total score for extrapyramidal side effects: Frequencies of greatest within-participant increase (worsening) from pre-treatment baseline, by treatment group. Total scores calculated by adding scores from scales #1-#11. Each scale ranges from 0=None/Normal to 4=Extreme/Severe. The minimum total score is 0 and the maximum score is 44. Higher scores indicate a more severe extrapyramidal side effect rating." (NCT01012167)
Timeframe: Baseline, week 3, and week 6

,,
Interventionpercentage of participants (Number)
No worsening (0)Worsening of 1Worsening of 2Worsening of 3Worsening of 4Worsening of 10
1: Oxytocin/Placebo-galantamine8016.676.676.6700
2: Galantamine/Placebo-oxytocin63.1610.5315.795.265.260
3: Placebo-galantamine /Placebo-oxytocin78.9510.5305.2605.26

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Vital Signs - Diastolic Blood Pressure

Mean diastolic blood pressure by treatment and follow-up week (NCT01012167)
Timeframe: Weekly for 6 weeks

,,
Interventionmm-Hg (Mean)
Treatment Week 0Treatment Week 1Treatment Week 2Treatment Week 3Treatment Week 4Treatment Week 5Treatment Week 6
1: Oxytocin/Placebo-galantamine78.878.476.775.073.976.274.4
2: Galantamine/Placebo-oxytocin76.676.277.579.175.179.280.7
3: Placebo-galantamine /Placebo-oxytocin78.375.579.778.973.777.276.0

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Vital Signs - Pulse

Mean sitting pulse (bpm) by treatment and follow-up week (NCT01012167)
Timeframe: Weekly for 6 weeks

,,
Interventionbpm (Mean)
Treatment Week 0Treatment Week 1Treatment Week 2Treatment Week 3Treatment Week 4Treatment Week 5Treatment Week 6
1: Oxytocin/Placebo-galantamine81.286.282.776.579.678.476.1
2: Galantamine/Placebo-oxytocin86.091.691.389.288.698.685.2
3: Placebo-galantamine /Placebo-oxytocin85.289.387.389.283.790.584.7

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Vital Signs - Systolic Blood Pressure

Mean systolic blood pressure by treatment and follow-up week (NCT01012167)
Timeframe: Weekly for 6 weeks

,,
Interventionmm-Hg (Mean)
Treatment Week 0Treatment Week 1Treatment Week 2Treatment Week 3Treatment Week 4Treatment Week 5Treatment Week 6
1: Oxytocin/Placebo-galantamine128.4126.1121.9129.5124.8128.4124.0
2: Galantamine/Placebo-oxytocin123.4123.9123.7127.3123.8126.9129.6
3: Placebo-galantamine /Placebo-oxytocin132.3127.4136.2137.7129.9132.8134.5

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Willingness to Interact

"Participant reported responses after Brief Role Play. The Willingness to Interact item calculated by totaling scores from items 1-6. Each score ranges from 1-5, with 1 being definitely willing and 5 being definitely unwilling. The minimum score for this measure is 6 and the maximum score is 30. Lower scores indicate more willingness to interact with their role play partner again in the future." (NCT01012167)
Timeframe: Treatment Week 0 and Week 6

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change from Week 0 at Week 6
1: Oxytocin23.6724.470.80
2: Galantamine23.1824.241.06
3: Placebo24.4125.000.59

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Vital Signs - Weight

Mean weight (kg) by treatment and follow-up week (NCT01012167)
Timeframe: Weekly for 6 weeks

,,
Interventionkg (Mean)
Treatment Week 0Treatment Week 1Treatment Week 2Treatment Week 3Treatment Week 4Treatment Week 5Treatment Week 6
1: Oxytocin/Placebo-galantamine96.597.898.098.0100.098.197.6
2: Galantamine/Placebo-oxytocin96.297.597.594.595.594.095.1
3: Placebo-galantamine /Placebo-oxytocin96.497.998.398.4100.3100.897.9

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Side Effect Checklist (SEC) - Abdominal Pain

"Percentage of participants with new onset or worsening compared to baseline of Abdominal Pain rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin12.5
2: Galantamine5.0
3: Placebo10.0

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Side Effect Checklist (SEC) - Anorexia

"Percentage of participants with new onset or worsening compared to baseline of Anorexia rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine10.0
3: Placebo15.0

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Side Effect Checklist (SEC) - Bruising Easily

"Percentage of participants with new onset or worsening compared to baseline of Bruising Easily rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin0.0
2: Galantamine10.0
3: Placebo0.0

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Side Effect Checklist (SEC) - Constipation

"Percentage of participants with new onset or worsening compared to baseline of Constipation rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin0.0
2: Galantamine0.0
3: Placebo0.0

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Side Effect Checklist (SEC) - Diarrhea

"Percentage of participants with new onset or worsening compared to baseline of Diarrhea rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine30.0
3: Placebo5.0

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Side Effect Checklist (SEC) - Dizziness

"Percentage of participants with new onset or worsening compared to baseline of Dizziness rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine30.0
3: Placebo5.0

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Side Effect Checklist (SEC) - Dry Eye

"Percentage of participants with new onset or worsening compared to baseline of Dry Eye rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin6.7
2: Galantamine0.0
3: Placebo5.9

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Side Effect Checklist (SEC) - Dry Mouth

"Percentage of participants with new onset or worsening compared to baseline of Dry Mouth rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine5.0
3: Placebo10.0

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Side Effect Checklist (SEC) - Enuresis

"Percentage of participants with new onset or worsening compared to baseline of Enuresis rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin25.0
2: Galantamine5.0
3: Placebo0.0

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Side Effect Checklist (SEC) - Excessive Tearing of the Eye

"Percentage of participants with new onset or worsening compared to baseline of Excessive Tearing of the Eye rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin6.7
2: Galantamine5.6
3: Placebo5.9

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Side Effect Checklist (SEC) - Fever

"Percentage of participants with new onset or worsening compared to baseline of Fever rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin0.0
2: Galantamine5.0
3: Placebo0.0

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Side Effect Checklist (SEC) - Headache

"Percentage of participants with new onset or worsening compared to baseline of Headache rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin12.5
2: Galantamine25.0
3: Placebo15.0

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Side Effect Checklist (SEC) - Hyperhydrosis

"Percentage of participants with new onset or worsening compared to baseline of Hyperhydrosis rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin0.0
2: Galantamine0.0
3: Placebo0.0

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Side Effect Checklist (SEC) - Hypersalivation

"Percentage of participants with new onset or worsening compared to baseline of Hypersalivation rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine15.0
3: Placebo25.0

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Side Effect Checklist (SEC) - Insomnia

"Percentage of participants with new onset or worsening compared to baseline of Insomnia rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine10.0
3: Placebo5.0

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Side Effect Checklist (SEC) - Malaise

"Percentage of participants with new onset or worsening compared to baseline of Malaise rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine0.0
3: Placebo10.0

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Side Effect Checklist (SEC) - Mucosal Ulceration

"Percentage of participants with new onset or worsening compared to baseline of Mucosal Ulceration rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin6.3
2: Galantamine5.0
3: Placebo0.0

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Side Effect Checklist (SEC) - Nasal Irritation

"Percentage of participants with new onset or worsening compared to baseline of Nasal Irritation rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin33.3
2: Galantamine16.7
3: Placebo23.5

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Side Effect Checklist (SEC) - Nausea

"Percentage of participants with new onset or worsening compared to baseline of Nausea rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine15.0
3: Placebo5.0

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Side Effect Checklist (SEC) - Rash

"Percentage of participants with new onset or worsening compared to baseline of Rash rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin12.5
2: Galantamine10.0
3: Placebo10.0

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Side Effect Checklist (SEC) - Restlessness

"Percentage of participants with new onset or worsening compared to baseline of Restlessness rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine10.0
3: Placebo15.0

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Side Effect Checklist (SEC) - Sedation

"Percentage of participants with new onset or worsening compared to baseline of Sedation rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin12.5
2: Galantamine15.0
3: Placebo10.0

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Side Effect Checklist (SEC) - Sore Throat

"Percentage of participants with new onset or worsening compared to baseline of Sore Throat rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin6.3
2: Galantamine10.0
3: Placebo5.0

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Side Effect Checklist (SEC) - Stiffness

"Percentage of participants with new onset or worsening compared to baseline of Stiffness rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin6.3
2: Galantamine10.0
3: Placebo10.0

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Side Effect Checklist (SEC) - Tinnitus

"Percentage of participants with new onset or worsening compared to baseline of Tinnitus rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin0.0
2: Galantamine0.0
3: Placebo10.5

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Side Effect Checklist (SEC) - Tremor

"Percentage of participants with new onset or worsening compared to baseline of Tremor rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin6.3
2: Galantamine15.0
3: Placebo10.0

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Side Effect Checklist (SEC) - Urticaria

"Percentage of participants with new onset or worsening compared to baseline of Urticaria rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine15.0
3: Placebo15.0

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Side Effect Checklist (SEC) - Uterine Contractions

"Percentage of participants with new onset or worsening compared to baseline of Uterine Contractions rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin0.0
2: Galantamine0.0
3: Placebo0.0

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Side Effect Checklist (SEC) - Vomiting

"Percentage of participants with new onset or worsening compared to baseline of Vomiting rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin12.5
2: Galantamine5.0
3: Placebo10.0

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Side Effect Checklist (SEC) - Weight Loss

"Percentage of participants with new onset or worsening compared to baseline of Weight Loss rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin18.8
2: Galantamine5.0
3: Placebo25.0

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Side Effect Checklist (SEC) - Wheezing

"Percentage of participants with new onset or worsening compared to baseline of Wheezing rating on the SEC, by Treatment Group." (NCT01012167)
Timeframe: Weekly for 6 weeks

Interventionpercentage of participants (Number)
1: Oxytocin13.3
2: Galantamine5.6
3: Placebo11.8

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Abnormal Involuntary Movement Scale (AIMS)

"AIMS Total Score: Frequencies of Maximum Within- Participant Increases (worsening) from Baseline by Treatment Group. Total score calculated by adding scores from scales #1-#10. Each scale ranges from 0=None to 4=Severe. The minimum total AIMS score is 0 and the maximum score is 40. Higher scores indicate a more severe abnormal involuntary movement rating." (NCT01012167)
Timeframe: Treatment Week 0 and Week 6

,,
Interventionpercentage of participants (Number)
No worsening (0)Worsening of 1Worsening of 2Worsening of 3Worsening of 5
1: Oxytocin/Placebo-galantamine86.676.676.6700
2: Galantamine/Placebo-oxytocin77.7816.67005.56
3: Placebo-galantamine /Placebo-oxytocin76.4717.6505.880

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Arizona Sexual Experience Questionnaire (ASEX) Female

"Mean ASEX total scores by treatment and week for female participants. Total scores are calculated by adding scores for scales #1-#5. Each scale ranges from 1=Easily/Extremely to 6=Never/None. The minimum total ASEX score is 5 and the maximum score is 30. Lower scores indicate more positive sexual experiences." (NCT01012167)
Timeframe: Once during evaluation and once at the end of 6 weeks of study treatment

,,
Interventionunits on a scale (Mean)
Treatment Week 0Treatment Week 6Change
1: Oxytocin/Placebo-galantamine10.513.53.0
2: Galantamine/Placebo-oxytocin21.219.2-2.0
3: Placebo-galantamine /Placebo-oxytocin29.030.00.0

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Change From Baseline in Choice Reaction Time

The Choice Reaction Time is a computerized attention test that evaluates the reaction time and the number of errors by showing patients one card on the computer screen and making them find the same one among similar four cards. The test is performed a total of 12 times. (NCT01054976)
Timeframe: Baseline, Week 12

Interventionseconds (Mean)
Week 4 (n=80)Week 12 (n=73)
Galantamine429.541331

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Change From Baseline in Alzheimer's Disease Assessment Scale - Cognitive Subscale (ADAS-Cog)

The Alzheimer's disease Assessment Scale-Cognitive subscale (ADAS-Cog) is an instrument used to assess cognitive dysfunction in individuals with Alzheimer disease and other dementias. It consists of 11 items, with scores ranging from 1 to 70. Maximum score is 70. Higher scores indicate worsening. (NCT01054976)
Timeframe: Baseline, Week 12

Interventionscores on a scale (Mean)
Galantamine1.31

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Change From Baseline in Korean Version of Disability Assessment for Demential Scale (DAD-K)

"DAD-K is the Korean version of the Assessment for Dementia Scale, a tool developed to evaluate the Alzheimer patients' function including both basic and instrumental Activities of Daily Livings (ADL). It evaluates one function from various perspectives including behavior initiation, plan and preparation, and valid performance. It consists of 10 questions, each can score either 0 (no) or 1 (yes), if not applicable, patient will check on not applicable (x) which will not count in the calculation. Scores range from 0 to 100. Higher score represents better function" (NCT01054976)
Timeframe: Baseline, Week 12

Interventionscores on a scale (Mean)
Galantamine-1.41

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Change From Baseline in Seoul-Instrumental Activities of Daily Livings (S-IADL)

The Seoul-Instrumental Activities of Daily Living (S-IADL) assesses patients' abilities to perform instrumental and social activities of daily living. These include the ability to prepare a balanced meal, remember appointments, keep financial records, remember to take medication, and so on. It is composed of 15 items, with scores ranging from 0 to 45. Lower scores indicate better functioning. (NCT01054976)
Timeframe: Baseline, Week 12

Interventionscores on a scale (Mean)
Galantamine1.22

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Change From Baseline in Simple Reaction Time

The Simple Reaction Time is a computerized attention test that evaluates the patient's reaction time when the color of the computer screen changes from black to white by performing a total of 70 times for six minutes. (NCT01054976)
Timeframe: Baseline, Week 12

Interventionseconds (Mean)
Week 4 (n=83)Week 12 (n=73)
Galantamine-30.92180.83

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Trust Game (Dollar Amount Earned)

Participants compete in a social trust game in which they are paired with a partner (the computer program). Over the course of 24 rounds he participant can offer up to $10 to their partner. The partner can either accept the offer, in which case the total amount offered is split equally between the participant and their partner (i.e. $10 is split into $5 each). Or the partner can reject the offer and receive a portion of the toal offer for themselves and give the participant nothing ($0). The total amount of money that can be offered ranges from $0-240. (NCT01100775)
Timeframe: 20 minutes (total duration of the trust game cognitive test)

InterventionDollars (Mean)
Galantamine147.7
Placebo131.4

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Facial Affect Recognition Score (Number of Responses)

This computer administered test includes 40 color photogralhs of four emotions (happy, sad, angry, and fearful) balanced for the posers gender, age and ethnicity, including four low intensity and four high intensity facila expressions of each emotion, plus 8 neutral faces. The stimuli are presented in random order and subjects are asked to identify which stimuli were presented to them at the end. Performance on this test correlates with negative symptom severity (NCT01100775)
Timeframe: 10 minutes (time usually needed to complete this test)

,
InterventionNumber of Responses (Mean)
Facial Affect TotalFacial Affect HitsFacial Affect False Alarms
Galantamine31.212.35.1
Placebo3314.385.38

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The Brief Smell Identification Test (B-SIT) Score (Number of Correct Responses)

The Brief Smell Identification Test (B-SIT) is a 5-minute, 12-item screening test. Participants try to identify 12 different odors with four multiple choice options given for each odor. (NCT01100775)
Timeframe: 5 minutes (duration usually needed to complete this test)

InterventionNumber of correct responses (Mean)
Galantamine10.2
Placebo10.222

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RVIP Target Hit and False Alarm (Number of Responses)

Rapid Visual Information Processing (RVIP) measures primarily sustained attention but perhaps also working memory. The task was continuous stimuli presentation of a stream of single digits (from 1 to 9) presented in the center of the computer monitor at a rate of 1/600milliseconds; the subjects respond when the they see a target sequence of 3 odds or 3 evens in consecutive sequence. Two target sequences are separated by a minimum and maximum of 30 non-target digits. (NCT01100775)
Timeframe: 25 minutes (duration needed to complete this test)

,
InterventionNumber of responses (Mean)
RVIP Practice Mean Target HitsRVIP Practice Mean False AlarmsRVIP First Half Mean Target HitsRVIP First Half Mean False Alarms
Galantamine23.419.725.420.7
Placebo22.814.8819.7518.88

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Hopkins Verbal Learning Test (HVLT) Score

HVLT comes in 6 different forms. Forms 4 and 5 were used for this study with one form administered on the first day and the other on the second and were counterbalanced between subjects. Each form contains 12 nouns, four words each from one of three semantic categories, to be learned over the course of three learning trials. (NCT01100775)
Timeframe: 15 minutes (duration needed to complete this test)

,
InterventionNumber of correct responses (Mean)
HVLT Trial 1HVLT Trial 2HVLT Trial 3
Galantamine7.79.710.8
Placebo7.2210.2210.78

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RVIP Reaction Times (ms)

Rapid Visual Information Processing (RVIP) measures primarily sustained attention but perhaps also working memory. The task was continuous stimuli presentation of a stream of single digits (from 1 to 9) presented in the center of the computer monitor at a rate of 1/600milliseconds; the subjects respond when the they see a target sequence of 3 odds or 3 evens in consecutive sequence. Two target sequences are separated by a minimum and maximum of 30 non-target digits. (NCT01100775)
Timeframe: 25 minutes (total duration to test RVIP)

,
Interventionmilliseconds (Mean)
RVIP Practice Mean Target Reaction TimeRVIP Practice Mean False Alarm Reaction TimeRVIP First Half Mean Target Reaction TimeRVIP First Half Mean False Alarm Reaction Time
Galantamine534.2290.5525.1215
Placebo581.5380.5544260

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Reading the Mind in the Eyes Score (Number of Correct Responses)

A 30 item task presents a picture of a person's eyes and the participant is asked to determine the person's mental state from 4 multiple choice options. (NCT01100775)
Timeframe: 10 minutes (duration needed to complete the test)

InterventionNumber of correct responses (Mean)
Galantamine24.9
Placebo24.12

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Brief Assessment of Cognition for Schizophrenia (BACS) Score

The BACS Symbol Coding subtest will be used to assess processing speed, and the demographically corrected T score, will be used for data analysis. This test requires less than 5 minutes to administer adn provides a highly reliable measure of processing speed. There are nine symbols coded 1 through 9. Participants are given 90 seconds to match a series of these symbols with their corresponding number. The total correct matches in the participants score. Scores range from 0-110. (NCT01100775)
Timeframe: 5 minutes (duration needed to complete the assessment)

InterventionNumber of correct responses (Mean)
Galantamine49
Placebo52

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Social Affiliation Measured by Social Affiliative Role Play (Rating Scale Score)

In a videotaped session, research staff engages the participant in social interaction based on a role play. The tape is rated on social skills and on Positive and Negative Affect Scale. participants are rated on a 5 point likert scale ranging from very poor (1) to very good (5) (NCT01100775)
Timeframe: 30 minutes (time needed to complete this test)

,
Interventionunits on a scale (Mean)
Overall AffectOverall Social Skill
Galantamine3.9584.15
Placebo3.83.8

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Discontinuation Rates

We are not seeking to establish efficacy of these three medications for the indication of Alzheimer's disease. Each of these medications already has FDA-approval for Alzheimer's. The primary outcome measure is the discontinuation rate among the three medications. Based on previous systematic reviews, these rates are reportedly in the range of 30% by 12 weeks compared with placebo. We will determine the approximate date of discontinuation by self-reports from the caregiver through the telephone-based interview at 6, 12, and 18 weeks. (NCT01362686)
Timeframe: 6, 12, and 18 week interviews from enrollment

Interventionparticipants (Number)
Donepezil26
Galantamine35
Rivastigmine37

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Healthy Aging Brain Care (HABC)-Monitor

The current HABC-Monitor includes 30 items covering four clinically relevant domains of dementia, ie, cognitive, functional, behavioral, and psychological symptoms, and caregiver quality of life. For brevity and practical use in the clinical setting, each item on the four scales was designed to have the same item response options consisting of four categories that use the frequency of the target problem in the past 2 weeks. The HABC- Monitor took approximately 6 minutes to complete. The scores of the four scales are summed to create the total scores which were used in this analysis.The higher the total score, the higher the level of self reported caregiver burden. The minimum score is 0 and the maximum score is 90. (NCT01362686)
Timeframe: baseline, 6, 12, and 18 week interviews

,,
Interventionunits on a scale (Mean)
Baseline HABC6 Week HABC12 Week HABC18 Week HABC
Donepezil18.7618.6116.0416.90
Galantamine18.3419.1618.0019.92
Rivastigmine16.6116.4313.6315.80

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Neuropsychiatric Inventory (NPI)

The NPI is based on a structured interview administered to an informal caregiver and has been adopted by the Alzheimer's Disease Cooperative Studies Group to obtain information on the presence of psychopathology in behavioral areas including delusions, apathy, hallucinations, disinhibition, agitation, depression, aberrant motor behavior, anxiety, night-time behavior, and euphoria.9 For each of 12 symptoms, if the caregiver reports the presence of psychopathology, a frequency and severity score are multiplied to yield a possible item score range of 0-12, and a possible total score range of 0-144. The NPI can be used to assess changes in the patient's behavior over the past month. The NPI also assesses the level of caregiver distress attributable to each of the 12 patient behaviors, with a possible total caregiver distress score range of 0-60. Higher scores indicate higher severity of psychopathology and caregiver disress. The NPI has excellent reliability and validity. (NCT01362686)
Timeframe: Baseline, 6, 12, 18 week interviews from enrollment

,,
Interventionunits on a scale (Mean)
6 WeekNPI Patient6 Week NPI Caregiver12 Week NPI Patient12 Week NPI Caregiver18 Week NPI Patient18 Week NPI Caregiver
Donepezil12.715.949.625.669.065.56
Galantamine9.424.408.404.3310.676.22
Rivastigmine8.633.915.242.227.262.89

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Heart Rate

Pulse (NCT01531153)
Timeframe: once a day for up to two days over 12 Weeks

,,
Interventionbeats per minute (bpm) (Mean)
Week 1Week 2Week 3Week 4Week 5Week 6Week 7Week 8Week 9Week 10Week 11Week 12
Galantamine 16mg77.7679.7480.4277.8378.8275.5580.5077.4681.3181.2880.5176.33
Galantamine 8mg78.8580.2478.6882.3580.9180.4478.6582.7380.5980.0382.9081.07
Placebo75.0177.1374.9874.8476.7275.8076.4878.5678.0980.0280.0277.38

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Stroop- RT Correct Neutral

Drug Stroop Task is a computerized task which presents words either cocaine-related ('drug') words or non-drug-related ('neutral') words written in colored font. The subject is asked to press a button to indicate the color of the font as quickly and accurately as possible. The task is thought to measure attentional bias to drug-related stimuli. RT Correct Neutral is the mean response time to neutral trials where the subject pressed the correct color response. (NCT01531153)
Timeframe: weeks 0, 4, 8, 12, 16, 24, 36

,,
Interventionmilliseconds (Mean)
BaselineWeek 4Week 8Week 12Week 16Week 24Week 36
Galantamine 16mg805.24813.66741.33756.00802.90769.47747.65
Galantamine 8mg785.18821.37817.69764.53849.17814.09824.54
Placebo871.07845.66830.22816.47895.03876.61989.42

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Digit Span- LDSF

Digit Span Task description: Orally administered (not computerized) task where subjects are read-aloud lists of digits and asked to repeat them in the same order they heard them (Forward condition). Subjects are given a pair of lists for each digit length - and given a point for each list they get entirely correct. If they get at least one out of the two correct for that length, then the researcher gives them another one of a longer length (one digit longer). If they get both wrong at a given length- that task is ended. The task is then repeated with different digit lists to recall, but they are asked to repeat them or in the reverse order that they heard them (Backward condition). Longest Digit Span Forward (LDSF) is the longest digit span a participant gets correct, in the forward condition. Higher scores are better (Scale of 0 to 9). (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionunits on a scale (Mean)
Baseline12 Weeks
Galantamine 16mg5.76.8
Galantamine 8mg5.96.5
Placebo6.47.4

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Digit Span- LDSB

Digit Span Task description: Orally administered (not computerized) task where subjects are read-aloud lists of digits and asked to repeat them in the same order they heard them (Forward condition). Subjects are given a pair of lists for each digit length - and given a point for each list they get entirely correct. If they get at least one out of the two correct for that length, then the researcher gives them another one of a longer length (one digit longer). If they get both wrong at a given length- that task is ended. The task is then repeated with different digit lists to recall, but they are asked to repeat them or in the reverse order that they heard them (Backward condition). Longest Digit Span Backward (LDSB) is the longest digit span participants got correct, in the backward condition. Higher scores are better (Scale of 0 to 8). (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionunits on a scale (Mean)
Baseline12 Weeks
Galantamine 16mg3.24.3
Galantamine 8mg4.24.2
Placebo4.03.9

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Digit Span- DSF

Digit Span Task description: Orally administered (not computerized) task where subjects are read-aloud lists of digits and asked to repeat them in the same order they heard them (Forward condition). Subjects are given a pair of lists for each digit length - and given a point for each list they get entirely correct. If they get at least one out of the two correct for that length, then the researcher gives them another one of a longer length (one digit longer). If they get both wrong at a given length- that task is ended. The task is then repeated with different digit lists to recall, but they are asked to repeat them or in the reverse order that they heard them (Backward condition). Digit Span Forward (DSF) is the number of digit span trials participants got correct in the forward condition. Higher scores are better (Scale of 0 to 14). (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionunits on a scale (Mean)
Baseline12 Weeks
Galantamine 16mg9.910.7
Galantamine 8mg9.310.5
Placebo10.711.2

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Digit Span- DSB

Digit Span Task description: Orally administered (not computerized) task where subjects are read-aloud lists of digits and asked to repeat them in the same order they heard them (Forward condition). Subjects are given a pair of lists for each digit length - and given a point for each list they get entirely correct. If they get at least one out of the two correct for that length, then the researcher gives them another one of a longer length (one digit longer). If they get both wrong at a given length- that task is ended. The task is then repeated with different digit lists to recall, but they are asked to repeat them or in the reverse order that they heard them (Backward condition). Digit Span Forward (DSB) is the number of digit span trials participants got correct in the backward condition. Higher scores are better (Scale of 0 to 14). (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionunits on a scale (Mean)
Baseline12 Weeks
Galantamine 16mg7.28.5
Galantamine 8mg8.38.3
Placebo7.67.3

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CANTAB SST- SD Correct

This is the CANTAB SST measure which evaluates response inhibition. Stop Signal Reaction Time (SSRT): The estimate of the length of time between the go stimulus and the stop stimulus at which the subject is able to successfully inhibit their response on 50% of the trials. Range of scores from 0 to 1500 (unit=milliseconds) and lower scores are 'better'. SD Correct is the standard deviation of response times across 'go' trials where the subject has responded on the correct button (right or left). (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionmilliseconds (Mean)
Baseline12 Weeks
Galantamine 16mg302.3410.6
Galantamine 8mg276.5337.8
Placebo363.4492.6

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CANTAB SST- SSRT

This is the CANTAB SST measure which evaluates response inhibition. Stop Signal Reaction Time (SSRT): The estimate of the length of time between the go stimulus and the stop stimulus at which the subject is able to successfully inhibit their response on 50% of the trials. Range of scores from 0 to 1500 (unit=milliseconds) and lower scores are 'better'. (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionmilliseconds (Mean)
Baseline12 Weeks
Galantamine 16mg277.2267.9
Galantamine 8mg215.3241.9
Placebo244.1234.8

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CANTAB SST- Median Correct

This is the CANTAB SST measure which evaluates response inhibition. Stop Signal Reaction Time (SSRT): The estimate of the length of time between the go stimulus and the stop stimulus at which the subject is able to successfully inhibit their response on 50% of the trials. Range of scores from 0 to 1500 (unit=milliseconds) and lower scores are 'better'. Median correct is the median of response times across 'go' trials where the subject has responded on the correct button (right or left). (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionmilliseconds (Mean)
Baseline12 Weeks
Galantamine 16mg619.7669.7
Galantamine 8mg706.3608.6
Placebo680.0631.5

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CANTAB RVIP Measure: RVP FALSE ALARM

RVIP is a computerized measure of attention. This is given at baseline and every 4 weeks over the course of the 12-week study. RVP FALSE ALARM is probability of false alarm. False alarms are responses to non-targets. Higher numbers are worse (i.e., could be seen as a measure of poor response inhibition). Scores range from 0-1 where 1 is the least desirable probablity. (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionunits on a scale (Mean)
BaselineWeek 12
Galantamine 16mg.01.03
Galantamine 8mg.04.03
Placebo.03.02

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CANTAB RVIP Measure: RVP B

"RVIP is a computerized measure of attention. This is given at baseline and every 4 weeks over the course of the 12-week study. RVP B: A measure of response bias (i.e., bias towards under-responding (to targets) versus over-responding (i.e., to non-targets)) range from -1 to +1, respectively." (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionunits on a scale (Mean)
BaselineWeek 12
Galantamine 16mg.91.91
Galantamine 8mg.77.77
Placebo.77.77

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CANTAB RVIP Measure: RVP A

RVIP is a computerized measure of attention. This is given at baseline and every 4 weeks over the course of the 12-week study. RVP A' (aka RVIP A PRIME): is a signal detection measure of target sensitivity (i.e., successful response to targets and withholding of responses to non-targets). Range of 0 to 1. Higher scores are better. (NCT01531153)
Timeframe: Baseline and 12 Weeks

,,
Interventionunits on a scale (Mean)
BaselineWeek 12
Galantamine 16mg.86.84
Galantamine 8mg.86.88
Placebo.85.87

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Blood Pressure- Systolic

Blood Pressure is taken for safety reasons (NCT01531153)
Timeframe: 2 times a week for 12 weeks

,,
InterventionmmHg (Mean)
Week 1 Time 1Week 1 Time 2Week 2 Time 1Week 2 Time 2Week 3 Time 1Week 3 Time 2Week 4 Time 1Week 4 Time 2Week 5 Time 1Week 5 Time 2Week 6 Time 1Week 6 Time 2Week 7 Time 1Week 7 Time 2Week 8 Time 1Week 8 Time 2Week 9 Time 1Week 9 Time 2Week 10 Time 1Week 10 Time 2Week 11 Time 1Week 11 Time 2Week 12 Time 1Week 12 Time 2
Galantamine 16mg127.75125.70125.62129.65123.05131.50131.47130.40133.12128.47125.94124.21121.50125.27129.56133.00121.93130.43127.00121.07125.79125.71125.54131.85
Galantamine 8mg133.62132.04132.92128.46132.29129.14129.42130.22132.30134.67131.04135.23133.68133.82136.43132.95140.95130.29136.95132.52133.86129.73131.57129.67
Placebo132.21136.68130.69130.21130.58129.00131.46131.00136.58133.27132.26132.96128.96129.86134.09134.76135.32133.50131.05128.00134.95136.18140.32134.62

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Blood Pressure- Diastolic

Blood Pressure is taken for safety reasons (NCT01531153)
Timeframe: 2 times a week for 12 weeks

,,
InterventionmmHg (Mean)
Week 1 Time 1Week 1 Time 2Week 2 Time 1Week 2 Time 2Week 3 Time 1Week 3 Time 2Week 4 Time 1Week 4 Time 2Week 5 Time 1Week 5 Time 2Week 6 Time 1Week 6 Time 2Week 7 Time 1Week 7 Time 2Week 8 Time 1Week 8 Time 2Week 9 Time 1Week 9 Time 2Week 10 Time 1Week 10 Time 2Week 11 Time 1Week 11 Time 2Week 12 Time 1Week 12 Time 2
Galantamine 16mg78.7575.7576.4880.7078.7979.5081.8881.6781.4176.5380.6380.43132.3180.0079.5082.7174.6783.5078.7577.5780.5775.3681.4680.15
Galantamine 8mg77.4279.1376.6877.4679.0074.5977.7576.0978.8776.4878.9677.7779.0579.0580.4376.90102.6474.8678.3276.1980.9576.3679.7674.90
Placebo79.5480.8879.0079.4278.3178.3580.0880.1380.1380.3680.5783.2279.8381.0981.8282.4881.2780.2381.7176.8185.0582.9184.0084.05

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Urine Toxicology

Presented are the average number of urine samples positive for cocaine over 12 weeks. This outcome was corrected from the protocol registration when the study data were entered. (NCT01531153)
Timeframe: 12 weeks

Interventionaverage cocaine positive urine samples (Mean)
Placebo16.1
Galantamine 8mg17
Galantamine 16mg14.9

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Stroop- Effect Drug Neutral Mean Correct

Drug Stroop Task is a computerized task which presents words either cocaine-related ('drug') words or non-drug-related ('neutral') words written in colored font. The subject is asked to press a button to indicate the color of the font as quickly and accurately as possible. The task is thought to measure attentional bias to drug-related stimuli. Stroop Effect is difference in response time to drug versus neutral trials (i.e., RT Correct Drug - RT Correct Neutral). A larger stroop effect is 'worse' (thought to indicate more attentional bias to drug related stimuli). (NCT01531153)
Timeframe: weeks 0, 4, 8, 12, 16, 24, 36

,,
Interventionmilliseconds (Mean)
BaselineWeek 4Week 8Week 12Week 16Week 24Week 36
Galantamine 16mg1.332.310.13-0.12-0.56-0.53-0.25
Galantamine 8mg.223.711.692.36-1.27-1.444.73
Placebo1.370.92-0.121.43-0.87-2.051.17

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Stroop- RT Correct Drug

Drug Stroop Task is a computerized task which presents words either cocaine-related ('drug') words or non-drug-related ('neutral') words written in colored font. The subject is asked to press a button to indicate the color of the font as quickly and accurately as possible. The task is thought to measure attentional bias to drug-related stimuli. RT Correct Drug is the mean response time to drug trials where the subject pressed the correct color response. (NCT01531153)
Timeframe: weeks 0, 4, 8, 12, 16, 24, 36

,,
Interventionmilliseconds (Mean)
BaselineWeek 4Week 8Week 12Week 16Week 24Week 36
Galantamine 16mg806.57815.97741.46755.87802.33768.93747.40
Galantamine 8mg795.40825.09819.39766.90847.89812.65829.28
Placebo872.44846.59829.90817.91894.15874.56990.59

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Number of Days of Abstinence During a 7-day Quit Attempt

Participants will undergo a 6-week study medication period. Day 36 will be the beginning of a 7-day practice quit attempt, during which number of days of abstinence will be assessed. (NCT01548638)
Timeframe: Days 36-43; following a 5-week dose run-up

Interventiondays (Mean)
Galantamine ER5

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Cognitive Performance: Working Memory Accuracy

"Participants will complete neurocognitive test designed to test working memory and attention and are similar to computer games, in that participants will push a button in response to the pictures they see. Working memory was measured using a computerized N-back task. During the N-back, participants are instructed to remember the location of a stimulus, a grey circle that is approximately 5 cm in diameter, as it appears randomly in 8 possible locations around the perimeter of a computer screen. Stimulus duration is 200 ms, followed by an interstimulus interval (ISI) of 2800 ms. The N-back task includes 4 conditions of varying difficulty levels: the 0-back, 1-back, 2-back, and 3-back.~Number of correct responses (true positives) is described below.~The maximum number of correct responses is 60." (NCT01548638)
Timeframe: At Baseline (Day 0), Day 35 (Day before Target Quit Day), and Day 43

Interventioncorrect responses (Mean)
Working Memory Accuracy BaselineWorking Memory Day 35Working Memory Day 43
Galantamine ER4647.446.7

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Cognitive Performance: Working Memory Reaction Time

"Participants will complete neurocognitive test designed to test working memory and attention and are similar to computer games, in that participants will push a button in response to the pictures they see. Working memory was measured using a computerized N-back task. During the N-back, participants are instructed to remember the location of a stimulus, a grey circle that is approximately 5 cm in diameter, as it appears randomly in 8 possible locations around the perimeter of a computer screen. Stimulus duration is 200 ms, followed by an interstimulus interval (ISI) of 2800 ms. The N-back task includes 4 conditions of varying difficulty levels: the 0-back, 1-back, 2-back, and 3-back.~Median reaction time to correct responses is described below.~Typical responses range from 250 ms to 1500 ms." (NCT01548638)
Timeframe: At Baseline (Day 0), Day 35 (Day before Target Quit Day), and Day 43

Interventionms (Mean)
Working Memory Reaction Time BaselineWorking Memory Reaction Time Day 35Working Memory Reaction Time Day 43
Galantamine ER575641709

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Side Effects of Galantamine

"Side effects of galantamine were assessed at the following in-person sessions: Baseline session, Days 7, 14, 21, and 28 (brief monitoring visits), Day 35 (Day before Target Quit Day), and Days 37, 39, and 43 (during the 7-day quit attempt). A 37-item checklist of side effects based on the product insert (e.g., Nausea, Vomiting, Diarrhea, Loss of appetite, Stomach pain, Constipation, Gastroesophageal Reflux Problems (Heartburn)) was administered to participants at all study visits after the Intake. An open-ended side effects question was also be included.~Items were measured on a scale from 0 (None) to 3 (Severe).~The side effect summary score (total side effects averaged from the 37 item checklist) at each visit is reported below. Each score ranges from 0 (None) to 3 (Severe)." (NCT01548638)
Timeframe: Days 7, 14, 21, 28, 35, 37, 39, and 43; Baseline session

Interventionunits on a scale (Mean)
BaselineDay 7Day 14Day 21Day 28Day 35Day 37Day 39Day 43
Galantamine ER0.0860.130.0680.0730.0570.110.0420.070.06

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Subjective Symptoms (Negative Affect)

"Subjects were asked to complete the Positive and Negative Affect Scale (PANAS) to assess symptoms of negative affect (the positive affect scale was not administered). This 10-item scale assesses was assessed at the following in-person sessions: Baseline session, Days 7, 14, 21, and 28 (brief monitoring visits), Day 35 (Day before Target Quit Day), and Days 37, 39, and 43 (during the 7-day quit attempt).~The range of possible total scores on the PANAS negative affect scale is 10-50, with higher values indicating an increased nicotine withdrawal. This range of scores represent a total score; there are no subscales within the negative affect scale of the PANAS." (NCT01548638)
Timeframe: Days 7, 14, 21, 28, 35, and 43; Baseline session

Interventionunits on a scale (Mean)
BaselineDay 7Day 14Day 21Day 28Day 35Day 37Day 39Day 43
Galantamine ER11.410.110.610.014.811.111.212.511.3

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Subjective Symptoms (Nicotine Withdrawal)

"Subjects were asked to complete the Minnesota Nicotine Withdrawal Scale - Revised version (MNWS). The scale assesses eight DSM-IV items of nicotine withdrawal. The subjective symptoms listed above were assessed at the following in-person sessions: Baseline session, Days 7, 14, 21, and 28 (brief monitoring visits), Day 35 (Day before Target Quit Day), and Days 37, 39, and 43 (during the 7-day quit attempt).~The range of possible total scores on the MNWS is 0-60, with higher values indicating an increased nicotine withdrawal. This range of scores represent a total score; there are no subscales." (NCT01548638)
Timeframe: Days 7, 14, 21, 28, 35, and 43; Baseline session

Interventionunits on a scale (Mean)
BaselineDay 7Day 14Day 21Day 28Day 35Day 37Day 39Day 43
Galantamine ER4.34.333.93.2744.92.4

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Subjective Symptoms (Smoking Urges)

"During each visit, we asked subjects to complete the Questionnaire for Smoking Urges-Brief (QSU-B). This measure is an index of urges to smoke, or cigarette craving. The subjective symptoms listed above will be assessed at the following in-person sessions: Baseline session, Days 7, 14, 21, and 28 (brief monitoring visits), Day 35 (Day before Target Quit Day), and Days 37, 39, and 43 (during the 7-day quit attempt).~The range of possible scores on the QSU-B is 10-70, with higher values indicating increased urges to smoke. This range of scores represents a total score; there are no subscales." (NCT01548638)
Timeframe: Days 7, 14, 21, 28, 35, and 43; Baseline session

Interventionunits on a scale (Mean)
BaselineDay 7Day 14Day 21Day 28Day 35Day 37Day 39Day 43
Galantamine ER30.322.31720.721.534.121.319.517.5

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Subjective Symptoms

"Smoking urges [Questionnaire of Smoking Urges-Brief; QSU-B; 10-items rated on a 7-point scale (1=strongly disagree, 7=strongly agree) and summed for total score (range: 10-70). Higher scores=greater urge to smoke.] Negative mood [Negative Affect scale (10 items) from the Positive and Negative Affect Schedule; PANAS; 20-item Likert-format measure; The subscale was summed to create a summary score (range: 10-50); Lower negative affect indicates better outcomes.] Nicotine withdrawal [Minnesota Nicotine Withdrawal Scale-Revised; MNWS-R; 15 symptoms are rated on intensity with the following scale: 0=none, 1=slight, 2=mild, 3=moderate, 4=severe. The first 9 items are summed for total score (range: 0-36); higher scores=more severe withdrawal.].~Measures assessed at the following visits: Baseline; Day 7 (monitoring visit); Day 14 (Day before 24-hour abstinence period), Day 16 (after 24-hour abstinence period), and Days 17-23 (7-day quit attempt)." (NCT01669538)
Timeframe: Baseline (day 0), Days 7, 14, 16, 17, 19, 21, and 23

,
Interventionunits on a scale (Mean)
Smoking urges (baseline)Smoking urges (day 7)Smoking urges (day 14)Smoking urges (day 16)Smoking urges (day 17)Smoking urges (day 19)Smoking urges (day 21)Smoking urges (day 23)Negative Mood (baseline)Negative Mood (day 7)Negative Mood (day 14)Negative Mood (day 16)Negative Mood (day 17)Negative Mood (day 19)Negative Mood (day 21)Negative Mood (day 23)Withdrawal (baseline)Withdrawal (day 7)Withdrawal (day 14)Withdrawal (day 16)Withdrawal (day 17)Withdrawal (day 19)Withdrawal (day 21)Withdrawal (day 23)
Galantamine29.421.621.13321.720.719.818.812.211.211.813.711.611.612.011.154.65.17.64.65.24.73.2
Placebo30.225.924.13629.725.222.223.212.712.011.913.911.712.011.812.05.65.43.97.74.64.64.84.1

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Common Side Effects of Galantamine Check List

"Subjects completed a side effect checklist at every in-person study visit over the course of the treatment period. Subjects rated the severity of 37 common side effects of galantamine on the following scale: 0=none, 1=mild, 2=moderate, 3=severe. The average of all items was used to create a summary side effect score (range for total summary score 0-3). Higher scores indicate greater severity of side effects.~Side effects of galantamine were assessed at the following in-person sessions: Baseline session; Day 7 (brief monitoring visit); Day 14 (Day before 24-hour abstinence period), Day 16 (after 24-hour abstinence period), and Days 17-23 (during the 7-day quit attempt)." (NCT01669538)
Timeframe: Baseline (day 0), Days 7, 14, 16, 17, 19, 21, and 23

,
Interventionunits on a scale (Mean)
BaselineDay 7Day 14Day 16Day 17Day 19Day 21Day 23
Galantamine.03.09.1.1.08.07.06.05
Placebo.04.07.06.08.05.05.05.05

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Cognitive Performance

Participants will complete neurocognitive tests designed to test working memory and attention. These tests are similar to computer games, in that participants will push a button in response to the pictures they see. (NCT01669538)
Timeframe: Baseline (Day 0), Day 14 (day before start of 24-hour abstinence period), Day 16 (after 24-hour abstinence period ends)

,
Interventionnumber of correct responses (Mean)
Working memory (Baseline)Working memory (Day 14)Working memory (Day 16)Attention (Baseline)Attention (Day 14)Attention (Day 16)
Galantamine47.349.049.3111.3113.9115.2
Placebo46.648.447.1103.4110.5111.0

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Total Number of Smoke-free Days (Biochemically Verified) During a 7-day Quit Attempt.

Day 17 will be the beginning of a 7-day quit attempt, during which the total number of days of abstinence will be assessed. (NCT01669538)
Timeframe: Days 17-23

Interventiondays (Mean)
Galantamine3.6
Placebo3.7

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Change From Screening at Week 16 in Mini Mental State Exam Scores (MMSE)

MMSC is a brief 30-point questionnaire test that is used for the assessment of dementia patients' cognitive impairment. Evaluation of points are as: 24-30 = No cognitive impairment, 18-23 = Mild cognitive impairment, 0-17 = Severe cognitive impairment. Lower scores indicate worsening. (NCT01734395)
Timeframe: Baseline, Week 16

InterventionUnits on a scale (Mean)
Galantamine-0.69

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Change From Baseline at Week 16 in Attention Questionnaire Scores (AQS)

AQS evaluates the attention of participants with dementia and is designed for their caregivers to evaluate the participant's attention directly. It has 15 questions devised to be suitable for cultural characteristics of Korea through the standardization study considering education and gender/culture gap. Each question is scored from 0 to 2 (0=never, 1=occasionally, 2=usually). In questions 1 to 8, the lower participant attention ability rated the higher score (AQS1), In questions 9 to 15, the higher participant attention ability rated the higher score (AQS2). The total score is calculated by the formula: 16-AQS1+AQS2 and the range is from 0 to 30. Higher score means better attention ability of participant. (NCT01734395)
Timeframe: Baseline (Week 1 [Day 1]), Week 16

InterventionUnits on a scale (Mean)
Galantamine-1.19

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Change From Baseline at Week 16 in Burden Interview (BI) Scores

BI is designed to evaluate subjective stress dementia patients' caregivers experience in relation to caregiving. It has total 22 questions with 4 options each and the calculated scores are from 1 to 88 (0-20 = Little or no burden, 21-40 = Mild to moderate burden, 41-60 = Moderate to severe burden, 61-88 = Severe burden). Higher scores indicate worsening. (NCT01734395)
Timeframe: Baseline, Week 16

InterventionUnits on a scale (Mean)
Galantamine1.48

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Smoking Choice Procedure

After overnight abstinence, participants will receive 10 tokens at the beginning of the smoking choice session. These tokens can be exchanged for money (0.75$ / token) or 2 cigarette puffs. The session starts with sample smoking of 2 puffs that allows subjective responses to me measured after abstinence. 15 min later, participants make their first choice, followed by 9 additional choices, every 15 minutes. (NCT01880099)
Timeframe: Data was acquired during a single test session during week 3 of drug intervention.

Intervention# of choices to smoke (out of 10) (Mean)
Placebo3.00
Galantamine 8mg1.00
Galantamine 16mg0.85

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KYN/TRP

The secondary outcome measure will be change in metabolite values. Values were collected in triplicate. AUC ratio reported. (NCT02234752)
Timeframe: Baseline and 6-Weeks

InterventionAUC Ratio (Number)
Baseline KYN/TRP Participant 1Week-6 KYN/TRP Participant 1Baseline KYN/TRP Participant 2Week-6 KYN/TRP Participant 2Baseline KYN/TRP Participant 3
KP Metabolites Values1.211.311.060.80.79

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KYNA/KYN

The secondary outcome measure will be change in metabolite values. Values were collected in triplicate. AUC ratio reported. (NCT02234752)
Timeframe: Baseline and 6-Weeks

InterventionAUC Ratio (Number)
Baseline KYNA/KYN Participant 1Week-6 KYNA/KYN Participant 1Baseline KYNA/KYN Participant 2Week-6 KYNA/KYN Participant 2Baseline KYNA/KYN Participant 3
KP Metabolites Values0.0750.0500.1210.1140.152

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Kynurenic Acid (KYNA)

The secondary outcome measure will be change in metabolite values. Values were collected in triplicate. MS* AUC is mass spectrometry times area under the curve. (NCT02234752)
Timeframe: Baseline and 6-Weeks

InterventionMS* AUC (Mean)
Baseline KYNA Participant 1Week-6 KYNA Participant 1Baseline KYNA Participant 2Week-6 KYNA Participant 2Baseline KYNA Participant 3
KP Metabolites Values10391183737951397328093163

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Kynurenine (KYN)

The secondary outcome measure will be change in metabolite values. Values were collected in triplicate. (NCT02234752)
Timeframe: Baseline and 6-Weeks

InterventionµM (Mean)
Baseline KYN Participant 1Week-6 KYN Participant 1Baseline KYN Participant 2Week-6 KYN Participant 2Baseline KYN Participant 3
KP Metabolites Values1.621.850.860.710.76

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PIC/KYN

The secondary outcome measure will be change in metabolite values. Values were collected in triplicate. AUC ratio reported. (NCT02234752)
Timeframe: Baseline and 6-Weeks

InterventionAUC Ratio (Number)
Baseline PIC/KYN Participant 1Week-6 PIC/KYN Participant 1Baseline PIC/KYN Participant 2Week-6 PIC/KYN Participant 2Baseline PIC/KYN Participant 3
KP Metabolites Values0.03170.01750.10390.09890.0655

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Picolinic Acid (PIC)

The secondary outcome measure will be change in metabolite values. Values were collected in triplicate. MS* AUC is mass spectrometry times area under the curve. (NCT02234752)
Timeframe: Baseline and 6-Weeks

InterventionMS* AUC (Mean)
Baseline PIC Participant 1Week-6 PIC Participant 1Baseline PIC Participant 2Week-6 PIC Participant 2Baseline PIC Participant 3
KP Metabolites Values4402129542818836374540189

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Free Tryptophan (TRP)

The secondary outcome measure will be change in metabolite values. Values were collected in triplicate. (NCT02234752)
Timeframe: Baseline and 6-Weeks

InterventionµM (Mean)
Baseline tryptophan Participant 1Week-6 tryptophan Participant 1Baseline tryptophan Participant 2Week-6 tryptophan Participant 2Baseline tryptophan Participant 3
KP Metabolites Values51.9455.7232.1724.9635.07

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Change in Level of Cognition

The primary outcome measure will be the change in level of cognition as measured by the MATRICS Consensus Cognitive Battery (MCCB). In schizophrenia, usual composite scores are 20-39. In healthy controls, usual composite scores are normalized to 40-60. Higher values of composite scores mean better cognition. Test scores are normalized to healthy controls, therefore no min-max range is available. Final scores calculated by MATRICS Consensus Cognitive Battery software. Exact minimum/maximum are not known to provider. Overall composite scores are reported. (NCT02234752)
Timeframe: Baseline and 6-Weeks

Interventionunits on a scale (Number)
Baseline Participant 1Week 6 Participant 1Baseline Participant 2Week 6 Participant 2Baseline Participant 3
Galantamine ER, Memantine XR484832259

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Change in Oxidative Stress: Baseline to 4 Hours

Measure F-2 isoprostanes as a marker of oxidation (NCT02365285)
Timeframe: Baseline to 4 hours

Interventionpg/ml (Mean)
Galantamine 16 mg (African-American)0
Galantamine 16 mg(White)-0.008
Placebo (African-American)0.003
Placebo(White)-0.008

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Change in Oxidative Stress: Baseline to 2 Hours

Measure F-2 isoprostanes as a marker of oxidation (NCT02365285)
Timeframe: Baseline to 2 hours

Interventionpg /ml (Mean)
Galantamine 16 mg (African-American)-0.003
Galantamine 16 mg (White)-0.006
Placebo (African-American)0.01
Placebo (White)-0.006

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Change Detection Task Reaction Time

"The task requires encoding the color of 1 or 5 shape items and reporting whether or not one of the items changed color.~One participant's data were excluded from this task because of excessive no-response trials." (NCT02420327)
Timeframe: 15 min

Interventionms (Mean)
Placebo Patch and Placebo Capsule1018
Nicotine Patch and Placebo Capsule1023
Placebo Patch and Galantamine Capsule1043
Nicotine Patch and Galantamine Capsule973

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Change Detection Task Accuracy

"The task requires encoding the color of 1 or 5 shape items and reporting whether or not one of the items changed color. Accuracy refers to the percentage of all trials in which a correct response was given.~One participant's data were excluded from this task because of excessive no-response trials." (NCT02420327)
Timeframe: 15 min

Interventionpercentage of all trials (Mean)
Placebo Patch and Placebo Capsule83
Nicotine Patch and Placebo Capsule83
Placebo Patch and Galantamine Capsule84
Nicotine Patch and Galantamine Capsule84

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Spatial Attentional Resource Allocation Task (SARAT) Non-predictive Trial Reaction Time

The task requires responding to brief target stimuli presented randomly in one of four locations in the four corners of the screen. On non-predictive trial, the cue does not provide any advance information about where the target will occur. (NCT02420327)
Timeframe: 45 min

Interventionms (Mean)
Placebo Patch and Placebo Capsule472
Nicotine Patch and Placebo Capsule455
Placebo Patch and Galantamine Capsule465
Nicotine Patch and Galantamine Capsule449

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Spatial Attentional Resource Allocation Task Predictive Trials Reaction Time

The task requires detecting brief target stimuli presented at one of four locations in the four corner of the screen. On predictive trials, a central cue predicts the target location. (NCT02420327)
Timeframe: 45 min

Interventionms (Mean)
Placebo Patch and Placebo Capsule420
Nicotine Patch and Placebo Capsule408
Placebo Patch and Galantamine Capsule416
Nicotine Patch and Galantamine Capsule413

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Rapid Visual Information Processing Task Reaction Time

The task requires the detection of three consecutive odd or three consecutive even digits in a stream of sequentially presented digits. (NCT02420327)
Timeframe: 30 min

Interventionms (Mean)
Placebo Patch and Placebo Capsule463
Nicotine Patch and Placebo Capsule459
Placebo Patch and Galantamine Capsule473
Nicotine Patch and Galantamine Capsule459

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Rapid Visual Information Processing Task Hit Rate

The task requires following a stream of digits and detecting three consecutive odd or even numbers. The Hit Rate reflects the percentage of all target sequences that were detected. (NCT02420327)
Timeframe: 30 min

Interventionpercentage of all targets (Mean)
Placebo Patch and Placebo Capsule50
Nicotine Patch and Placebo Capsule54
Placebo Patch and Galantamine Capsule49
Nicotine Patch and Galantamine Capsule54

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Profile of Mood Scale - Total Mood Disturbance

"Participants rate their current subjective state on a list of adjectives, which contribute to six factors/subscales. Total Mood Disturbance is a composite measure, obtained by summing the scores of all subscales, each with a range of 0-4, weighting the one positively valenced factor negatively. Thus, smaller or more negative values represent a more positive mood state. The theoretical range of the Total Mood Disturbance measure is from -4 to +20." (NCT02420327)
Timeframe: 5 min

Interventionscore on a scale (Mean)
Placebo Patch and Placebo Capsule-0.32
Nicotine Patch and Placebo Capsule-0.48
Placebo Patch and Galantamine Capsule-0.60
Nicotine Patch and Galantamine Capsule-0.43

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Montreal Cognitive Assessment (MoCA)

MoCA scores range between 0 and 30. Higher scores indicate a better outcome, and a score of 26 or over is considered to be normal. (NCT02872857)
Timeframe: baseline (in hospital)

Interventionscore on a scale (Mean)
Galantamine7.5
Placebo8.2

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Mortality

(NCT02872857)
Timeframe: 90 days

InterventionParticipants (Count of Participants)
Galantamine1
Placebo4

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Montreal Cognitive Assessment (MoCA)

MoCA scores range between 0 and 30. Higher scores indicate a better outcome, and a score of 26 or over is considered to be normal. (NCT02872857)
Timeframe: 90 days

Interventionscore on a scale (Mean)
Galantamine14.0
Placebo15.8

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EuroQOL Score as Assessed by a Visual Analogue Scale (VAS)

"In the EuroQOL VAS assessment, health status is marked on a 20 cm vertical scale with end points of 0 and 100. 0 corresponds to the worst health you can imagine, and 100 corresponds to the best health you can imagine." (NCT02872857)
Timeframe: 90 days

Interventionunits on a scale (Mean)
Galantamine76.2
Placebo74.0

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Tolerability as Assessed by the Number of Participants Who Stop Study Medication Due to Adverse Event Possibly Associated With Study Drug

(NCT02872857)
Timeframe: 90 days

InterventionParticipants (Count of Participants)
Galantamine1
Placebo1

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Substance Use Calendar

number of days of opioid use, assessed by self-report (NCT03547622)
Timeframe: during 10 weeks of study

InterventionDays (Mean)
MAT Taper With Galantamine1.0
MAT Taper With Placebo0

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Clinical Opioid Withdrawal Scale (COWS)

"opioid withdrawal score at week 0 (baseline) and at 10 weeks (post treatment).~11-item scale designed to be administered by a clinician. Rates common signs and symptoms of opiate withdrawal and can be monitored over time. The summed score for the complete scale can be used to help clinicians determine the stage or severity of opiate withdrawal and assess the level of physical dependence on opioids. Score of 5-12 = mild; 13-24=moderate; 25-36=moderately severe; more than 36=severe withdrawal (Scale of 0 to 40)." (NCT03547622)
Timeframe: Data at week 0 (baseline) and week 10 (post treatment)

,
Interventionscore on a scale (Mean)
Week 0 (baseline) ScoreWeek 10 (Post Treatment Score)
MAT Taper With Galantamine04.3
MAT Taper With Placebo.334.2

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Change in Methadone/Buprenorphine Dose to 0 mg for Successful Completion of Taper

"Number of participants who were able to taper to 0 mg from methadone or buprenorphine over 10 weeks of treatment.~Data about current medication and dose in mg was collected at the start of treatment (week 1) was recorded on a weekly medical sheet. Data was then collected weekly from participant self-report and verified through the clinic database." (NCT03547622)
Timeframe: during 10 weeks of study and up to 3 months after the end of opioid taper

InterventionParticipants (Count of Participants)
MAT Taper With Galantamine3
MAT Taper With Placebo2

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