Compounds > k 134 compound
Page last updated: 2024-11-12

k 134 compound

Description

OPC 33509: has both anti-thrombotic and anti-hyperplastic activities; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9908900
CHEMBL ID284838
SCHEMBL ID5383733
MeSH IDM0508586

Synonyms (24)

Synonym
CHEMBL284838
k-134
opc-33509
k134 ,
189362-06-9
k134 compound
k 134 compound
6-(3-(3-cyclopropyl-3-(2-hydroxycyclohexyl)ureido)propoxy)-2(1h)-quinolinone
k-134 compound
urea, n-cyclopropyl-n'-(3-((1,2-dihydro-2-oxo-6-quinolinyl)oxy)propyl)-n-((1r,2r)-2-hydroxycyclohexyl)-
opc 33509
j9j6nk6w4u ,
unii-j9j6nk6w4u
SCHEMBL5383733
DTXSID90172346
AKOS027337121
(-)-6-(3-(3-cyclopropyl-3-((1r,2r)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1h)-quinolinone
HY-U00186
CS-7279
DB12685
1-cyclopropyl-1-((1r,2r)-2-hydroxycyclohexyl)-3-(3-((2-oxo-1,2-dihydroquinolin-6-yl)oxy)propyl)urea
Q27281383
MS-26772
1-cyclopropyl-1-[(1r,2r)-2-hydroxycyclohexyl]-3-[3-[(2-oxo-1h-quinolin-6-yl)oxy]propyl]urea

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Safety evaluations performed during 14- and 28-day visits which included in-clinic dosing and assessments at peak drug concentrations provided core data for the DMC review."( Application of adaptive design and decision making to a phase II trial of a phosphodiesterase inhibitor for the treatment of intermittent claudication.
Brass, EP; Connor, JT; Cooper, LT; Hiatt, WR; Lewis, RJ; Murphy, JR; Teerlink, JR, 2011)		0.37
" On the other hand, the effects of cilostazol on MCA occlusion time and cerebral infarct size are relatively weak even at the high dosage of 300 mg/kg."( K-134, a phosphodiesterase 3 inhibitor, prevents brain damage by inhibiting thrombus formation in a rat cerebral infarction model.
Asanuma, A; Ashikawa, Y; Hidaka, H; Inoue, Y; Itoh, S; Nakagawa, T; Tanabe, S; Yoshida, H, 2012)		0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID184172In vivo anti-hyperplastic activity was evaluated by the inhibition of balloon injury model in rats at a dose of 30 mg/kg (p.o.)1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities.
AID167829In vitro inhibitory activity against Adenosine diphosphate (ADP) induced rabbit platelet aggregation1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities.
AID134685In vivo anti-thrombotic activity was evaluated by the inhibition of pulmonary thromboembolism model in mice at a dose of 30 mg/kg (p.o.)1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities.
AID167830In vitro inhibitory activity against collagen induced rabbit platelet aggregation1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities.
AID134684In vivo anti-thrombotic activity was evaluated by the inhibition of pulmonary thromboembolism model in mice at a dose of 10 mg/kg (p.o.)1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities.
AID184049In vivo anti-hyperplastic activity was evaluated by the inhibition of balloon injury model in rats at a dose of 10 mg/kg (p.o.)1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
2(1H)-quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (8.33)18.2507
2000's3 (25.00)29.6817
2010's6 (50.00)24.3611
2020's2 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.32

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

MetricThis Compound (vs All)
Research Demand Index12.32 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index5.03 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (16.67%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		6.79122isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
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.		2.4220benzoic 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
cilostamide
cilostamide: selective inhibitor of cyclic AMP phosphodiesterase & platelet aggregation; structure		2.420quinolines
cilostazol
[no description available]		4.1131lactam;
tetrazoles		anticoagulant;
bronchodilator agent;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
fibrin modulating drug;
neuroprotective agent;
platelet aggregation inhibitor;
vasodilator agent
lauric acid
dodecanoic acid : A straight-chain, twelve-carbon medium-chain saturated fatty acid with strong bactericidal properties; the main fatty acid in coconut oil and palm kernel oil.		2.0710medium-chain fatty acid;
straight-chain saturated fatty acid		algal metabolite;
antibacterial agent;
plant metabolite
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		2.420monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		2.0610amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
tirofiban
Tirofiban: Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME.. tirofiban : A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group.		2.0610L-tyrosine derivative;
piperidines;
sulfonamide		anticoagulant;
fibrin modulating drug;
platelet glycoprotein-IIb/IIIa receptor antagonist
ristocetin
Ristocetin: An antibiotic mixture of two components, A and B, obtained from Nocardia lurida (or the same substance produced by any other means). It is no longer used clinically because of its toxicity. It causes platelet agglutination and blood coagulation and is used to assay those functions in vitro.. ristocetin : A heterodetic cyclic peptide that is produced by species of Amycolatopsis and Nocardia.		2.0610glycopeptide;
heterodetic cyclic peptide;
macrocycle;
tetrasaccharide derivative		antibacterial drug;
antimicrobial agent;
bacterial metabolite;
platelet-activating factor receptor agonist
cyclic gmp
Cyclic GMP: Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed). 3',5'-cyclic GMP : A 3',5'-cyclic purine nucleotide in which the purine nucleobase is specified as guanidine.		2.06103',5'-cyclic purine nucleotide;
guanyl ribonucleotide		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
ConditionIndicatedRelationship StrengthStudiesTrials
Blood Clot
[description not available]		02.7230
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.		01.9910
Hyperplasia
An increase in the number of cells in a tissue or organ without tumor formation. It differs from HYPERTROPHY, which is an increase in bulk without an increase in the number of cells.		01.9910
Thrombosis
Formation and development of a thrombus or blood clot in the blood vessel.		02.7230
Apoplexy
[description not available]		02.4110
Cerebral Microangiopathies
[description not available]		02.4110
Brain Hemorrhage, Cerebral
[description not available]		02.4110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.8130
Cerebral Hemorrhage
Bleeding into one or both CEREBRAL HEMISPHERES including the BASAL GANGLIA and the CEREBRAL CORTEX. It is often associated with HYPERTENSION and CRANIOCEREBRAL TRAUMA.		02.4110
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)		02.4110
Cerebral Small Vessel Diseases
Pathological processes or diseases where cerebral MICROVESSELS show abnormalities. They are often associated with aging, hypertension and risk factors for lacunar infarcts (see LACUNAR INFARCTION); LEUKOARAIOSIS; and CEREBRAL HEMORRHAGE.		02.4110
Complication, Postoperative
[description not available]		02.0410
Postoperative Complications
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.		02.0410
Peripheral Arterial Diseases
[description not available]		05.8542
Intermittent Claudication
A symptom complex characterized by pain and weakness in SKELETAL MUSCLE group associated with exercise, such as leg pain and weakness brought on by walking. Such muscle limpness disappears after a brief rest and is often relates to arterial STENOSIS; muscle ISCHEMIA; and accumulation of LACTATE.		17.3322
Peripheral Arterial Disease
Lack of perfusion in the EXTREMITIES resulting from atherosclerosis. It is characterized by INTERMITTENT CLAUDICATION, and an ANKLE BRACHIAL INDEX of 0.9 or less.		05.8542
Vascular Injuries
[description not available]		02.0710
Necrosis
The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.		02.0710
Gait Disorders, Animal
[description not available]		02.0710
Anterior Choroidal Artery Infarction
[description not available]		02.0710
Cerebral Infarction
The formation of an area of NECROSIS in the CEREBRUM caused by an insufficiency of arterial or venous blood flow. Infarcts of the cerebrum are generally classified by hemisphere (i.e., left vs. right), lobe (e.g., frontal lobe infarction), arterial distribution (e.g., INFARCTION, ANTERIOR CEREBRAL ARTERY), and etiology (e.g., embolic infarction).		02.0710
chemdatabank.com