Compounds > itazigrel
Page last updated: 2024-12-06

itazigrel

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

Cross-References

ID SourceID
PubMed CID51087
CHEMBL ID277592
SCHEMBL ID564056
MeSH IDM0107573

Synonyms (28)

Synonym
itazigrel
itazogrel
u-53059
itazigrel (usan/inn)
70529-35-0
D04643
brn 1161179
itazigrelum [latin]
4,5-bis(p-methoxyphenyl)-2-(trifluoromethyl)thiazole
u 53059
ly 108048
4,5-bis(4-methoxyphenyl)-2-trifluoromethylthiazole
itazigrel [usan:inn]
4,5-bis(4-methoxyphenyl)-2-(trifluoromethyl)thiazole
u-53,059
thiazole, 4,5-bis(4-methoxyphenyl)-2-(trifluoromethyl)-
CHEMBL277592
4,5-bis(4-methoxyphenyl)-2-(trifluoromethyl)-1,3-thiazole
itazigrelum
unii-n835i8cxy0
n835i8cxy0 ,
SCHEMBL564056
itazigrel [usan]
itazigrel [inn]
DTXSID70220798
ly 108048; u 53059
Q27284689
cipbqtcsxvedsg-uhfffaoysa-n

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
"Liquid and semi-solid enteric dosage forms were prepared by entrapping drug with an appropriate partition coefficient in a lipid base vehicle which would then be released by the action of intestinal enzymes."( Use of enzymatic activity for design of orally administered enteric dosing forms.
Ishizaka, M; Nishihata, T; Yamamoto, K, 1993)		0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID76874Percent inhibition of platelet aggregation at 4 hours following oral administration to guinea pigs at 5 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID196872Induction of acute stomach lesion at a dose of 100 mg/Kg was determined in 5 animals1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID176610In vitro vasodilatory activity in isolated rat aorta1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID76871Percent inhibition of platelet aggregation at 16 hours following oral administration to guinea pigs at 5 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID76875Percent inhibition of platelet aggregation at 8 hours following oral administration to guinea pigs at 5 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID76870Percent inhibition of platelet aggregation at 12 hours following oral administration to guinea pigs at 5 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID76869Percent inhibition of platelet aggregation at 0 hours following oral administration to guinea pigs at 5 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID76035Inhibitory effect on platelet aggregation induced by Collagen in guinea pigs ex vivo at a dose of 1 mg/Kg after 6 hr of oral administration1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID76034Inhibitory effect on platelet aggregation induced by Collagen in guinea pigs ex vivo at a dose of 1 mg/Kg after 1 hr of oral administration1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID76872Percent inhibition of platelet aggregation at 2 hours following oral administration to guinea pigs at 5 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID76029Inhibitory effect on platelet aggregation induced by Arachidonic acid (AA) in guinea pigs ex vivo at a dose of 1 mg/Kg after 6 hr of oral administration1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID76882Percent inhibition of platelet aggregation following oral administration to guinea pigs at a dose of 5 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID76873Percent inhibition of platelet aggregation at 24 hours following oral administration to guinea pigs at 5 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID229999Induction of acute stomach lesion at a dose of 100 mg/Kg to determine the number of rats with ulceration; 2/51994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID76028Inhibitory effect on platelet aggregation induced by Arachidonic acid (AA) in guinea pigs ex vivo at a dose of 1 mg/Kg after 1 hr of oral administration1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID230186Induction of acute stomach lesion at a dose of 32 mg/Kg to determine the number of rats with ulceration; 1/51994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID196874Induction of acute stomach lesion at a dose of 32 mg/Kg was determined in 5 animals1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID89236In vitro inhibition of collagen-induced platelet aggregation in human platelet rich plasma1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID165617In vitro antiplatelet activity against arachidonic acid induced malondialdehyde production1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.
AID76878Percent inhibition of platelet aggregation following oral administration to guinea pigs at a dose of 0.5 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID76876Percent inhibition of platelet aggregation following oral administration to guinea pigs at a dose of 0.1 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID76881Percent inhibition of platelet aggregation following oral administration to guinea pigs at a dose of 1 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID76880Percent inhibition of platelet aggregation following oral administration to guinea pigs at a dose of 10 mg/kg1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
AID78137In vitro inhibition of collagen-induced platelet aggregation in guinea pig platelet rich plasma1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis and platelet aggregation inhibitory activity of 4,5-bis(aryl)-2-substituted-thiazoles.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906 (46.15)18.7374
1990's6 (46.15)18.2507
2000's0 (0.00)29.6817
2010's1 (7.69)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (15.38%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (84.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
1-anilino-8-naphthalenesulfonate
1-anilino-8-naphthalenesulfonate: RN given refers to parent cpd. 8-anilinonaphthalene-1-sulfonic acid : A naphthalenesulfonic acid that is naphthalene-1-sulfonic acid substituted by a phenylamino group at position 8.		1.9810aminonaphthalene;
naphthalenesulfonic acid		fluorescent probe
aspirin
Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.		9.0531benzoic acids;
phenyl acetates;
salicylates		anticoagulant;
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
EC 1.1.1.188 (prostaglandin-F synthase) inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
plant activator;
platelet aggregation inhibitor;
prostaglandin antagonist;
teratogenic agent
baclofen
[no description available]		1.9710amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid;
monochlorobenzenes;
primary amino compound		central nervous system depressant;
GABA agonist;
muscle relaxant
flurbiprofen
Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain.		1.9610fluorobiphenyl;
monocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
indomethacin
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.		2.3820aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		1.9710ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
4-bromophenacyl bromide
4-bromophenacyl bromide: phospholipidase A(2) inhibitor; structure		1.9710
thiazoles
[no description available]		5.711121,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
sudan red
[no description available]		1.9810
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		1.9710adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
timegadine
timegadine: first source states that SR 1368 is synonym for cpd; SR 1368 is a different cpd in Chemline; structure given in first source		1.9810
masoprocol
Masoprocol: A potent lipoxygenase inhibitor that interferes with arachidonic acid metabolism. The compound also inhibits formyltetrahydrofolate synthetase, carboxylesterase, and cyclooxygenase to a lesser extent. It also serves as an antioxidant in fats and oils.. masoprocol : The meso-form of nordihydroguaiaretic acid. An antioxidant found in the creosote bush, Larrea divaricata, it is a potent lipoxygenase inhibitor that interferes with arachidonic acid metabolism. It also inhibits (though to a lesser extent) formyltetrahydrofolate synthetase, carboxylesterase, and cyclooxygenase.		1.9710nordihydroguaiaretic acidantineoplastic agent;
hypoglycemic agent;
lipoxygenase inhibitor;
metabolite
fr 122047
[no description available]		1.9810aromatic amide;
thiazoles
arachidonic acid
icosa-5,8,11,14-tetraenoic acid : Any icosatetraenoic acid with the double bonds at positions 5, 8, 11 and 14.. arachidonate : A long-chain fatty acid anion resulting from the removal of a proton from the carboxy group of arachidonic acid.		1.9710icosa-5,8,11,14-tetraenoic acid;
long-chain fatty acid;
omega-6 fatty acid		Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
human metabolite;
mouse metabolite
leukotriene b4
Leukotriene B4: The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene B4 : A leukotriene composed of (6Z,8E,10E,14Z)-icosatetraenoic acid having (5S)- and (12R)-hydroxy substituents. It is a lipid mediator of inflammation that is generated from arachidonic acid via the 5-lipoxygenase pathway.		3.3711dihydroxy monocarboxylic acid;
hydroxy polyunsaturated fatty acid;
leukotriene;
long-chain fatty acid		human metabolite;
mouse metabolite;
plant metabolite;
vasoconstrictor agent
thromboxane b2
Thromboxane B2: A stable, physiologically active compound formed in vivo from the prostaglandin endoperoxides. It is important in the platelet-release reaction (release of ADP and serotonin).. thromboxane B2 : A member of the class of thromboxanes B that is (5Z,13E)-thromboxa-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15.		3.3711thromboxanes Bhuman metabolite;
mouse metabolite
ConditionIndicatedRelationship StrengthStudiesTrials
Thromboembolism
Obstruction of a blood vessel (embolism) by a blood clot (THROMBUS) in the blood stream.		01.9610
Gastric Ulcer
[description not available]		01.9810
Stomach Ulcer
Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).		01.9810
Dirofilariasis
Infection with nematodes of the genus DIROFILARIA, usually in animals, especially dogs, but occasionally in man.		01.9610