lipocrine profile

lipocrine: anti-Alzheimer's drug; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	11375002
CHEMBL ID	194823
SCHEMBL ID	14341601
MeSH ID	M0535543

Synonym
n-{3-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]propyl}-5-(1,2-dithiolan-3-yl)pentanamide
bdbm10512
tacrine-lipoic acid hybrid 7
chembl194823 ,
n-[3-[(6-chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]propyl]-5-(dithiolan-3-yl)pentanamide
lipocrine
rac-lipocrine
SCHEMBL14341601

Excerpt	Reference	Relevance
"Lipocrine has been selected as an effective candidate for in vivo investigation because of its multiple biological properties, namely inhibition of AChE and BChE activities, inhibition of AChE-induced Aβ aggregation, and ability to protect cells against reactive oxygen species. "	( Reversible human serum albumin binding of lipocrine: a circular dichroism study. Bertucci, C; De Simone, A; Pistolozzi, M; Rosini, M, 2011)	2.08

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Amyloid-beta precursor protein	Homo sapiens (human)	IC50 (µMol)	45.0000	0.0005	3.8895	10.0000	AID1395840
Cholinesterase	Homo sapiens (human)	IC50 (µMol)	0.0109	0.0000	1.5599	10.0000	AID1796463; AID241230; AID439595; AID625547
Cholinesterase	Homo sapiens (human)	Ki	0.1550	0.0000	1.5173	9.7300	AID1796463
Acetylcholinesterase	Homo sapiens (human)	IC50 (µMol)	10.0014	0.0000	0.9332	10.0000	AID1127774; AID1127775; AID1395839; AID1796463; AID241200; AID314091; AID314112; AID439594; AID625546
Acetylcholinesterase	Homo sapiens (human)	Ki	0.1550	0.0000	1.2786	9.7300	AID1796463
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
regulation of gene expression	Amyloid-beta precursor protein	Homo sapiens (human)
cognition	Amyloid-beta precursor protein	Homo sapiens (human)
G2/M transition of mitotic cell cycle	Amyloid-beta precursor protein	Homo sapiens (human)
microglial cell activation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of protein phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
suckling behavior	Amyloid-beta precursor protein	Homo sapiens (human)
astrocyte activation involved in immune response	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of translation	Amyloid-beta precursor protein	Homo sapiens (human)
protein phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
intracellular copper ion homeostasis	Amyloid-beta precursor protein	Homo sapiens (human)
endocytosis	Amyloid-beta precursor protein	Homo sapiens (human)
response to oxidative stress	Amyloid-beta precursor protein	Homo sapiens (human)
cell adhesion	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of epidermal growth factor-activated receptor activity	Amyloid-beta precursor protein	Homo sapiens (human)
Notch signaling pathway	Amyloid-beta precursor protein	Homo sapiens (human)
axonogenesis	Amyloid-beta precursor protein	Homo sapiens (human)
learning or memory	Amyloid-beta precursor protein	Homo sapiens (human)
learning	Amyloid-beta precursor protein	Homo sapiens (human)
mating behavior	Amyloid-beta precursor protein	Homo sapiens (human)
locomotory behavior	Amyloid-beta precursor protein	Homo sapiens (human)
axo-dendritic transport	Amyloid-beta precursor protein	Homo sapiens (human)
cholesterol metabolic process	Amyloid-beta precursor protein	Homo sapiens (human)
negative regulation of cell population proliferation	Amyloid-beta precursor protein	Homo sapiens (human)
adult locomotory behavior	Amyloid-beta precursor protein	Homo sapiens (human)
visual learning	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of gene expression	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of gene expression	Amyloid-beta precursor protein	Homo sapiens (human)
negative regulation of gene expression	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycle	Amyloid-beta precursor protein	Homo sapiens (human)
microglia development	Amyloid-beta precursor protein	Homo sapiens (human)
axon midline choice point recognition	Amyloid-beta precursor protein	Homo sapiens (human)
neuron remodeling	Amyloid-beta precursor protein	Homo sapiens (human)
dendrite development	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of Wnt signaling pathway	Amyloid-beta precursor protein	Homo sapiens (human)
extracellular matrix organization	Amyloid-beta precursor protein	Homo sapiens (human)
forebrain development	Amyloid-beta precursor protein	Homo sapiens (human)
neuron projection development	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of chemokine production	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of interleukin-1 beta production	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of interleukin-6 production	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of tumor necrosis factor production	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of multicellular organism growth	Amyloid-beta precursor protein	Homo sapiens (human)
negative regulation of neuron differentiation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of glycolytic process	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of mitotic cell cycle	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of JNK cascade	Amyloid-beta precursor protein	Homo sapiens (human)
astrocyte activation	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of long-term neuronal synaptic plasticity	Amyloid-beta precursor protein	Homo sapiens (human)
collateral sprouting in absence of injury	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of inflammatory response	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of peptidyl-tyrosine phosphorylation	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of synapse structure or activity	Amyloid-beta precursor protein	Homo sapiens (human)
synapse organization	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of calcium-mediated signaling	Amyloid-beta precursor protein	Homo sapiens (human)
neuromuscular process controlling balance	Amyloid-beta precursor protein	Homo sapiens (human)
synaptic assembly at neuromuscular junction	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of protein metabolic process	Amyloid-beta precursor protein	Homo sapiens (human)
neuron apoptotic process	Amyloid-beta precursor protein	Homo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasis	Amyloid-beta precursor protein	Homo sapiens (human)
neuron cellular homeostasis	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Amyloid-beta precursor protein	Homo sapiens (human)
response to interleukin-1	Amyloid-beta precursor protein	Homo sapiens (human)
modulation of excitatory postsynaptic potential	Amyloid-beta precursor protein	Homo sapiens (human)
NMDA selective glutamate receptor signaling pathway	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of spontaneous synaptic transmission	Amyloid-beta precursor protein	Homo sapiens (human)
cytosolic mRNA polyadenylation	Amyloid-beta precursor protein	Homo sapiens (human)
negative regulation of long-term synaptic potentiation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of long-term synaptic potentiation	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transduction	Amyloid-beta precursor protein	Homo sapiens (human)
cellular response to amyloid-beta	Amyloid-beta precursor protein	Homo sapiens (human)
regulation of presynapse assembly	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of amyloid fibril formation	Amyloid-beta precursor protein	Homo sapiens (human)
amyloid fibril formation	Amyloid-beta precursor protein	Homo sapiens (human)
neuron projection maintenance	Amyloid-beta precursor protein	Homo sapiens (human)
positive regulation of T cell migration	Amyloid-beta precursor protein	Homo sapiens (human)
central nervous system development	Amyloid-beta precursor protein	Homo sapiens (human)
xenobiotic metabolic process	Cholinesterase	Homo sapiens (human)
learning	Cholinesterase	Homo sapiens (human)
negative regulation of cell population proliferation	Cholinesterase	Homo sapiens (human)
neuroblast differentiation	Cholinesterase	Homo sapiens (human)
peptide hormone processing	Cholinesterase	Homo sapiens (human)
response to alkaloid	Cholinesterase	Homo sapiens (human)
cocaine metabolic process	Cholinesterase	Homo sapiens (human)
negative regulation of synaptic transmission	Cholinesterase	Homo sapiens (human)
response to glucocorticoid	Cholinesterase	Homo sapiens (human)
response to folic acid	Cholinesterase	Homo sapiens (human)
choline metabolic process	Cholinesterase	Homo sapiens (human)
acetylcholine catabolic process	Cholinesterase	Homo sapiens (human)
acetylcholine catabolic process in synaptic cleft	Acetylcholinesterase	Homo sapiens (human)
regulation of receptor recycling	Acetylcholinesterase	Homo sapiens (human)
osteoblast development	Acetylcholinesterase	Homo sapiens (human)
acetylcholine catabolic process	Acetylcholinesterase	Homo sapiens (human)
cell adhesion	Acetylcholinesterase	Homo sapiens (human)
nervous system development	Acetylcholinesterase	Homo sapiens (human)
synapse assembly	Acetylcholinesterase	Homo sapiens (human)
receptor internalization	Acetylcholinesterase	Homo sapiens (human)
negative regulation of synaptic transmission, cholinergic	Acetylcholinesterase	Homo sapiens (human)
amyloid precursor protein metabolic process	Acetylcholinesterase	Homo sapiens (human)
positive regulation of protein secretion	Acetylcholinesterase	Homo sapiens (human)
retina development in camera-type eye	Acetylcholinesterase	Homo sapiens (human)
acetylcholine receptor signaling pathway	Acetylcholinesterase	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Acetylcholinesterase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Amyloid-beta precursor protein	Homo sapiens (human)
DNA binding	Amyloid-beta precursor protein	Homo sapiens (human)
serine-type endopeptidase inhibitor activity	Amyloid-beta precursor protein	Homo sapiens (human)
signaling receptor binding	Amyloid-beta precursor protein	Homo sapiens (human)
protein binding	Amyloid-beta precursor protein	Homo sapiens (human)
heparin binding	Amyloid-beta precursor protein	Homo sapiens (human)
enzyme binding	Amyloid-beta precursor protein	Homo sapiens (human)
identical protein binding	Amyloid-beta precursor protein	Homo sapiens (human)
transition metal ion binding	Amyloid-beta precursor protein	Homo sapiens (human)
receptor ligand activity	Amyloid-beta precursor protein	Homo sapiens (human)
PTB domain binding	Amyloid-beta precursor protein	Homo sapiens (human)
protein serine/threonine kinase binding	Amyloid-beta precursor protein	Homo sapiens (human)
signaling receptor activator activity	Amyloid-beta precursor protein	Homo sapiens (human)
amyloid-beta binding	Cholinesterase	Homo sapiens (human)
catalytic activity	Cholinesterase	Homo sapiens (human)
acetylcholinesterase activity	Cholinesterase	Homo sapiens (human)
cholinesterase activity	Cholinesterase	Homo sapiens (human)
protein binding	Cholinesterase	Homo sapiens (human)
hydrolase activity, acting on ester bonds	Cholinesterase	Homo sapiens (human)
enzyme binding	Cholinesterase	Homo sapiens (human)
choline binding	Cholinesterase	Homo sapiens (human)
identical protein binding	Cholinesterase	Homo sapiens (human)
amyloid-beta binding	Acetylcholinesterase	Homo sapiens (human)
acetylcholinesterase activity	Acetylcholinesterase	Homo sapiens (human)
cholinesterase activity	Acetylcholinesterase	Homo sapiens (human)
protein binding	Acetylcholinesterase	Homo sapiens (human)
collagen binding	Acetylcholinesterase	Homo sapiens (human)
hydrolase activity	Acetylcholinesterase	Homo sapiens (human)
serine hydrolase activity	Acetylcholinesterase	Homo sapiens (human)
acetylcholine binding	Acetylcholinesterase	Homo sapiens (human)
protein homodimerization activity	Acetylcholinesterase	Homo sapiens (human)
laminin binding	Acetylcholinesterase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular space	Amyloid-beta precursor protein	Homo sapiens (human)
dendrite	Amyloid-beta precursor protein	Homo sapiens (human)
extracellular region	Amyloid-beta precursor protein	Homo sapiens (human)
extracellular space	Amyloid-beta precursor protein	Homo sapiens (human)
nuclear envelope lumen	Amyloid-beta precursor protein	Homo sapiens (human)
cytoplasm	Amyloid-beta precursor protein	Homo sapiens (human)
mitochondrial inner membrane	Amyloid-beta precursor protein	Homo sapiens (human)
endosome	Amyloid-beta precursor protein	Homo sapiens (human)
early endosome	Amyloid-beta precursor protein	Homo sapiens (human)
endoplasmic reticulum	Amyloid-beta precursor protein	Homo sapiens (human)
endoplasmic reticulum lumen	Amyloid-beta precursor protein	Homo sapiens (human)
smooth endoplasmic reticulum	Amyloid-beta precursor protein	Homo sapiens (human)
Golgi apparatus	Amyloid-beta precursor protein	Homo sapiens (human)
Golgi lumen	Amyloid-beta precursor protein	Homo sapiens (human)
Golgi-associated vesicle	Amyloid-beta precursor protein	Homo sapiens (human)
cytosol	Amyloid-beta precursor protein	Homo sapiens (human)
plasma membrane	Amyloid-beta precursor protein	Homo sapiens (human)
clathrin-coated pit	Amyloid-beta precursor protein	Homo sapiens (human)
cell-cell junction	Amyloid-beta precursor protein	Homo sapiens (human)
synaptic vesicle	Amyloid-beta precursor protein	Homo sapiens (human)
cell surface	Amyloid-beta precursor protein	Homo sapiens (human)
membrane	Amyloid-beta precursor protein	Homo sapiens (human)
COPII-coated ER to Golgi transport vesicle	Amyloid-beta precursor protein	Homo sapiens (human)
axon	Amyloid-beta precursor protein	Homo sapiens (human)
growth cone	Amyloid-beta precursor protein	Homo sapiens (human)
platelet alpha granule lumen	Amyloid-beta precursor protein	Homo sapiens (human)
neuromuscular junction	Amyloid-beta precursor protein	Homo sapiens (human)
endosome lumen	Amyloid-beta precursor protein	Homo sapiens (human)
trans-Golgi network membrane	Amyloid-beta precursor protein	Homo sapiens (human)
ciliary rootlet	Amyloid-beta precursor protein	Homo sapiens (human)
dendritic spine	Amyloid-beta precursor protein	Homo sapiens (human)
dendritic shaft	Amyloid-beta precursor protein	Homo sapiens (human)
perikaryon	Amyloid-beta precursor protein	Homo sapiens (human)
membrane raft	Amyloid-beta precursor protein	Homo sapiens (human)
apical part of cell	Amyloid-beta precursor protein	Homo sapiens (human)
synapse	Amyloid-beta precursor protein	Homo sapiens (human)
perinuclear region of cytoplasm	Amyloid-beta precursor protein	Homo sapiens (human)
presynaptic active zone	Amyloid-beta precursor protein	Homo sapiens (human)
spindle midzone	Amyloid-beta precursor protein	Homo sapiens (human)
recycling endosome	Amyloid-beta precursor protein	Homo sapiens (human)
extracellular exosome	Amyloid-beta precursor protein	Homo sapiens (human)
receptor complex	Amyloid-beta precursor protein	Homo sapiens (human)
early endosome	Amyloid-beta precursor protein	Homo sapiens (human)
membrane raft	Amyloid-beta precursor protein	Homo sapiens (human)
cell surface	Amyloid-beta precursor protein	Homo sapiens (human)
Golgi apparatus	Amyloid-beta precursor protein	Homo sapiens (human)
plasma membrane	Amyloid-beta precursor protein	Homo sapiens (human)
extracellular region	Cholinesterase	Homo sapiens (human)
nuclear envelope lumen	Cholinesterase	Homo sapiens (human)
endoplasmic reticulum lumen	Cholinesterase	Homo sapiens (human)
blood microparticle	Cholinesterase	Homo sapiens (human)
plasma membrane	Cholinesterase	Homo sapiens (human)
extracellular space	Cholinesterase	Homo sapiens (human)
extracellular region	Acetylcholinesterase	Homo sapiens (human)
basement membrane	Acetylcholinesterase	Homo sapiens (human)
extracellular space	Acetylcholinesterase	Homo sapiens (human)
nucleus	Acetylcholinesterase	Homo sapiens (human)
Golgi apparatus	Acetylcholinesterase	Homo sapiens (human)
plasma membrane	Acetylcholinesterase	Homo sapiens (human)
cell surface	Acetylcholinesterase	Homo sapiens (human)
membrane	Acetylcholinesterase	Homo sapiens (human)
neuromuscular junction	Acetylcholinesterase	Homo sapiens (human)
synaptic cleft	Acetylcholinesterase	Homo sapiens (human)
synapse	Acetylcholinesterase	Homo sapiens (human)
perinuclear region of cytoplasm	Acetylcholinesterase	Homo sapiens (human)
side of membrane	Acetylcholinesterase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay ID	Title	Year	Journal	Article
AID625547	Inhibition of human serum recombinant BChE after 20 mins using butyrylthiocholine iodide as a substrate by Ellman's assay	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11	Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
AID314112	Inhibition of human AchE-induced amyloid beta aggregation	2008	Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3	Multi-target-directed ligands to combat neurodegenerative diseases.
AID250075	Percentage increase of intracellular reactive oxygen species in neuronal cells at 0.5 uM	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
AID241230	Inhibitory concentration against human recombinant butyrylcholinesterase	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
AID625546	Inhibition of human serum recombinant AChE after 20 mins using acetylthiocholine iodide as a substrate by Ellman's assay	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11	Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
AID1395873	Antioxidant activity assessed as reduction in oxidative stress	2018	European journal of medicinal chemistry, May-10, Volume: 151	Success stories of natural product-based hybrid molecules for multi-factorial diseases.
AID250066	Percentage increase of intracellular reactive oxygen species in neuronal cells at 5 uM	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
AID250069	Percentage increase of intracellular reactive oxygen species in neuronal cells at 10 uM	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
AID625637	Inhibition of human AChE-induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by thioflavin T based fluorometric assay	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11	Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
AID439594	Inhibition of human recombinant AChE by Ellman's method	2009	Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23	Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.
AID1127775	Inhibition of AChE (unknown origin)-mediated amyloid beta aggregation	2014	Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7	Oxidative stress in Alzheimer's disease: are we connecting the dots?
AID625548	Antioxidant activity in human SH-SY5Y cells assessed as inhibition of tert-butyl hydroperoxide-induced intracellular ROS production at 1 uM after 24 hrs using DCFH-DA by fluorescence assay (Rvb = 82.4 +/- 6.6 %)	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11	Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
AID1127774	Inhibition of AChE (unknown origin)	2014	Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7	Oxidative stress in Alzheimer's disease: are we connecting the dots?
AID439592	Antioxidant activity in human T67 cells assessed as inhibition of tert-butyl hydroperoxide-induced ROS production at 10 uM after 24 hrs by fluorescence assay in presence of 2.5 uM sulforaphane treated for 24 hrs before compound addition	2009	Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23	Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.
AID250064	Percentage increase of intracellular reactive oxygen species in neuronal cells at 0 uM	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
AID1395840	Inhibition of beta amyloid (unknown origin) deposition	2018	European journal of medicinal chemistry, May-10, Volume: 151	Success stories of natural product-based hybrid molecules for multi-factorial diseases.
AID439595	Inhibition of human recombinant BChE by Ellman's method	2009	Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23	Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.
AID625549	Antioxidant activity in human SH-SY5Y cells assessed as inhibition of tert-butyl hydroperoxide-induced intracellular ROS production at 5 uM after 24 hrs using DCFH-DA by fluorescence assay (Rvb = 82.4 +/- 6.6 %)	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11	Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
AID1395839	Inhibition of AChE (unknown origin)	2018	European journal of medicinal chemistry, May-10, Volume: 151	Success stories of natural product-based hybrid molecules for multi-factorial diseases.
AID439593	Inhibition of amyloid beta (1 to 42) self-aggregation assessed as amyloid fibril formation at 10 uM by thioflavin-T based fluorometric assay	2009	Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23	Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.
AID625550	Antioxidant activity in human SH-SY5Y cells assessed as inhibition of tert-butyl hydroperoxide-induced intracellular ROS production at 10 uM after 24 hrs using DCFH-DA by fluorescence assay (Rvb = 82.4 +/- 6.6 %)	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11	Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
AID625634	Antioxidant activity in human SH-SY5Y cells assessed as inhibition of tert-butyl hydroperoxide-induced intracellular ROS production at 50 uM after 24 hrs using DCFH-DA by fluorescence assay (Rvb = 82.4 +/- 6.6 %)	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11	Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
AID250074	Percentage increase of intracellular reactive oxygen species in neuronal cells at 0.1 uM	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
AID314091	Inhibition of human AchE	2008	Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3	Multi-target-directed ligands to combat neurodegenerative diseases.
AID250070	Percentage increase of intracellular reactive oxygen species in neuronal cells at 50 uM	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
AID241200	Inhibitory concentration against human recombinant acetylcholinesterase	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
AID314099	Protection against ROS induced by oxidative stress at 10 uM in neuronal cells	2008	Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3	Multi-target-directed ligands to combat neurodegenerative diseases.
AID250065	Percentage increase of intracellular reactive oxygen species in neuronal cells at 1 uM	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
AID1796463	Enzyme Inhibition Assay from Article 10.1021/jm049112h: \\Rational approach to discover multipotent anti-Alzheimer drugs.\\	2005	Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2	Rational approach to discover multipotent anti-Alzheimer drugs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	5 (50.00)	29.6817
2010's	5 (50.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	5 (50.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (50.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
thioctic acid Thioctic Acid: An octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.	5.09	5	dithiolanes; heterocyclic fatty acid; thia fatty acid	fundamental metabolite; geroprotector
tacrine Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.	5.49	6	acridines; aromatic amine	EC 3.1.1.7 (acetylcholinesterase) inhibitor
benextramine benextramine: RN given refers to parent cpd	3.14	1
donepezil Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group.	3.14	1	aromatic ether; indanones; piperidines; racemate	EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; nootropic agent
fluoxetine Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group.	3.14	1	(trifluoromethyl)benzenes; aromatic ether; secondary amino compound
sulforaphane sulforaphane: from Cardaria draba L.. sulforaphane : An isothiocyanate having a 4-(methylsulfinyl)butyl group attached to the nitrogen.	2.05	1	isothiocyanate; sulfoxide	antineoplastic agent; antioxidant; EC 3.5.1.98 (histone deacetylase) inhibitor; plant metabolite
berlition berlition: antioxidant preparation containing alpha-lipoic acid, used in the neuroprotective therapy of chronic brain ischemia for correction of free-radical processes. (R)-lipoic acid : The (R)-enantiomer of lipoic acid. A vitamin-like, C8 thia fatty acid with anti-oxidant properties.. lipoic acid : A heterocyclic thia fatty acid comprising pentanoic acid with a 1,2-dithiolan-3-yl group at the 5-position.	3.83	3	dithiolanes; heterocyclic fatty acid; lipoic acid; thia fatty acid	cofactor; nutraceutical; prosthetic group
selegiline Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.	3.14	1	selegiline; terminal acetylenic compound	geroprotector
rivastigmine [no description available]	3.55	2	carbamate ester; tertiary amino compound	cholinergic drug; EC 3.1.1.8 (cholinesterase) inhibitor; neuroprotective agent
propidium iodide [no description available]	3.14	1	organic iodide salt
latrepirdine latrepirdine: structure	3.14	1	methylpyridines; pyridoindole	geroprotector
tv3326 [no description available]	3.14	1	indanes
rasagiline [no description available]	3.14	1	indanes; secondary amine; terminal acetylenic compound	EC 1.4.3.4 (monoamine oxidase) inhibitor; neuroprotective agent
8-(3-chlorostyryl)caffeine 8-(3-chlorostyryl)caffeine: adenosine antagonist. 8-(3-chlorostyryl)caffeine : Caffeine substituted at its 8-position by an (E)-3-chlorostyryl group.	3.14	1	monochlorobenzenes; trimethylxanthine	adenosine A2A receptor antagonist; EC 1.4.3.4 (monoamine oxidase) inhibitor
sarizotan sarizotan: serotonin 5-HT1A agonist improves motor complications in rodent and primate parkinsonian models	3.14	1
ap 2238 [no description available]	3.14	1
memoquin memoquin: structure in first source	10.1	5
caproctamine caproctamine: an M1 and M3 receptor antagonist; also inhibits acetylcholinesterase; structure in first source	3.14	1
xanthostigmine xanthostigmine: structure in first source	3.14	1

Condition	Relationship Strength	Studies
Acute Confusional Senile Dementia [description not available]	5.5	8
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	5.5	8
Degenerative Diseases, Central Nervous System [description not available]	2.96	1
Amyloid Deposits [description not available]	2.96	1
Akinetic-Rigid Variant of Huntington Disease [description not available]	2.96	1
MS (Multiple Sclerosis) [description not available]	2.96	1
Idiopathic Parkinson Disease [description not available]	2.96	1
Huntington Disease A familial disorder inherited as an autosomal dominant trait and characterized by the onset of progressive CHOREA and DEMENTIA in the fourth or fifth decade of life. Common initial manifestations include paranoia; poor impulse control; DEPRESSION; HALLUCINATIONS; and DELUSIONS. Eventually intellectual impairment; loss of fine motor control; ATHETOSIS; and diffuse chorea involving axial and limb musculature develops, leading to a vegetative state within 10-15 years of disease onset. The juvenile variant has a more fulminant course including SEIZURES; ATAXIA; dementia; and chorea. (From Adams et al., Principles of Neurology, 6th ed, pp1060-4)	2.96	1
Multiple Sclerosis An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)	2.96	1
Parkinson Disease A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)	2.96	1
Neurodegenerative Diseases Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.	2.96	1

lipocrine

Description

Cross-References

Synonyms (8)

Research Excerpts

Effects

Protein Targets (3)

Inhibition Measurements

Biological Processes (101)

Molecular Functions (25)

Ceullar Components (46)

Bioassays (29)

Research

Studies (10)

Study Types

lipocrine

Description

Cross-References

Synonyms (8)

Research Excerpts

Effects

Protein Targets (3)

Inhibition Measurements

Biological Processes (101)

Molecular Functions (25)

Ceullar Components (46)

Bioassays (29)

Research

Studies (10)

Study Types

Related Drugs (19)

Related Conditions (11)