Page last updated: 2024-12-04

huperzine a

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Description

huperzine A: RN given refers to 5R-(5alpha,9beta,11E)-isomer; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

huperzine A : A sesquiterpene alkaloid isolated from a club moss Huperzia serrata that has been shown to exhibit neuroprotective activity. It is also an effective inhibitor of acetylcholinesterase and has attracted interest as a therapeutic candidate for Alzheimer's disease. [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
HuperziagenusA plant genus of the family LYCOPODIACEAE. Members contain huperzine, one of the CHOLINESTERASE INHIBITORS.[MeSH]LycopodiaceaeThe club-moss plant family of the order Lycopodiales, class Lycopodiopsida, division Lycopodiophyta, subkingdom TRACHEOPHYTA. The common name of clubmoss applies to several genera of this family. Despite the name this is not one of the true mosses (BRYOPSIDA ).[MeSH]
Huperzia serrataspecies[no description available]LycopodiaceaeThe club-moss plant family of the order Lycopodiales, class Lycopodiopsida, division Lycopodiophyta, subkingdom TRACHEOPHYTA. The common name of clubmoss applies to several genera of this family. Despite the name this is not one of the true mosses (BRYOPSIDA ).[MeSH]

Cross-References

ID SourceID
PubMed CID1253
CHEMBL ID3184073
MeSH IDM0143991
PubMed CID854026
CHEMBL ID395280
CHEBI ID78330
CHEBI ID94624
SCHEMBL ID136368
MeSH IDM0143991

Synonyms (106)

Synonym
120786-18-7
CBIOL_001885
huperzine a
fordine
BIO2_000882
BIO2_000402
BIO1_001149
BIO1_000171
BIO1_000660
BSPBIO_001143
selagine
(-)-huperzine a ,
bdbm10441
(+)-huperzine a
(13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7}]trideca-2(7),3,10-trien-5-one
(1r,13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7}]trideca-2(7),3,10-trien-5-one
(5s,11e)-5-amino-11-ethylidene-7-methyl-5,6,9,10-tetrahydro-5,9-methanocycloocta[b]pyridin-2(1h)-one
(1s,13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7}]trideca-2(7),3,10-trien-5-one
(+/-)huperzine a
IDI1_002157
(+/-)-huperzine a
NCGC00163246-01
KBIO2_003051
KBIOSS_000483
KBIO2_000483
KBIO3_000885
KBIO2_005619
KBIOGR_000483
KBIO3_000886
102518-79-6
HMS1990I05
103735-86-0
huperzine-a
FT-0642946
5,9-methanocycloocta(b)pyridin-2(1h)-one,5-amino-11-ethylidene-5,6,9,10-tetrah
CHEMBL3184073
(-)-huperzine a-d5 (major)
1290113-17-5
AKOS032962044
Q27163539
lsm-1581
BCP31534
fordine; (+/-)-huperzine a
1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.02,7]trideca-2(7),3,10-trien-5-one
(1r,9r)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7]trideca-2(7),3,10-trien-5-one
(1r,9r,13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7]trideca-2(7),3,10-trien-5-one
(13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.02,7]trideca-2(7),3,10-trien-5-one
BRD-K62240499-001-02-6
SDCCGMLS-0066755.P001
hup a
cerebra
5,9-methanocycloocta(b)pyridin-2(1h)-one, 5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-, (5r-(5-alpha,9-beta,11e))-
5,9-methanocycloocta(b)pyridin-2(1h)-one, 5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-, (5r,9r,11e)-
HUP ,
huperaine a
1VOT
SPECTRUM1505255
1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0~2,7~]trideca-2(7),3,10-trien-5-one
1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one((+/-)-huperzine a)
(+-)-ha
bdbm50199522
(huperazine a)(-)-1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one
(r)-1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one
1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one((-)-huperzine a)
(-)-huperazine a
1-amino-13-eth-(e)-ylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one
(-)1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one( (-)-huperzine a)
1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one
1-amino-13-eth-(z)-ylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one
hyperazzine a
(-)-1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one(huperzine a)
(r)-1-amino-13-eth-(e)-ylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one
(1r,9r)-1-amino-13-eth-(e)-ylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one
chebi:78330 ,
CHEMBL395280 ,
l-huperzine a
tox21_111603
dtxcid6026038
cas-102518-79-6
dtxsid8046038 ,
CCG-40292
kimpukan a
0111871i23 ,
unii-0111871i23
huperzine a [who-dd]
(5r,9r,11e)-5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-5,9-methanocycloocta(b)pyridin-2(1h)-one
huperzine a [vandf]
huperzine a [mi]
DB04864
SCHEMBL136368
NCGC00263655-01
tox21_111603_1
H1700
(5r,9r,11e)-5-amino-11-ethylidene-7-methyl-5,6,9,10-tetrahydro-5,9-methanocycloocta[b]pyridin-2(1h)-one
(5r,9r,e)-5-amino-11-ethylidene-7-methyl-5,6,9,10-tetrahydro-5,9-methanocycloocta[b]pyridin-2(1h)-one
Q-100029
5,9-methanocycloocta[b]pyridin-2(1h)-one, 5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-, (5r,9r,11e)-
CHEBI:94624
huperzin a
1369-64-8
Q425198
AS-15723
AKOS016842839
(-)-huperazinea
(1r,9r,13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0,2,7]trideca-2(7),3,10-trien-5-one
EN300-33171546

Research Excerpts

Overview

Huperzine A (Hup A) is a purified alkaloid compound extracted from a club moss called Huperzia serrata. It is an effective inhibitor of acetylcholinesterase and has attracted great interest as a therapeutic candidate for Alzheimer's disease.

ExcerptReferenceRelevance
"Huperzine A (Hup A) is a purified alkaloid compound extracted from a club moss called Huperzia serrata."( A Synopsis of Multitarget Potential Therapeutic Effects of Huperzine A in Diverse Pathologies-Emphasis on Alzheimer's Disease Pathogenesis.
Govitrapong, P; Shukla, M; Wongchitrat, P, 2022
)
1.69
"Huperzine A (HpzA) is a natural sesquiterpene alkaloid found in"( Mechanistic Insight into Binding of Huperzine A with Human Serum Albumin: Computational and Spectroscopic Approaches.
Abdullaev, B; Al Abdulmonem, W; Alhumaydhi, FA; Alsagaby, SA; Khan, MS; Shahwan, M; Shamsi, A; Yadav, DK, 2022
)
1.72
"Huperzine A (HupA) is a plant-derived lycopodium alkaloid used for the treatment of Alzheimer's disease due to its inhibition against acetylcholinesterase. "( Delineating biosynthesis of Huperzine A, A plant-derived medicine for the treatment of Alzheimer's disease.
Li, W; Li, X; Tan, T; Tian, P, 2022
)
2.46
"Huperzine A (HupA) is a natural acetylcholinesterase inhibitor (AChEI) with the advantages of high efficiency, selectivity as well as reversibility and can exhibit significant therapeutic effects against certain neurodegenerative diseases. "( Huperzine-A Improved Animal Behavior in Cuprizone-Induced Mouse Model by Alleviating Demyelination and Neuroinflammation.
Sun, J; Wang, D; Wang, J; Wang, Y; Wu, S; Zhang, H, 2022
)
2.16
"Huperzine A (HupA) is a selective acetylcholinesterase inhibitor used to treat Alzheimer's disease. "( The Optimization Design Of Lactoferrin Loaded HupA Nanoemulsion For Targeted Drug Transport Via Intranasal Route.
Ding, Z; Han, T; Jiang, Y; Liu, C; Zhai, W; Zhuang, N, 2019
)
1.96
"Huperzine A (Hup A) is an important drug for treating Alzheimer's disease (AD) and mainly extracted from the Huperzia serrata (Thunb.) Trevis. "( Five novel and highly efficient endophytic fungi isolated from Huperzia serrata expressing huperzine A for the treatment of Alzheimer's disease.
Fei, L; Han, Z; Li-Bin, Y; Lu, H; Min, J; Ning, Z; Wei-Ze, L; Wen-Xia, H; Xiao-Feng, L; Zhong-Wen, H, 2020
)
2.22
"Huperzine A (HupA) is an effective inhibitor of acetylcholinesterase and has attracted great interest as a therapeutic candidate for Alzheimer's disease. "( Research on endophytic fungi for producing huperzine A on a large-scale.
Sang, X; Su, J; Yang, M, 2020
)
2.26
"Huperzine A (HupA) is an anti-Alzheimer's therapeutic and a dietary supplement for memory boosting that is extracted mainly from Huperziacae plants. "( Response surface methodology-mediated improvement of the irradiated endophytic fungal strain, Alternaria brassicae AGF041 for Huperzine A-hyperproduction.
Ahmed, AS; Al-Hagar, OEA; El-Shatoury, EH; Zaki, AG, 2021
)
2.27
"Huperzine A (HupA) is a potent acetylcholinesterase inhibitor (AChEI) that has been used treatment of Alzheimer's disease (AD)."( Huperzine A alleviates neuroinflammation, oxidative stress and improves cognitive function after repetitive traumatic brain injury.
Mei, Z; Situ, B; Tan, X; Wang, Y; Zheng, P, 2017
)
2.62
"Huperzine A (HupA) is a naturally occurring acetylcholinesterase inhibitor with newly discovered potent GABA-mediated antiepileptic capacity, which is reliably detected by ppTMS."( Alterations in the Timing of Huperzine A Cerebral Pharmacodynamics in the Acute Traumatic Brain Injury Setting.
Collins, S; Damar, U; Gersner, R; Johnstone, JT; Kapur, K; Rotenberg, A; Schachter, S, 2018
)
1.49
"Huperzine A (HupA) is a potent acetylcholinesterase (AChE) inhibitor of a great consideration as a prospective drug candidate for Alzheimer's disease treatment. "( Production and enhancement of the acetylcholinesterase inhibitor, huperzine A, from an endophytic Alternaria brassicae AGF041.
Ahmed, AS; Al-Hagar, OEA; El-Shatoury, EH; Zaki, AG, 2019
)
2.19
"Huperzine A (Hup-A) is a natural compound, which might have potential in treating neurological disorders including epilepsy and Alzheimer's disease."( The potential role of human multidrug resistance protein 1 (MDR1) and multidrug resistance-associated protein 2 (MRP2) in the transport of Huperzine A
Baum, L; Fei, Z; Hong, T; Hu, M; Kwan, P; Zhang, C, 2020
)
1.48
"Huperzine A (HupA) is a kind of Lycopodium alkaloid with potential disease-modifying qualities that has been reported to protect against β-amyloid (Aβ)-mediated mitochondrial damage in Alzheimer's disease. "( ABAD/17β-HSD10 reduction contributes to the protective mechanism of huperzine a on the cerebral mitochondrial function in APP/PS1 mice.
Chen, Q; Wang, Y; Xiao, X; Zhu, X, 2019
)
2.19
"Huperzine A (Hup A) is a lycopodium alkaloid from Huperzia serrata, which has been used as a therapeutic agent in several neurological disorders. "( Huperzine A promotes hippocampal neurogenesis in vitro and in vivo.
Gong, K; Gong, Y; Ma, T; Tang, P; Yan, Y; Zhang, L; Zhang, X, 2013
)
3.28
"Huperzine A (HupA) is a plant alkaloid that is of great interest as a therapeutic candidate for the treatment of Alzheimer's disease. "( Ethanol and methanol can improve huperzine A production from endophytic Colletotrichum gloeosporioides ES026.
Ahn, YJ; Hu, X; Shu, SH; Wang, M; Wang, WJ; Wang, ZQ; Xu, HJ; Zhao, XM, 2013
)
2.11
"Huperzine A is a Chinese herb extract used for Alzheimer's disease. "( Huperzine A for Alzheimer's disease: a systematic review and meta-analysis of randomized clinical trials.
Liu, JP; Tian, J; Wang, Y; Yang, G, 2013
)
3.28
"Huperzine A (HupA) is an alkaloid isolated from the Chinese folk medicine huperzia serrate, which has possessed diverse pharmacological actions."( The protective effect of huperzine A against hepatic ischemia reperfusion injury in mice.
Jiang, Q; Yang, J; Yang, Y, 2014
)
1.43
"Huperzine A (HupA) is a naturally occurring compound found in the firmoss Huperzia serrata. "( Huperzine A prophylaxis against pentylenetetrazole-induced seizures in rats is associated with increased cortical inhibition.
Dhamne, SC; Ekstein, D; Gersner, R; Rotenberg, A; Schachter, SC, 2015
)
3.3
"Huperzine A (HupA) is an acetylcholinesterase (AChE) inhibitor extracted from Huperzia Serrata, a firmoss, which has been used for various diseases in traditional Chinese medicine for fever and inflammation. "( Huperzine A as a neuroprotective and antiepileptic drug: a review of preclinical research.
Damar, U; Gersner, R; Johnstone, JT; Rotenberg, A; Schachter, S, 2016
)
3.32
"Huperzine A is a well-tolerated drug that could significantly improve cognitive performance and ADL in patients with AD."( Efficacy and safety of natural acetylcholinesterase inhibitor huperzine A in the treatment of Alzheimer's disease: an updated meta-analysis.
Chen, HZ; Song, YY; Wang, BS; Wang, H; Wei, ZH; Zhang, L, 2009
)
1.31
"Huperzine A (HupA) is an alkaloid isolated from the Chinese club moss Huperzia serrata and has been used for improving memory, cognitive and behavioral function in patients with Alzheimer's disease in China. "( Intrathecal huperzine A increases thermal escape latency and decreases flinching behavior in the formalin test in rats.
Park, P; Schachter, S; Yaksh, T, 2010
)
2.18
"Huperzine A is a reversible acetylcholinesterase (AChE) inhibitor, its administration results in regionally specific increases in acetylcholine levels in the brain."( The effects of huperzine A and IDRA 21 on visual recognition memory in young macaques.
Gale, K; Kozikowski, AP; Malkova, L, 2011
)
1.44
"Huperzine A (HupA) is a reversible and selective inhibitor of acetylcholinesterase (AChE), and it has multiple targets when used for Alzheimer's disease (AD) therapy. "( Huperzine A activates Wnt/β-catenin signaling and enhances the nonamyloidogenic pathway in an Alzheimer transgenic mouse model.
Teng, WP; Wang, CY; Wang, SL; Wang, T; Wang, ZY; Xie, JW; Zhao, BL; Zheng, W, 2011
)
3.25
"Huperzine A is a natural cholinesterase inhibitor derived from the Chinese herb Huperzia serrata that may compare favorably in symptomatic efficacy to cholinesterase inhibitors currently in use for Alzheimer disease (AD)."( A phase II trial of huperzine A in mild to moderate Alzheimer disease.
Aisen, PS; Behan, K; Jin, S; Little, JT; Rafii, MS; Reynolds, B; Thomas, R; Walsh, S; Ward, C, 2011
)
2.14
"Huperzine A (HupA) is a potent acetylcholinesterase inhibitor (AChEI) used in the treatment of Alzheimer's disease (AD). "( Huperzine A alleviates synaptic deficits and modulates amyloidogenic and nonamyloidogenic pathways in APPswe/PS1dE9 transgenic mice.
Tang, XC; Wang, Y; Zhang, HY, 2012
)
3.26
"Huperzine A is an important compound that is used to treat Alzheimer's disease."( Chiral separation of Huperzine A using CE - method validation and application in pharmaceutical formulations.
Kapnissi-Christodoulou, CP; Moore, L; Nicolaou, IN; Tsioupi, DA, 2012
)
1.42
"Huperzine A is a bioactive compound derived from traditional Chinese medicine plant Qian Ceng Ta (Huperzia serrata), and was found to have multiple neuroprotective effects. "( Examining the interactome of huperzine A by magnetic biopanning.
Gao, G; Guo, W; Liu, S; Peng, J; Qiu, Y; Sun, Y; Wang, P; Wei, X; Xu, Y, 2012
)
2.11
"[-]-Huperzine A ([-]-Hup A), is a naturally occurring potent reversible AChE inhibitor that penetrates the blood-brain barrier."( A combination of [+] and [-]-Huperzine A improves protection against soman toxicity compared to [+]-Huperzine A in guinea pigs.
Doctor, BP; Nambiar, MP; Oguntayo, S; Wang, Y; Wei, Y, 2013
)
1.16
"Huperzine A (HupA) is a selective inhibitor of acetylcholinesterase (AChE) and has been shown to significantly reduce cognitive impairment in animal models of dementia."( Huperzine A, but not tacrine, stimulates S100B secretion in astrocyte cultures.
Abib, R; Gonçalves, CA; Guerra, MC; Leite, MC; Lunardi, P; Nardin, P, 2013
)
2.55
"Huperzine A is a reversible and selective cholinesterase inhibitor approved for the treatment of Alzheimer's disease. "( Identification of cytochrome P450 1A2 as enzyme involved in the microsomal metabolism of Huperzine A.
Ma, X; Tu, Z; Wang, H; Xin, J; Zhang, T, 2003
)
1.98
"(-) Huperzine A is an inhibitor of AChE and is being considered for the treatment of Alzheimer's disease."( Enantiomer effects of huperzine A on the aryl acylamidase activity of human cholinesterases.
Darvesh, S; Martin, E; Walsh, R, 2003
)
1.11
"Huperzine A is a potent, reversible red cells acetylcholinesterases (AChE) inhibitor, which shows high specificity for AChE preserving scavenger capacity of plasma butyrylcholinesterase (BuChE) for OP agents, and cross the blood-brain barrier smoothly preventing the AChE in CNS, so the CNS damages induced by the acute OP poisoning were prevented."( [Advances on study of organophosphate poisoning prevented by Huperzine A].
Liu, L; Sun, JX, 2005
)
1.29
"Huperzine A is a potent, reversible acetylcholinesterase inhibitor. "( Simple determination of huperzine A in human plasma by liquid chromatographic-tandem mass spectrometric method.
Jiang, XH; Lan, K; Li, YX; Wang, L, 2007
)
2.09
"Huperzine A is an anticholinesterase and cognitive enhancer, which is able to alleviate the symptoms of memory dysfunction in the mouse. "( Prolonged effects of poly(lactic-co-glycolic acid) microsphere-containing huperzine A on mouse memory dysfunction induced by scopolamine.
Fu, F; Liu, J; Liu, K; Ma, H; Wang, C; Zhang, T, 2007
)
2.01
"Huperzine A is a natural cholinesterase inhibitor derived from the Chinese herb Huperzia serrata. "( An update on huperzine A as a treatment for Alzheimer's disease.
Aisen, PS; Little, JT; Walsh, S, 2008
)
2.16
"Huperzine A is a linearly competitive, reversible inhibitor of acetyl cholinesterase that is said to have both central and peripheral activity with the ability to protect cells against hydrogen peroxide, beta-amyloid protein (or peptide), glutamate, ischemia and staurosporine-induced cytotoxicity and apoptosis."( Huperzine A for Alzheimer's disease.
Dong, BR; Li, J; Liu, GJ; Wu, HM; Zhou, RL, 2008
)
2.51
"Huperzine A (HUP) is a naturally-occurring, potent, reversible inhibitor of acetylcholinesterase (AChE) that crosses the blood-brain barrier. "( Huperzine A as a pretreatment candidate drug against nerve agent toxicity.
Ashani, Y; Doctor, BP; Grunwald, J; Raveh, L, 1994
)
3.17
"Huperzine A (HUP) is a potent reversible inhibitor of acetylcholinesterase (AChE) that crosses the blood-brain barrier. "( Efficacy of huperzine in preventing soman-induced seizures, neuropathological changes and lethality.
Aubriot, S; Baubichon, D; Burckhart, MF; Lallement, G; Masqueliez, C; Veyret, J, 1997
)
1.74
"Huperzine A is a strong inhibitor of cholinesterases with high selectivity to acetylcholinesterase and in China is developed as therapeutic against Alzheimer's disease."( Huperzine A--an interesting anticholinesterase compound from the Chinese herbal medicine.
Patocka, J, 1998
)
2.46
"Huperzine A is an alkaloid isolated from a chinese club-moss. "( [Huperzine a: an acetylcholinesterase inhibitor with high pharmacological potential].
Masson, P; Pilotaz, F, 1999
)
2.66
"Huperzine A is an alkaloid which was first isolated from Huperzia serrata (Thumb) Trev by Zhejiang Academy of Medical Sciences and Shanghai Institute of Materia Medica, Chinese Academy of Sciences. "( [Drug evaluation of huperzine A in the treatment of senile memory disorders].
Han, YY; Ma, YX; Sang, GW; Tang, XC; Yang, RM; Zhang, CL; Zhang, RW; Zhang, YD, 1991
)
2.05
"Huperzine A (Hup-A) is a new alkaloid extracted from Huperzia serata in China. "( [Effects of huperzine A on electroencephalography power spectrum in rabbits].
Chen, SS; Guan, LC; Lu, WH; Tang, XC, 1989
)
2.1

Effects

Huperzine A has been shown to be useful in the treatment of symptoms of dementia of the Alzheimer type.

ExcerptReferenceRelevance
"Huperzine A has been identified as a potent natural product against Alzheimer's disease."( Natural Products as Bioactive Agents in the Prevention of Dementia.
Asif, M; Hussain, A; Nawaz, F; Rasool, M; Ullah, H, 2023
)
1.63
"Huperzine A (Hup A) has attracted considerable attention as an effective therapeutic candidate drug used to treat Alzheimer's disease. "( Diversity of endophytic fungal community in Huperzia serrata from different ecological areas and their correlation with Hup A content.
He, A; Jia, Q; Liang, Z; Liu, Q; Ma, N; Pang, B; Qiu, L; Shen, H; Wang, D; Yin, D; Zhai, Y, 2022
)
2.16
"Huperzine A has been used for improving symptoms of Alzheimer's disease. "( Abcb1a but not Abcg2 played a predominant role in limiting the brain distribution of Huperzine A in mice.
Li, J; Wang, M; Yue, M; Zhang, H; Zhou, D, 2017
)
2.12
"Huperzine A has been shown to be useful in the treatment of symptoms of dementia of the Alzheimer type. "( Natural and synthetic Huperzine A: effect on cholinergic function in vitro and in vivo.
Hanin, I; Kindel, GL; Kozikowski, AP; Tang, XC, 1993
)
2.04

Actions

Huperzine A can inhibit cholinesterase in the brain to improve the cognitive function of rats recovering from general anesthesia.

ExcerptReferenceRelevance
"Huperzine A can inhibit cholinesterase to increase Ach, which has a positive effect on cerebral cholinergic system in elderly patients during recovery from general anesthesia."( [Effect of huperzine A on cerebral cholinesterase and acetylcholine in elderly patients during recovery from general anesthesia].
Wang, G; Zhan, H; Zhang, SQ, 2006
)
2.17
"Huperzine A can inhibit cholinesterase in the brain to improve the cognitive function of rats recovering from general anesthesia."( [Effects of huperzine A on cognitive function of rats recovering from general anesthesia].
Chen, HW; Luo, GJ; Wang, G; Zhan, H; Zhang, SQ, 2008
)
2.17

Treatment

Huperzine A treatment (0.1 mg/kg) resulted in significant protection against both HI-induced brain tissue losses and spatial memory impairments. Treatment also reduced glutamate-induced calcium mobilization, but did not affect elevations in intraneuronal free Ca2+ caused by KCl or (-)Bay K 8644.

ExcerptReferenceRelevance
"Huperzine A treatment was shown to significantly attenuate the neurotoxicity of oligomeric Aβ(42), as demonstrated by increased neuronal viability."( Involvement of Intracellular and Mitochondrial Aβ in the Ameliorative Effects of Huperzine A against Oligomeric Aβ42-Induced Injury in Primary Rat Neurons.
Jiang, HL; Lei, Y; Qin, MY; Tang, XC; Yang, HY; Yang, L; Ye, CY; Zhang, HY, 2015
)
1.36
"Huperzine A treatment significantly ameliorated all these phenomena."( Huperzine a improves chronic inflammation and cognitive decline in rats with cerebral hypoperfusion.
Tang, XC; Wang, J; Zhang, HY, 2010
)
2.52
"Huperzine A treatment (0.1 mg/kg) resulted in significant protection against both HI-induced brain tissue losses and spatial memory impairments (mean escape latency: 34 s vs 44 s, P < 0.05, probe time: 35 s vs 14 s,P < 0.01)."( [Huperzine A attenuates cognitive deficits and brain injury after hypoxia-ischemic brain damage in neonatal rats].
Shao, XM; Tang, XC; Wang, LS; Zhou, J, 2003
)
1.95
"Huperzine A pretreatment also reduced glutamate-induced calcium mobilization, but did not affect elevations in intraneuronal free Ca2+ ([Ca]i) caused by KCl or (-)Bay K 8644."( Huperzine A, a potential therapeutic agent for dementia, reduces neuronal cell death caused by glutamate.
Dave, JR; Doctor, BP; Koenig, ML; Ved, HS, 1997
)
2.46
"Treatment with Huperzine A, a compound isolated from Chinese club moss with NMDA receptor blocking activity, anticholinesterase activity, and anticonvulsant properties, produced useful suppression of the abnormal behavior for more than months."( Clinical use of an herbal-derived compound (Huperzine A) to treat putative complex partial seizures in a dog.
Dodman, NH; Faissler, D; Ogata, N; Schneider, BM, 2009
)
0.95

Toxicity

Huperzine A is toxic at higher doses due to potent AChE inhibition which limits the utilization of its neuroprotective properties. Mild and transient adverse events (edema of bilateral ankles and insomnia) were observed in 3% of huperzine Alpha treated patients.

ExcerptReferenceRelevance
" LD50 of soman was determined at various time intervals after pretreatment."( Huperzine A as a pretreatment candidate drug against nerve agent toxicity.
Ashani, Y; Doctor, BP; Grunwald, J; Raveh, L, 1994
)
1.73
" Mild and transient adverse events (edema of bilateral ankles and insomnia) were observed in 3% of huperzine Alpha treated patients."( [Clinical efficacy and safety of huperzine Alpha in treatment of mild to moderate Alzheimer disease, a placebo-controlled, double-blind, randomized trial].
Chen, Q; Shan, G; Shu, L; Wang, J; Wang, X; Zhang, Z, 2002
)
0.81
"A safe and effective medicine, huperzine Alpha remarkably improves the cognition, behavior, ADL,and mood of AD patients."( [Clinical efficacy and safety of huperzine Alpha in treatment of mild to moderate Alzheimer disease, a placebo-controlled, double-blind, randomized trial].
Chen, Q; Shan, G; Shu, L; Wang, J; Wang, X; Zhang, Z, 2002
)
0.88
" Our data show that a combination of HUP with IMI is a prophylactic, potent, and safe therapeutic strategy to overcome DFP toxicity."( The combination of huperzine A and imidazenil is an effective strategy to prevent diisopropyl fluorophosphate toxicity in mice.
Auta, J; Costa, E; Guidotti, A; Kadriu, B; Kozikowski, AP; Pibiri, F; Pinna, G, 2008
)
0.67
" Most adverse events were cholinergic in nature and no serious adverse events occurred."( Efficacy and safety of natural acetylcholinesterase inhibitor huperzine A in the treatment of Alzheimer's disease: an updated meta-analysis.
Chen, HZ; Song, YY; Wang, BS; Wang, H; Wei, ZH; Zhang, L, 2009
)
0.59
"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
)
0.6
" However, [-]-Huperzine A is toxic at higher doses due to potent AChE inhibition which limits the utilization of its neuroprotective properties."( [+]-Huperzine A protects against soman toxicity in guinea pigs.
Doctor, BP; Jensen, N; Nambiar, MP; Oguntayo, S; Wang, Y; Wei, Y, 2011
)
1.29
" The synthetic stereoisomer, [+]-Hup A, is less toxic due to poor AChE inhibition and is suitable for both pre-/post-exposure treatments of nerve agent toxicity."( A combination of [+] and [-]-Huperzine A improves protection against soman toxicity compared to [+]-Huperzine A in guinea pigs.
Doctor, BP; Nambiar, MP; Oguntayo, S; Wang, Y; Wei, Y, 2013
)
0.68
"Huperzine A was safe and well-tolerated and compared with placebo, treatment with huperzine A did not cause significant changes in any cocaine pharmacokinetic parameters (all P>."( Safety and Preliminary Efficacy of the Acetylcholinesterase Inhibitor Huperzine A as a Treatment for Cocaine Use Disorder.
De La Garza, R; Mahoney, JJ; Newton, TF; Thompson-Lake, DG; Verrico, CD, 2015
)
2.09
" The elevations of p-Akt and p-mTOR were abrogated under toxic conditions after blockade of TrkB by TrkB IgG."( Huperzine A Alleviates Oxidative Glutamate Toxicity in Hippocampal HT22 Cells via Activating BDNF/TrkB-Dependent PI3K/Akt/mTOR Signaling Pathway.
Li, X; Liu, ZQ; Mao, XY; Zhou, HH, 2016
)
1.88
" Huperzine is safe with mild side effects."( [Efficacy and safety of huperzine A in treating patients with mild cognitive impairment: a systematic review and Meta-analysis].
Feng, S; Guo, YH; Hu, J; Huang, P; Li, B; Liu, QQ, 2019
)
0.82

Pharmacokinetics

Huperzine A, an acetylcholinesterase inhibitor used to treat Alzheimer's disease (AD) patients in China, exhibits different pharmacokinetic features in elderly and young healthy subjects. After single-dose administration of ZT-1, the mean tmax of Hup A was 0.

ExcerptReferenceRelevance
" The pharmacokinetic parameters were calculated with a 3P87 program by computer."( Pharmacokinetics of tablet huperzine A in six volunteers.
Chen, GS; Chen, K; Qian, BC; Wang, M; Zhou, RR; Zhou, ZF, 1995
)
0.59
" The pharmacokinetic parameters were as follows: T 1/2ka = 12."( Pharmacokinetics of tablet huperzine A in six volunteers.
Chen, GS; Chen, K; Qian, BC; Wang, M; Zhou, RR; Zhou, ZF, 1995
)
0.59
" Pharmacokinetic parameters were calculated by non-compartmental methods."( Pharmacokinetics of huperzine A in dogs following single intravenous and oral administrations.
Chu, D; Gu, J; Li, P; Li, Y; Liu, K; Liu, W, 2006
)
0.66
" The method facilitated a clinical pharmacokinetic study after oral administration of a single dose of matrine soft gelatin capsules (100, 200 and 400mg) in a three-period crossover design."( Matrine determination and pharmacokinetics in human plasma using LC/MS/MS.
Chen, WL; Chu, NN; Li, XN; Liu, GY; Xu, HR; Yu, C; Zhang, XL, 2009
)
0.35
"The aim of this study was to investigate the pharmacokinetic behavior of huperzine A (Hup A) in plasma and cerebrospinal fluid (CSF) after intranasal administration (0."( Pharmacokinetic behavior of huperzine A in plasma and cerebrospinal fluid after intranasal administration in rats.
Chen, G; Wang, Q, 2009
)
0.88
" Pharmacokinetic parameters, including Cmax, AUC0-72 h and AUC0-∞ were calculated."( Phase I study on the pharmacokinetics and tolerance of ZT-1, a prodrug of huperzine A, for the treatment of Alzheimer's disease.
Gui, YZ; Hong, Z; Jia, JY; Liu, GY; Liu, Y; Yu, C; Zhao, QH; Zhu, DY, 2013
)
0.62
"Our preliminary results show that huperzine A, an acetylcholinesterase inhibitor used to treat Alzheimer's disease (AD) patients in China, exhibits different pharmacokinetic features in elderly and young healthy subjects."( Population pharmacokinetic modeling and simulation of huperzine A in elderly Chinese subjects.
Hu, CY; Jia, JY; Li, XN; Liu, GY; Liu, Y; Lu, C; Qu, Y; Sheng, L; Wang, HY; Wang, WL; Wang, YJ; Xu, HR; Yan, J; Yu, C; Zhang, MQ, 2016
)
0.96
"A total of 341 serum huperzine A concentration records was obtained from 2 completed clinical trials (14 elderly healthy subjects in a phase I pharmacokinetic study; 35 elderly AD patients in a phase II study)."( Population pharmacokinetic modeling and simulation of huperzine A in elderly Chinese subjects.
Hu, CY; Jia, JY; Li, XN; Liu, GY; Liu, Y; Lu, C; Qu, Y; Sheng, L; Wang, HY; Wang, WL; Wang, YJ; Xu, HR; Yan, J; Yu, C; Zhang, MQ, 2016
)
1
" The optimized hup A-M-TPISG formulation was further evaluated by in vitro release and in vivo pharmacokinetic studies via microdialysis."( A Nasal Temperature and pH Dual-Responsive In Situ Gel Delivery System Based on Microemulsion of Huperzine A: Formulation, Evaluation, and In Vivo Pharmacokinetic Study.
Chen, S; Chen, Y; Cheng, G; Fang, W; Gao, S; Hu, R; Lu, W; Nie, X; Shen, Q; Sun, C; Wang, B; Xia, H, 2019
)
0.73
" This study aimed to prepare nanoemulsions (NEs) of HupA to investigate their potential "nose-to-brain" pathways and to evaluate their pharmacokinetic and brain-targeting parameters."( Investigation of the "Nose-to-Brain" Pathways in Intranasal HupA Nanoemulsions and Evaluation of Their in vivo Pharmacokinetics and Brain-Targeting Ability.
Ding, Z; Jiang, Y; Yu, Q, 2022
)
0.72
" Immunohistochemistry, pharmacokinetic and targeting index analyses were performed to investigate the in vivo effects of HupA-NE and Lf-HupA-NE."( Investigation of the "Nose-to-Brain" Pathways in Intranasal HupA Nanoemulsions and Evaluation of Their in vivo Pharmacokinetics and Brain-Targeting Ability.
Ding, Z; Jiang, Y; Yu, Q, 2022
)
0.72
" The findings of this study showed that NEs (especially Lf-HupA-NE) had better pharmacokinetic profiles and a better nose-to-brain drug transport efficiency than free HupA."( Investigation of the "Nose-to-Brain" Pathways in Intranasal HupA Nanoemulsions and Evaluation of Their in vivo Pharmacokinetics and Brain-Targeting Ability.
Ding, Z; Jiang, Y; Yu, Q, 2022
)
0.72

Bioavailability

Huperzine A (hup A) is a reversible and highly selective second-generation acetylcholine esterase (AchE) inhibitor for treating Alzheimer's disease (AD) But it suffers from low bioavailability in the brain.

ExcerptReferenceRelevance
" The results showed that huperzine A had high bioavailability and more selective inhibition on AChE activity in cortex and hippocampus."( Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities.
Cheng, DH; Tang, XC, 1998
)
0.91
" The relative bioavailability of huperzine A microspheres over a period of 14 days was 94."( Preparation and in vivo evaluation of huperzine A-loaded PLGA microspheres.
Fu, XD; Gao, YL; Ping, QN; Ren, T, 2005
)
0.88
"Huperzine A (hup A), extracted from the Chinese medicinal plant Huperzia serrata, is a reversible and highly selective second-generation acetylcholine esterase (AchE) inhibitor for treating Alzheimer's disease (AD), but it suffers from low bioavailability in the brain."( A Nasal Temperature and pH Dual-Responsive In Situ Gel Delivery System Based on Microemulsion of Huperzine A: Formulation, Evaluation, and In Vivo Pharmacokinetic Study.
Chen, S; Chen, Y; Cheng, G; Fang, W; Gao, S; Hu, R; Lu, W; Nie, X; Shen, Q; Sun, C; Wang, B; Xia, H, 2019
)
2.17
"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
"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

Dosage Studied

Huperzine A's permeability characteristics pave the way to the development of its oral extended release dosage form. The improving effects of huperZine A exhibited a bell-shaped dose-response curve. The effect of hSuperZine on memory impairments exhibited an inverted U-shapeddose-response pattern.

ExcerptRelevanceReference
" The improving effects of huperzine A exhibited a bell-shaped dose-response curve."( Huperzine A reverses scopolamine- and muscimol-induced memory deficits in chick.
Gao, Y; Guan, LC; Kuang, PZ; Tang, XC, 2000
)
2.05
" The effect of huperzine A on memory impairments exhibited an inverted U-shaped dose-response pattern."( Effect of huperzine A on working memory in reserpine- or yohimbine-treated monkeys.
Cai, JX; Ou, LY; Tang, XC, 2001
)
1.07
" The distributions of Hup A into rat brain tissues following intranasal dosing were compared with those after intravenous and intragastric dosing by tissue homogeneization."( [Preparation of huperzine A nasal in situ gel and evaluation of its brain targeting following intranasal administration].
Chen, QH; Dong, WX; Tao, T; Yue, P; Zhao, Y, 2006
)
0.68
" Tonic-clonic seizures were noticed, but only in highly dosed animals."( Huperzine induces alteration in oxidative balance and antioxidants in a guinea pig model.
Bandouchova, H; Drtinova, L; Hrabinova, M; Pikula, J; Pohanka, M; Zemek, F, 2011
)
0.37
" Furthermore, subcutaneous administration of Bis-Mep (10, 100 or 1000 ng/kg) significantly reversed the scopolamine-induced memory deficits in a typical bell-shaped dose-response manner."( Bis(9)-(-)-nor-meptazinol as a novel dual-binding AChEI potently ameliorates scopolamine-induced cognitive deficits in mice.
Chen, HZ; Cui, Y; Ge, XX; Li, J; Liu, T; Qiu, ZB; Wang, H; Xia, Z; Xie, Q; Xu, J; Xu, JR; Zhang, WW, 2013
)
0.39
" Huperzine A's permeability characteristics pave the way to the development of its oral extended release dosage form."( Transepithelial transport of a natural cholinesterase inhibitor, huperzine A, along the gastrointestinal tract: the role of ionization on absorption mechanism.
Burshtein, G; Friedman, M; Greenberg, S; Hoffman, A, 2013
)
1.54
" The existing dosage of HupA lacks brain selectivity and can cause serious side effects in the gastrointestinal and peripheral cholinergic systems."( The Optimization Design Of Lactoferrin Loaded HupA Nanoemulsion For Targeted Drug Transport Via Intranasal Route.
Ding, Z; Han, T; Jiang, Y; Liu, C; Zhai, W; Zhuang, N, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Occurs in Manufacturing (26 Product(s))

Product Categories

Product CategoryProducts
Active Lifestyle & Fitness22
Vitamins & Supplements2
Weight Management2

Products

ProductBrandCategoryCompounds Matched from IngredientsDate Retrieved
ABE Ultimate Pre-Workout - 30 Servings Baddy Berry -- 13.75 ozABEActive Lifestyle & FitnessBeta-Alanine, Caffeine Anhydrous, Choline, Huperzine A, Niacin, Taurine, Vitamin B122024-11-29 10:47:42
ABE Ultimate Pre-Workout - 30 Servings Blue Razz -- 13.75 ozABEActive Lifestyle & FitnessBeta-Alanine, Caffeine Anhydrous, Choline, Huperzine A, Niacin, Taurine, Vitamin B122024-11-29 10:47:42
ABE Ultimate Pre-Workout - 30 Servings Red Hawaiian -- 13.75 ozABEActive Lifestyle & FitnessBeta-Alanine, Caffeine Anhydrous, Choline, Huperzine A, Niacin, Taurine, Vitamin B122024-11-29 10:47:42
ABE Ultimate Pre-Workout - 30 Servings Sour Gummy Bear -- 13.75 ozABEActive Lifestyle & FitnessBeta-Alanine, Caffeine Anhydrous, Choline, Huperzine A, Niacin, Taurine, Vitamin B122024-11-29 10:47:42
Amazing Muscle Max Boost- Advanced Pre-Workout Formula Cherry Lemonade -- 60 ServingsAmazing MuscleActive Lifestyle & FitnessCaffeine Anhydrous, Folic Acid, L-Glutamine, Huperzine A, N-Acetyl-L-Tyrosine, Niacin, Vitamin B6, Vitamin B12, Vitamin B62024-11-29 10:47:42
Amazing Muscle Max Boost- Advanced Pre-Workout Formula Fruit Punch -- 60 ServingsAmazing MuscleActive Lifestyle & FitnessCaffeine Anhydrous, Folic Acid, L-Glutamine, Huperzine A, N-Acetyl-L-Tyrosine, Niacin, Vitamin B6, Vitamin B12, Vitamin B62024-11-29 10:47:42
Amazing Muscle Pre Boost Extreme- Pre-Workout with Caffeine Watermelon -- 20 ServingsAmazing MuscleActive Lifestyle & FitnessBeta-Alanine, Betaine Anhydrous, Caffeine Anhydrous, L-Citrulline Malate, Huperzine A, L-Arginine Alpha Ketoglutarate, N-Acetyl L-Tyrosine, Taurine2024-11-29 10:47:42
Bear Balanced Creatine Gummies Blueberry -- 90 GummiesBear BalancedActive Lifestyle & FitnessHuperzine A2024-11-29 10:47:42
Bear Balanced Creatine Gummies Peach Mango -- 90 GummiesBear BalancedActive Lifestyle & FitnessHuperzine A, Vitamin B122024-11-29 10:47:42
Bear Balanced Creatine Gummies Watermelon Burst -- 90 GummiesBear BalancedActive Lifestyle & FitnessHuperzine A, Vitamin B122024-11-29 10:47:42
Evlution Nutrition ENGN Focus Pre-Workout Engine Watermelon -- 9.52 oz - 30 ServingsEvlution NutritionActive Lifestyle & FitnessBeta-Alanine, Betaine Anhydrous, Caffeine Anhydrous, Chloride, Choline, Folate, Huperzine A, N-Acetyl L-Tyrosine, Vitamin B1, Vitamin B122024-11-29 10:47:42
Havasu Nutrition NeuroIgnite™ -- 30 CapsulesHavasu NutritionVitamins & SupplementsDMAE, Huperzine A2024-11-29 10:47:42
MuscleTech Burn iQ Smart Thermo - 50 servings Mango Chili Lime -- 7.58 ozMuscleTechActive Lifestyle & Fitness Citric acid, acesulfame-potassium, acesulfame-potassium, beta-carotene, Citric acid, Huperzine A, Vitamin B6, Taurine, sucralose, Vitamin B12, Vitamin B62024-11-29 10:47:42
MuscleTech Burn iQ Smart Thermo - 50 servings Sweet Heat -- 7.58 ozMuscleTechActive Lifestyle & Fitnesscitric acid, citric acid, Huperzine A, Malic acid, Vitamin B6, Taurine, sucralose, Vitamin B12, Vitamin B62024-11-29 10:47:42
MuscleTech EuphoriQ Pre-Workout - 20 Servings Boogieman Punch -- 12.06 ozMuscleTechActive Lifestyle & Fitness Citric acid, acesulfame-potassium, acesulfame-potassium, Beta-alanine, Betaine anhydrous, Choline, Citric acid, Huperzine A, malic acid, Vitamin B6, Taurine, sucralose, Vitamin B12, Vitamin B62024-11-29 10:47:42
MuscleTech EuphoriQ Pre-Workout - 20 Servings Icy Snow Cone -- 11.99 ozMuscleTechActive Lifestyle & Fitness Citric acid, Beta-alanine, beta-carotene, Betaine anhydrous, Choline, Citric acid, Huperzine A, malic acid, Vitamin B6, rebaudioside A, Taurine, sucralose, Vitamin B12, Vitamin B62024-11-29 10:47:42
MuscleTech EuphoriQ Pre-Workout - 20 Servings Watermelon Candy -- 12.06 ozMuscleTechActive Lifestyle & Fitness Citric acid, acesulfame-potassium, acesulfame-potassium, Beta-alanine, Betaine anhydrous, Choline, Citric acid, Huperzine A, malic acid, Vitamin B6, Taurine, sucralose, Vitamin B12, Vitamin B62024-11-29 10:47:42
MuscleTech EuphoriQ Pre-Workout - 20 Servings Yuzu Lemonade -- 11.99 ozMuscleTechActive Lifestyle & Fitness Citric acid, acesulfame-potassium, acesulfame-potassium, Beta-alanine, beta-carotene, Betaine anhydrous, Choline, Citric acid, Huperzine A, malic acid, Vitamin B6, Taurine, sucralose, Vitamin B12, Vitamin B62024-11-29 10:47:42
Natrol Memory Complex -- 60 TabletsNatrolVitamins & Supplementsdicalcium phosphate, Folate, glycerin, Huperzine A, Microcrystalline cellulose, maltodextrin, methylcellulose, Vitamin B3, Phosphorus, Vitamin B6, stearic acid, Thiamin, Vitamin B12, Vitamin B62024-11-29 10:47:42
Source Naturals HGH Surge -- 150 TabletsSource NaturalsActive Lifestyle & Fitness5-HTP, Acetyl L-Carnitine, Chromium, DMAE, GABA, L-Glutamine, Glycine, Huperzine A, microcrystalline cellulose, Niacin, Ornithine Ketoglutarate, stearic acid2024-11-29 10:47:42
Titan Nutrition Enlite Mai Tai -- 30 ServingsTitan NutritionWeight ManagementVitamin C, Chromium, DMAE, Huperzine A, malic acid, N-Acetyl L-Tyrosine, Niacin, Vitamin B6, L-Taurine, sucralose, Vitamin B12, Vitamin B62024-11-29 10:47:42
Titan Nutrition Enlite Peach Sangria -- 30 ServingsTitan NutritionWeight ManagementVitamin C, Chromium, DMAE, Huperzine A, malic acid, N-Acetyl L-Tyrosine, Niacin, Vitamin B6, L-Taurine, sucralose, Vitamin B12, Vitamin B62024-11-29 10:47:42
Titan Nutrition Kickin Pineapple Mango -- 25 ServingsTitan NutritionActive Lifestyle & Fitnesscitric acid, Beta-Alanine, Betaine Anhydrous, citric acid, Dimethylethanolamine, Huperzine A, malic acid, N-Acetyl L-Tyrosine, Taurine2024-11-29 10:47:42
Titan Nutrition Kickin Pink Lemonade -- 25 ServingsTitan NutritionActive Lifestyle & Fitnesscitric acid, Beta-Alanine, Betaine Anhydrous, citric acid, Dimethylethanolamine, Huperzine A, malic acid, N-Acetyl L-Tyrosine, Taurine2024-11-29 10:47:42
Titan Nutrition Pump Cherry Luau -- 20 ServingsTitan NutritionActive Lifestyle & Fitness Citric acid, Vitamin C, Betaine Anhydrous, Citric acid, Huperzine A, malic acid, Vitamin B122024-11-29 10:47:42
Type Zero Clean Phosphatidyl Serine + -- 400 mg - 90 CapsulesType ZeroActive Lifestyle & Fitnessdicalcium phosphate, cellulose, Huperzine A2024-11-29 10:47:42

Roles (4)

RoleDescription
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.
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
plant metaboliteAny eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms.
nootropic agentAny compound that improves mental functions such as cognition, memory, intelligence, motivation, attention, and concentration.
[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
quinolone
sesquiterpene alkaloid
pyridone
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
organic heterotricyclic compoundAn organic tricyclic compound in which at least one of the rings of the tricyclic skeleton contains one or more heteroatoms.
[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]

Protein Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency15.03210.001310.157742.8575AID1259253; AID1259255; AID1259256
acetylcholinesteraseHomo sapiens (human)Potency0.36470.002541.796015,848.9004AID1347395; AID1347397; AID1347398; AID1347399
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[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)
AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki1.17430.00000.76714.3000AID1796454; AID1796488
CholinesteraseHomo sapiens (human)IC50 (µMol)4.42880.00001.559910.0000AID1796478; AID1796482; AID1796572; AID1801945
CholinesteraseHomo sapiens (human)Ki0.52350.00001.51739.7300AID1796481
AcetylcholinesteraseMus musculus (house mouse)Ki0.00460.00001.42829.3000AID1800423
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)4.42880.00000.933210.0000AID1796478; AID1796482; AID1796572; AID1801945
AcetylcholinesteraseHomo sapiens (human)Ki0.35050.00001.27869.7300AID1796481; AID1800423
AcetylcholinesteraseRattus norvegicus (Norway rat)IC50 (µMol)35.13620.00020.52597.2000AID1796569
AcetylcholinesteraseRattus norvegicus (Norway rat)Ki0.11100.00021.640110.0000AID1796454
Chain A, AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki0.25000.25000.25000.2500AID977610
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50 (µMol)8.08500.00000.94539.9400AID1666849; AID1781505
CholinesteraseHomo sapiens (human)IC50 (µMol)5,050.00000.00001.559910.0000AID1537270; AID1862259
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.12000.00011.753610.0000AID1495954
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)2.12260.00000.933210.0000AID1273850; AID1386641; AID1537269; AID1639003; AID1862258
Acetylcholinesterase Bos taurus (cattle)IC50 (µMol)0.10000.00000.61068.7000AID1697408
CholinesteraseCanis lupus familiaris (dog)IC50 (µMol)10,000.00006.27006.27006.2700AID1666848
AcetylcholinesteraseRattus norvegicus (Norway rat)IC50 (µMol)0.09550.00020.52597.2000AID1319286; AID1347958; AID1495954; AID1682335
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC50 (µMol)49.07670.00041.48119.8700AID1347959; AID1495955; AID1682163
[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)Kd0.01700.00801.77505.3000AID1756683
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
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)
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)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (36)

Processvia Protein(s)Taxonomy
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
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 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)
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)
acetylcholinesterase activityCholinesteraseCanis lupus familiaris (dog)
cholinesterase activityCholinesteraseCanis lupus familiaris (dog)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
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)
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 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 regionCholinesteraseCanis lupus familiaris (dog)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (121)

Assay IDTitleYearJournalArticle
AID1796569Enzyme Inhibition Assay from Article 10.1021/jm0496178: \\Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.\\2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.
AID1796454Enzyme Inhibition Assay from Article 10.1021/ja021111w: \\Acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity.\\2003Journal of the American Chemical Society, Jan-15, Volume: 125, Issue:2
Acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity.
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.
AID1800423Assay of Substrate Hydrolysis from Article 10.1021/bi401043w: \\The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.\\2013Biochemistry, Oct-22, Volume: 52, Issue:42
The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.
AID1796478Enzyme Inhibition Assay from Article 10.1021/jm0496741: \\Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.\\2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.
AID1796488Enzyme Inhibition Assay from Article 10.1021/bi020151+: \\X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement.\\2002Biochemistry, Sep-03, Volume: 41, Issue:35
X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement.
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.
AID1796481Enzyme Inhibition Assay from Article 10.1021/jm060257t: \\Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.\\2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.
AID1801945AChE and BuChE Inhibition Assay from Article 10.1016/j.bioorg.2016.07.013: \\Design, synthesis and biological evaluation of coumarin derivatives as novel acetylcholinesterase inhibitors that attenuate H2O2-induced apoptosis in SH-SY5Y cells.\\2016Bioorganic chemistry, 10, Volume: 68Design, synthesis and biological evaluation of coumarin derivatives as novel acetylcholinesterase inhibitors that attenuate H2O2-induced apoptosis in SH-SY5Y cells.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC 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.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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).
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.
AID1682151Neuroprotective activity against Bay-K8644-induced calcium mobilization in rat forebrain derived neurons assessed as calcium elevation at 100 nM (Rvb = 521 nM)2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1756684Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as on rate constant at 298.15 K by surface plasmon resonance assay2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
AID1682157In vivo inhibition of acetylcholinesterase in rat at 0.066 micromol/kg, icv relative to control2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
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.
AID1682152Neuroprotective activity against glutamate-induced calcium mobilization in rat forebrain derived neurons assessed as calcium elevation at 100 nM (Rvb = 811 nM)2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1347960Selectivity index, ratio of IC50 for BuChE in rat serum to IC50 for AChE in rat cortex homogenate2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1319289Selectivity index, ratio of IC50 for rat serum BuChE to IC50 for rat cortex AChE2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents.
AID1666848Inhibition of dog serum BChE using butrylthiocholine iodide as substrate by spectrophotometry based Ellman's method2020Bioorganic & medicinal chemistry letters, 03-15, Volume: 30, Issue:6
Design, synthesis and evaluation of new 4-arylthiazole-2-amine derivatives as acetylcholinesterase inhibitors.
AID1682148Neuroprotective activity against NMDA-induced cell death in rat neurons assessed as cell survival pretreated for 45 mins followed by NMDA stimulation and measured after 30 mins by MTT assay (Rvb = 35%)2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1682158Potency index, ratio of in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by tacrine to in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by compound2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1862259Inhibition of BuChE (unknown origin) using butyrylthiocholine iodide as substrate by DTNB reagent based Ellman's method2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and evaluation of 2-(2-oxoethyl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors.
AID1495953Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.
AID1386641Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by Ellman's method2018Journal of natural products, 09-28, Volume: 81, Issue:9
Colocynthenins A-D, Ring-A seco-Cucurbitane Triterpenoids from the Fruits of Citrullus colocynthis.
AID1682162In vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex at 1 micromol/kg, IG administered once daily for 8 days and measured 30 mins post 8th dose by spectrophotometric method relative to control2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1862258Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by DTNB reagent based Ellman's method2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Design, synthesis and evaluation of 2-(2-oxoethyl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors.
AID1273850Inhibition of human acetylcholinesterase after 30 mins by microplate reader-based Ellman's method2015Journal of natural products, Dec-24, Volume: 78, Issue:12
Avertoxins A-D, Prenyl Asteltoxin Derivatives from Aspergillus versicolor Y10, an Endophytic Fungus of Huperzia serrata.
AID1319304Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 100 uM measured after 24 hrs by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents.
AID1682150Displacement of [3H]MK-801 from Guinea pig synaptosomal plasma membrane NMDA receptor2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1682156Potency index, ratio of in vivo inhibition of acetylcholinesterase in rat by tacrine to in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by compound2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1756683Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as dissociation constant at 298.15 K by surface plasmon resonance assay2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
AID1756685Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as off rate constant at 298.15 K by surface plasmon resonance assay2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
AID1666849Inhibition of Electric eel AChE using acetylcholine iodide as substrate by spectrophotometry based Ellman's method2020Bioorganic & medicinal chemistry letters, 03-15, Volume: 30, Issue:6
Design, synthesis and evaluation of new 4-arylthiazole-2-amine derivatives as acetylcholinesterase inhibitors.
AID1682153Neuroprotective activity against glutamate-induced cell death in rat forebrain derived neurons assessed as neuron death at 100 nM incubated for 45 mins (Rvb = 55%)2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
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.
AID1319287Inhibition of rat serum BuChE using butyrylthiocholine as substrate measured after 20 mins by Ellman's method2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents.
AID1319286Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate measured after 20 mins by Ellman's method2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents.
AID1781504Inhibition of equine serum BuChE at 100 uM using butylthiocholine chloride as substrate incubated for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method2021Journal of natural products, 08-27, Volume: 84, Issue:8
Pd-Catalyzed Direct Diversification of Natural Anti-Alzheimer's Disease Drug: Synthesis and Biological Evaluation of
AID1697408Inhibition of bovine erythrocytes AChE using acetylthiocholine iodide as substrate incubated for 15 to 20 mins by Ellman's methods
AID1682146Toxicity in male rat2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
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.
AID1682163Inhibition of rat cortex homogenate BuChE by spectrophotometric method2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1347958Inhibition of AChE in rat cortex homogenate using acetylthiocholine iodide as substrate after 20 mins by Ellman's method2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1639003Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate after 5 mins by spectrophotometric analysis2019Journal of natural products, 04-26, Volume: 82, Issue:4
Bialternacins A-F, Aromatic Polyketide Dimers from an Endophytic Alternaria sp.
AID1781505Inhibition of electric eel AChE using acetylthiocholine chloride as a substrate incubated for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method2021Journal of natural products, 08-27, Volume: 84, Issue:8
Pd-Catalyzed Direct Diversification of Natural Anti-Alzheimer's Disease Drug: Synthesis and Biological Evaluation of
AID1495955Inhibition of rat serum BChE using butyrylthiocholine iodide as substrate after 20 mins by by Ellman's method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.
AID1300690Inhibition of ACAT in human monocyte derived macrophages assessed as reduction in foam cell formation by measuring acetyl LDL-induced cholesterol ester accumulation at 30 uM after 24 hrs in presence of cholesteryl-[3H]oleate2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Serralongamines B-D, three new Lycopodium alkaloids from Lycopodium serratum var. longipetiolatum, and their inhibitory effects on foam cell formation in macrophages.
AID1682147Toxicity in female rat2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1319290Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity preincubated for 10 mins followed by AAPH challenge measured every min for 180 mins by ORAC-FL assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents.
AID1682149Displacement of [3H]TCP from NMDA receptor in Guinea pig synaptosomal plasma membrane2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1682335Inhibition of rat cortex homogenate acetylcholinesterase by spectrophotometric method2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1319303Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 10 and 30 uM measured after 24 hrs by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents.
AID1495954Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 20 mins by by Ellman's method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.
AID1347959Inhibition of BuChE in rat serum using butyrylthiocholine iodide as substrate after 20 mins by Ellman's method2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.
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.
AID1682159Potency index, ratio of in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by donepezil to in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by compound2020Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
Pyridine alkaloids with activity in the central nervous system.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC 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.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB1997Nature structural biology, Jan, Volume: 4, Issue:1
Structure of acetylcholinesterase complexed with the nootropic alkaloid, (-)-huperzine A.
AID1811Experimentally measured binding affinity data derived from PDB1997Nature structural biology, Jan, Volume: 4, Issue:1
Structure of acetylcholinesterase complexed with the nootropic alkaloid, (-)-huperzine A.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (472)

TimeframeStudies, This Drug (%)All Drugs %
pre-199012 (2.54)18.7374
1990's57 (12.08)18.2507
2000's182 (38.56)29.6817
2010's160 (33.90)24.3611
2020's61 (12.92)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 50.20

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 Index50.20 (24.57)
Research Supply Index6.18 (2.92)
Research Growth Index5.28 (4.65)
Search Engine Demand Index157.19 (26.88)
Search Engine Supply Index3.88 (0.95)

This Compound (50.20)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials15 (3.21%)5.53%
Trials0 (0.00%)5.53%
Reviews58 (12.39%)6.00%
Reviews1 (4.17%)6.00%
Case Studies2 (0.43%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other393 (83.97%)84.16%
Other23 (95.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (19)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Evaluation of Three Potential CNS Pretreatments for Soman Exposure - Huperzine A, Donepezil, and Galantamine - on Human Performance [NCT01194336]84 participants (Actual)Observational2012-02-29Completed
Effects of Huperzine A on Presbycusis-related Subjective Tinnitus and Cognitive Impairment [NCT03101722]60 participants (Anticipated)Interventional2017-05-15Enrolling by invitation
An Open-label, Three-period, Crossover Study in Healthy Volunteers to Evaluate the Relative Bioavailability of Two Different Release Rate Controlled Release Formulations of Huperzine A (0.4mg)Compared to the Equivalent Dose of an Immediate Release Formula [NCT01136551]8 participants (Anticipated)Interventional2010-09-30Not yet recruiting
A Multi-Center, Randomized, Double-Blind, Double-Dummy, Placebo- and Active-Controlled, Study to Evaluate the Safety and Efficacy of Huperzine A Sustained-Release Tablets in Patients With Mild to Moderate Alzheimer's Disease [NCT01282619]Phase 2/Phase 3390 participants (Anticipated)Interventional2010-05-31Recruiting
Huperzine for Cognitive and Functional Impairment in Schizophrenia [NCT00963846]Phase 256 participants (Actual)Interventional2010-03-31Completed
Huperzine-A for Cognitive Dysfunction and Functional Status in Schizophrenia [NCT01012830]Phase 415 participants (Anticipated)Interventional2009-12-31Not yet recruiting
Rivastigmine and Huperzine A as Treatments for Cocaine Dependence [NCT01030692]Phase 172 participants (Actual)Interventional2009-01-31Completed
Early Diagnosis and Early Treatment of Alzheimer's Disease Based on Senile Plaque Imaging [NCT02931136]Phase 4300 participants (Anticipated)Interventional2019-11-30Not yet recruiting
A Multi-center, Randomized, Double-blinded, Placebo-controlled Study of Huperzine A Injection in Reducing Postoperative Delirium in Elderly Patients Undergoing Non-cardiac Surgery [NCT05242419]40 participants (Anticipated)Interventional2022-06-10Recruiting
Effect of Huperzine A on Cognitive Function and Perception of Effort During Exercise [NCT03445104]Early Phase 115 participants (Actual)Interventional2018-01-16Completed
Brain Single Photon Emission Computed Tomography and Quantitative Electroencephalography In Former NFL Players: A Single-Site Exploratory Pilot Study [NCT01515839]100 participants (Actual)Interventional2009-05-31Completed
A Multi-Center, Double-Blind, Placebo-Controlled Therapeutic Trial to Determine Whether Natural Huperzine A Improves Cognitive Function [NCT00083590]Phase 2150 participants (Anticipated)Interventional2004-04-30Completed
The Effect of Huperzine A Injection on Postoperative Cognitive Dysfunction in Patients With Aneurysmal Subarachnoid Hemorrhage: a Pilot Study [NCT05560373]Phase 460 participants (Anticipated)Interventional2022-09-30Not yet recruiting
Evaluation of Safety and Efficacy of BIS-001-ER for the Treatment of Adult Focal Impaired Awareness Seizures [NCT03474770]Phase 1/Phase 216 participants (Anticipated)Interventional2018-04-10Active, not recruiting
RENAISSANCE Study: A Phase 2, Multicenter, Open Label Safety and Tolerability Study of SPN-817 in Adult Patients With Treatment Resistant Epilepsy [NCT05518578]Phase 235 participants (Anticipated)Interventional2023-02-07Recruiting
Huperzine A for the Treatment of Cognitive, Mood, and Functional Deficits After Moderate and Severe TBI [NCT01676311]Phase 214 participants (Actual)Interventional2013-12-31Terminated(stopped due to Insufficient accrual rate: 14 participants enrolled (target of 30).)
A Single-Center, Randomized, Open-label, Multiple-Dose, Single-Sequence Crossover Study, Evaluating the Safety and Relative Bioavailability of Three SPN-817 Treatments (A, B and C) in Healthy Adult Subjects [NCT05102552]Early Phase 130 participants (Actual)Interventional2021-10-19Completed
Evaluation of the Bioavailability, Safety, and Tolerability of BIS-001 ER Following Multiple Dose Administration in Healthy Subjects [NCT03156439]Phase 18 participants (Actual)Interventional2017-05-22Completed
A Randomized, Controlled, Single-center Clinical Study of Huperzine A in the Treatment of Brain Injury in Patients With Hypertensive Cerebral Hemorrhage [NCT04509323]Phase 420 participants (Anticipated)Interventional2020-08-03Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01676311 (5) [back to overview]Number of Participants Who Experienced Post-traumatic Seizure During 12-week Treatment Window
NCT01676311 (5) [back to overview]Amplitude of Event Related Potentials (ERPs) P50 and P300
NCT01676311 (5) [back to overview]California Verbal Learning Test- 2nd Edition (CVLT-II): Learning and Memory
NCT01676311 (5) [back to overview]Latency of Event Related Potentials (ERPs) P50 and P300
NCT01676311 (5) [back to overview]Number of Participants With Self-reported Side Effects During 12-week Treatment Window

Number of Participants Who Experienced Post-traumatic Seizure During 12-week Treatment Window

To determine whether Huperzine A changes the prevalence of post-traumatic seizure after moderate and severe TBI as compared to placebo at 12 weeks post-enrollment (immediate seizures prevalence). (NCT01676311)
Timeframe: Baseline and weekly for 12 weeks.

InterventionParticipants (Count of Participants)
Huperzine A2
Placebo1

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California Verbal Learning Test- 2nd Edition (CVLT-II): Learning and Memory

"Measure of learning and memory function. Three indices of the CVLT-II were calculated. The full name, abbreviated name, and the minimum and maximum possible scores of each index are indicated below:~California Verbal Learning Test- 2nd Edition- Total Learning [CVLT-II-TL] (Minimum score=0; Maximum score= 80)~California Verbal Learning Test- 2nd Edition- Short delay free recall [CVLT-II-SDFR] (Minimum score=0; Maximum score=16)~California Verbal Learning Test- 2nd Edition- Long delay free recall [CVLT-II-LDFR] (Minimum score=0; Maximum score=16)~High scores are indicative of greater memory and learning for each index (i.e. better outcome)." (NCT01676311)
Timeframe: Baseline, 6 weeks, 12 weeks, 24 weeks and at 52 weeks.

,
Interventionscore on a scale (Mean)
CVLT-II-TL - BaselineCVLT-II-TL - Week 6CVLT-II-TL - Week 12CVLT-II-TL - Week 24CVLT-II-TL - Week 52CVLT-II-SDFR - BaselineCVLT-II-SDFR - Week 6CVLT-II-SDFR - Week 12CVLT-II-SDFR - Week 24CVLT-II-SDFR - Week 52CVLT-II-LDFR - BaselineCVLT-II-LDFR - Week 6CVLT-II-LDFR - Week 12CVLT-II-LDFR - Week 24CVLT-II-LDFR - Week 52
Huperzine A28.5731.4338.2933.2937.433.864.146.294.865.435.004.436.004.296.14
Placebo34.4045.0049.6044.6049.405.807.8310.4010.009.807.008.3310.008.4010.00

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Number of Participants With Self-reported Side Effects During 12-week Treatment Window

To evaluate the safety and tolerability of Huperzine A in this patient population as compared to placebo the frequency of self-reported side effects during the 12-week treatment window were grouped categorically by system (behavioral, cardiac-respiratory, dermatological,gastrointestinal, genitourinary/neurological, hematological, musculoskeletal, neurological). (NCT01676311)
Timeframe: Baseline and weekly for 12 weeks.

,
InterventionParticipants (Count of Participants)
Behavioral side effectsCardiac-respiratory side effectsDematological side effectsGastrointestinal side effectsGenitourinary/neurological side effectsHematological side effectsMusculoskeletal side effectsNeurological side effects
Huperzine A56231637
Placebo44011625

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