Compounds > pactimibe
Page last updated: 2024-12-10

pactimibe

Cross-References

ID SourceID
PubMed CID3081927
CHEMBL ID478858
SCHEMBL ID282098
MeSH IDM0496795

Synonyms (31)

Synonym
d874r9pz9t ,
1h-indole-5-acetic acid, 7-((2,2-dimethyl-1-oxopropyl)amino)-2,3-dihydro-4,6-dimethyl-1-octyl-
unii-d874r9pz9t
pactimibe [inn:ban]
(7-(2,2-dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl)acetic acid hemisulfate
(7-(2,2-dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl)acetic acid
pactimibe
2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindol-5-yl]acetic acid
bdbm50263192
[7-(2,2-dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl]acetic acid
CHEMBL478858 ,
189198-30-9
pactimibe [who-dd]
pactimibe [inn]
SCHEMBL282098
TXIIZHHIOHVWJD-UHFFFAOYSA-N
n-(1-octyl-5-carboxymethyl-4,6-dimethylindolin-7-yl)-2,2-dimethyl-propanamide
n-(1- octyl-5-carboxymethyl-4,6-dimethylindolin-7-yl)-2,2-dimethyl-propanamide
n-(1-octyl-5-carboxymethyl-4,6-dimethylindolin-7-yl)-2,2-dimethylpropanamide
DTXSID80172315
DB12971
2-[7-(2,2-dimethylpropanoylamino)-4,6-dimethyl-1-octyl-2,3-dihydroindo l-5-yl]acetic acid
pactimibe free base
189198-30-9 (free base)
Q27276240
MS-27258
1h-indole-5-acetic acid, 7-[(2,2-dimethyl-1-oxopropyl)amino]-2,3-dihydro-4,6-dimethyl-1-octyl-
HY-100401
CS-0018790
GLXC-27010
AKOS040749113

Research Excerpts

Overview

Pactimibe sulfate is a novel acyl coenzyme A:cholesterol acyltransferase inhibitor. Developed for the treatment of hypercholesterolemia and atherosclerotic diseases.

ExcerptReferenceRelevance
"Pactimibe is a novel ACAT inhibitor. "( Effect of CYP2D6 polymorphism on pharmacokinetics of a novel ACAT inhibitor, pactimibe and its unique metabolite, R-125528.
Freudenthaler, S; Kotsuma, M; Nishimura, K; Tokui, T, 2008)		2.02
"Pactimibe sulfate is a novel acyl coenzyme A:cholesterol acyltransferase inhibitor. "( CYP2D6-Mediated metabolism of a novel acyl coenzyme A:cholesterol acyltransferase inhibitor, pactimibe, and its unique plasma metabolite, R-125528.
Honda, T; Ikeda, T; Ishizuka-Ozeki, T; Iwabuchi, H; Kotsuma, M; Murai, T; Saji, H; Tokui, T, 2008)		2.01
"Pactimibe sulfate is a novel acyl coenzyme A:cholesterol acyltransferase inhibitor developed for the treatment of hypercholesterolemia and atherosclerotic diseases. "( Effects of ketoconazole and quinidine on pharmacokinetics of pactimibe and its plasma metabolite, R-125528, in humans.
Freudenthaler, S; Kotsuma, M; Nishimura, K; Tokui, T, 2008)		2.03

Effects

Pactimibe has lower affinity than R-125528; however, the K(m) value was comparable with that of metoprolol.

ExcerptReferenceRelevance
"Pactimibe has lower affinity than R-125528; however, the K(m) value was comparable with that of metoprolol."( Novel binding mode of the acidic CYP2D6 substrates pactimibe and its metabolite R-125528.
Hanzawa, H; Iwata, Y; Kotsuma, M; Takahashi, K; Tokui, T, 2008)		1.32
"Pactimibe has two equally dominant clearance pathways forming R-125528 by CYP3A4 and M-1 by CYP2D6 in vitro."( Effects of ketoconazole and quinidine on pharmacokinetics of pactimibe and its plasma metabolite, R-125528, in humans.
Freudenthaler, S; Kotsuma, M; Nishimura, K; Tokui, T, 2008)		1.31

Actions

ExcerptReferenceRelevance
"Pactimibe has lower affinity than R-125528; however, the K(m) value was comparable with that of metoprolol."( Novel binding mode of the acidic CYP2D6 substrates pactimibe and its metabolite R-125528.
Hanzawa, H; Iwata, Y; Kotsuma, M; Takahashi, K; Tokui, T, 2008)		1.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sterol O-acyltransferase 2Homo sapiens (human)IC50 (µMol)3.00000.11003.20369.2000AID754943
Sterol O-acyltransferase 1Homo sapiens (human)IC50 (µMol)2.33330.02501.79758.0000AID342634; AID342640; AID754944
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)IC50 (µMol)6.33330.00600.98467.6000AID341878; AID342637; AID342641
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
cholesterol metabolic processSterol O-acyltransferase 2Homo sapiens (human)
macrophage derived foam cell differentiationSterol O-acyltransferase 2Homo sapiens (human)
cholesterol storageSterol O-acyltransferase 2Homo sapiens (human)
intestinal cholesterol absorptionSterol O-acyltransferase 2Homo sapiens (human)
cholesterol effluxSterol O-acyltransferase 2Homo sapiens (human)
very-low-density lipoprotein particle assemblySterol O-acyltransferase 2Homo sapiens (human)
low-density lipoprotein particle clearanceSterol O-acyltransferase 2Homo sapiens (human)
cholesterol homeostasisSterol O-acyltransferase 2Homo sapiens (human)
cholesterol metabolic processSterol O-acyltransferase 1Homo sapiens (human)
cholesterol metabolic processSterol O-acyltransferase 1Homo sapiens (human)
macrophage derived foam cell differentiationSterol O-acyltransferase 1Homo sapiens (human)
cholesterol storageSterol O-acyltransferase 1Homo sapiens (human)
cholesterol effluxSterol O-acyltransferase 1Homo sapiens (human)
very-low-density lipoprotein particle assemblySterol O-acyltransferase 1Homo sapiens (human)
low-density lipoprotein particle clearanceSterol O-acyltransferase 1Homo sapiens (human)
cholesterol homeostasisSterol O-acyltransferase 1Homo sapiens (human)
positive regulation of amyloid precursor protein biosynthetic processSterol O-acyltransferase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
fatty-acyl-CoA bindingSterol O-acyltransferase 2Homo sapiens (human)
sterol O-acyltransferase activitySterol O-acyltransferase 2Homo sapiens (human)
protein bindingSterol O-acyltransferase 2Homo sapiens (human)
cholesterol bindingSterol O-acyltransferase 2Homo sapiens (human)
acyltransferase activitySterol O-acyltransferase 2Homo sapiens (human)
cholesterol O-acyltransferase activitySterol O-acyltransferase 2Homo sapiens (human)
fatty-acyl-CoA bindingSterol O-acyltransferase 1Homo sapiens (human)
sterol O-acyltransferase activitySterol O-acyltransferase 1Homo sapiens (human)
protein bindingSterol O-acyltransferase 1Homo sapiens (human)
cholesterol bindingSterol O-acyltransferase 1Homo sapiens (human)
cholesterol O-acyltransferase activitySterol O-acyltransferase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
endoplasmic reticulumSterol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 2Homo sapiens (human)
brush borderSterol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulumSterol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 1Homo sapiens (human)
membraneSterol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (33)

Assay IDTitleYearJournalArticle
AID341893Hypolipidemic effect in regular diet fed Syrian hamster assessed as HDL:HDL cholesterol level at 3 mg/kg/day, po for 3 weeks2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID429636Half life in Sprague-Dawley rat at 10 mg/kg, po2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Novel indoline-based acyl-CoA: cholesterol acyltransferase inhibitor: Effects of introducing a methanesulfonamide group on physicochemical properties and biological activities.
AID754943Inhibition of macrophage ACAT2 (unknown origin)2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Manzamine A, a marine-derived alkaloid, inhibits accumulation of cholesterol ester in macrophages and suppresses hyperlipidemia and atherosclerosis in vivo.
AID429635Tmax in Sprague-Dawley rat at 10 mg/kg, po2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Novel indoline-based acyl-CoA: cholesterol acyltransferase inhibitor: Effects of introducing a methanesulfonamide group on physicochemical properties and biological activities.
AID341886Hypolipidemic effect in high-cholesterol diet fed Wistar rat assessed as LDL/VLDL cholesterol level at 3 mg/kg/day, po for 3 days2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341890Hypolipidemic effect in Western diet fed Beagle dog assessed as LDL/VLDL cholesterol level at 3 mg/kg/day, po for 7 days2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341880Inhibition of LCAT up to 10 uM2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341891Hypolipidemic effect in Western diet fed Beagle dog assessed as HDL:HDL cholesterol level at 3 mg/kg/day, po for 7 days2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341883Cmax in Sprague-Dawley rat at 10 mg/kg, po2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341882Inhibition of LDL oxidation in genetically hypercholesterolemic KHC rabbit plasma assessed as malonaldehyde level after 1 hr2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID429633Inhibition of hepatic cholesterol secretion in ICR mouse at 10 mg/kg, po after 3 hrs by enzymatic method2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Novel indoline-based acyl-CoA: cholesterol acyltransferase inhibitor: Effects of introducing a methanesulfonamide group on physicochemical properties and biological activities.
AID341887Hypolipidemic effect in high-cholesterol diet fed Wistar rat assessed as HDL cholesterol level at 3 mg/kg/day, po for 3 days2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341884Cmax in Japanese white rabbit at 10 mg/kg, po2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID429631Protein binding in rat plasma assessed as total and protein free fraction concentration at 10 ug/ML after 150 mins by ultracentrifugation method2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Novel indoline-based acyl-CoA: cholesterol acyltransferase inhibitor: Effects of introducing a methanesulfonamide group on physicochemical properties and biological activities.
AID342643Inhibition of ACAT in hyperlipidemic white rabbit intestine microsomes assessed as esterified cholesterol accumulation2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID429637AUC (0 to 24 hrs) in Sprague-Dawley rat at 10 mg/kg, po2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Novel indoline-based acyl-CoA: cholesterol acyltransferase inhibitor: Effects of introducing a methanesulfonamide group on physicochemical properties and biological activities.
AID342634Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL during differentiation assessed as effect on foam cell formation2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID342637Inhibition of normocholesterolemic rabbit liver ACAT2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID342640Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL after differentiation assessed as effect on foam cell formation2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID429632Anti-foam cell formation activity in human THP1 cells assessed as inhibition of esterified cholesterol accumulation after 24 hrs in presence of albumin2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Novel indoline-based acyl-CoA: cholesterol acyltransferase inhibitor: Effects of introducing a methanesulfonamide group on physicochemical properties and biological activities.
AID342639AUC in Sprague-Dawley rat at 10 mg/kg, po2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341888Hypolipidemic effect in high-cholesterol diet fed Japanese white rabbit assessed as LDL/VLDL cholesterol level at 1 mg/kg/day, po for 7 days2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID429634Cmax in Sprague-Dawley rat at 10 mg/kg, po2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Novel indoline-based acyl-CoA: cholesterol acyltransferase inhibitor: Effects of introducing a methanesulfonamide group on physicochemical properties and biological activities.
AID341879Adrenotoxicity in guinea pig at 100 mg/kg/day administered for 4 days2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID754944Inhibition of ACAT1 (unknown origin)2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Manzamine A, a marine-derived alkaloid, inhibits accumulation of cholesterol ester in macrophages and suppresses hyperlipidemia and atherosclerosis in vivo.
AID341878Inhibition of ACAT in hyperlipidemic white rabbit adrenal microsomes assessed as esterified cholesterol accumulation2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID342638Antiperoxidative activity in Sprague-Dawley rat brain assessed as inhibition of malonaldehyde level2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341881Inhibition of lipid peroxidation in genetically hypercholesterolemic KHC rabbit serum assessed as malonaldehyde level after 4 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341889Hypolipidemic effect in high-cholesterol diet fed Japanese white rabbit assessed as HDL cholesterol level at 1 mg/kg/day, po for 7 days2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID342641Inhibition of ACAT in microsomes from hyperlipidemic white rabbit macrophages assessed as esterified cholesterol accumulation2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341885Cmax in Beagle dog at 10 mg/kg, po2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID341892Hypolipidemic effect in regular diet fed Syrian hamster assessed as LDL/VLDL cholesterol level at 3 mg/kg/day, po for 3 weeks2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
AID342642Inhibition of ACAT in hyperlipidemic white rabbit liver microsomes assessed as esterified cholesterol accumulation2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and biological activities by introduction of carboxylic acid.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's18 (94.74)29.6817
2010's1 (5.26)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.20

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.20 (24.57)
Research Supply Index3.22 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.20)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (20.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
glycine
[no description available]		2.0310alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid		EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		8.4311dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
probucol
Probucol: A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).. probucol : A dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood.		2.0410dithioketal;
polyphenol		anti-inflammatory drug;
anticholesteremic drug;
antilipemic drug;
antioxidant;
cardiovascular drug
oxazoles
Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.		2.03101,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
indoline
indoline: structure given in first source		2.0510indoles
norharman
norharman: RN given refers to parent cpd. beta-carboline : The parent compound of the beta-carbolines, a tricyclic structure comprising an indole ring system ortho- fused to C-3 and C-4 of a pyridine ring.		2.0810beta-carbolines;
mancude organic heterotricyclic parent		fungal metabolite;
marine metabolite
methanesulfonamide
[no description available]		2.0510
avasimibe
[no description available]		2.4620monoterpenoid
f 1394
F 1394: an acyl-CoA:cholesterol acyltransferase (ACAT) inibitor; structure given in first source		2.0810
muraglitazar
muraglitazar: has glucose- and lipid-lowering activities; structure in first source; molecule composed of benzyloxazole-phenoxy-oxybenzylglycine-phenoxyl having structural analogy to PHENOXYBENZAMINE		2.03101,3-oxazoles
quinidine
Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.		8.4311cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
epinephrine
ircinal A: from an Indonesian Acanthostrongylophora sponge with activity against infectious, tropical parasitic, and Alzheimer's diseases; structure in first source		2.0810
oleoyl-coenzyme a
oleoyl-coenzyme A: RN given refers to (Z)-isomer		2.0310octadecenoyl-CoAEscherichia coli metabolite;
mouse metabolite
manzamine a
manzamine A: RN given refers to (1R-(1R*,9Z,13S*,13aR*,20aR*,21aR*)-isomer; RN for cpd without isomeric designation not avail 12/92. manzamine A : An alkaloid of the class of beta-carbolines isolated from Haliclona and Acanthostrongylophora. It exhibits inhibitory activity against Glycogen Synthase Kinase-3 (EC 2.7.11.26).		2.0810alkaloid;
beta-carbolines;
isoquinolines		animal metabolite;
anti-HSV-1 agent;
antimalarial;
antineoplastic agent;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
marine metabolite
ConditionIndicatedRelationship StrengthStudiesTrials
Atherogenesis
[description not available]		03.1450
Hyperlipemia
[description not available]		02.4620
Hyperlipidemias
Conditions with excess LIPIDS in the blood.		02.4620
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		15.1450
Disease Exacerbation
[description not available]		06.2842
Arterial Diseases, Carotid
[description not available]		04.7521
Apolipoprotein B-100, Familial Defective
[description not available]		04.7521
Carotid Artery Diseases
Pathological conditions involving the CAROTID ARTERIES, including the common, internal, and external carotid arteries. ATHEROSCLEROSIS and TRAUMA are relatively frequent causes of carotid artery pathology.		04.7521
Hyperlipoproteinemia Type II
A group of familial disorders characterized by elevated circulating cholesterol contained in either LOW-DENSITY LIPOPROTEINS alone or also in VERY-LOW-DENSITY LIPOPROTEINS (pre-beta lipoproteins).		04.7521
Hyperlipoproteinemia
[description not available]		02.0510
Hyperlipoproteinemias
Conditions with abnormally elevated levels of LIPOPROTEINS in the blood. They may be inherited, acquired, primary, or secondary. Hyperlipoproteinemias are classified according to the pattern of lipoproteins on electrophoresis or ultracentrifugation.		02.0510
Arteriosclerosis, Coronary
[description not available]		05.2541
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		04.3311
Coronary Artery Disease
Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.		05.2541
Elevated Cholesterol
[description not available]		02.4320
Arteriosclerosis
Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.		02.0310
Hypercholesterolemia
A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population.		02.4320
Alloxan Diabetes
[description not available]		02.0310
Coronary Heart Disease
[description not available]		02.0310
Coronary Disease
An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.		14.0310
Apoplexy
[description not available]		02.0310
Coronary Thrombosis
Coagulation of blood in any of the CORONARY VESSELS. The presence of a blood clot (THROMBUS) often leads to MYOCARDIAL INFARCTION.		02.0310
Diabetes Mellitus, Adult-Onset
[description not available]		02.0310
Cardiac Failure
[description not available]		02.0310
Cardiovascular Stroke
[description not available]		02.0310
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		02.0310
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		02.0310
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		02.0310
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		02.0310
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		03.4311
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