Compounds > bms 747158-02
Page last updated: 2024-11-12

bms 747158-02

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

Description

BMS 747158-02: a PET myocardial imaging agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11405965
CHEMBL ID2107799
SCHEMBL ID12453262
MeSH IDM0517688

Synonyms (33)

Synonym
[18f]bms-747158-01
2-tert-butyl-4-chloro-5-[4-(2-[18f]fluoroethoxymethyl)-benzyloxy]-2h-pyridazin-3-one
BMS-747158-02 ,
bms 747158-02
flurpiridaz f 18 (usan)
D10009
CHEMBL2107799
fluripiridaz f 18
bms-747158
flurpiridaz f-18
flurpiradaz f 18 [usan:inn]
4-chloro-2-(1,1-dimethylethyl)-5-((4-((2-((sup 18)f)fluoroethoxy)methyl)phenyl) methoxy)pyridazin-3(2h)-one
ty3v24c029 ,
flurpiridaz, f-18
863887-89-2
flurpiridaz (18f)
flurpiridaz (18f) [inn]
flurpiridaz f 18
bms747158
flurpiridaz f 18 [usan]
flurpiradaz f 18
3(2h)-pyridazinone, 4-chloro-2-(1,1-dimethylethyl)-5-((4-((2-(fluoro-(sup 18)f)ethoxy)methyl)phenyl)methoxy)-
unii-ty3v24c029
SCHEMBL12453262
flurpiridaz ((1)f) [inn]
flurpiridaz (18f) [who-dd]
3(2h)-pyridazinone, 4-chloro-2-(1,1-dimethylethyl)-5-((4-((2-(fluoro-18f)ethoxy)methyl)phenyl)methoxy)-
2-tert-butyl-4-chloro-5-((4-((2-(18f)fluoroethoxy)methyl)phenyl)methoxy)pyridazin-3(2h)-one
DTXSID00235517
18f-flurpiridaz
2-tert-butyl-4-chloro-5-[[4-(2-(18f)fluoranylethoxymethyl)phenyl]methoxy]pyridazin-3-one
flurpiridaz (18f); flurpiridaz f 18
Q27290481

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" There were no drug-related adverse events, and the tracer was well tolerated in all subjects."( Phase I, first-in-human study of BMS747158, a novel 18F-labeled tracer for myocardial perfusion PET: dosimetry, biodistribution, safety, and imaging characteristics after a single injection at rest.
Crane, P; Czernin, J; Dahlbom, M; Devine, M; Ehlgen, A; Huang, SC; Lazewatsky, J; Maddahi, J; Phelps, M; Schelbert, H; Sparks, R; Zhu, Q, 2011)		0.37
" Extensive safety assessment revealed that flurpiridaz F 18 was safe in this cohort."( Phase II safety and clinical comparison with single-photon emission computed tomography myocardial perfusion imaging for detection of coronary artery disease: flurpiridaz F 18 positron emission tomography.
Berman, DS; Bhat, G; Czernin, J; Devine, M; Gibson, CM; Lazewatsky, J; Maddahi, J; Taillefer, R; Tamarappoo, BK; Udelson, JE; Washburn, D, 2013)		0.39
"In this phase 2 trial, PET MPI with flurpiridaz F 18 was safe and superior to SPECT MPI for image quality, interpretative certainty, and overall CAD diagnosis."( Phase II safety and clinical comparison with single-photon emission computed tomography myocardial perfusion imaging for detection of coronary artery disease: flurpiridaz F 18 positron emission tomography.
Berman, DS; Bhat, G; Czernin, J; Devine, M; Gibson, CM; Lazewatsky, J; Maddahi, J; Taillefer, R; Tamarappoo, BK; Udelson, JE; Washburn, D, 2013)		0.39
" There were no drug-related adverse events, and the tracer was well tolerated in all subjects."( Dosimetry, biodistribution, and safety of flurpiridaz F 18 in healthy subjects undergoing rest and exercise or pharmacological stress PET myocardial perfusion imaging.
Bengel, F; Crane, P; Czernin, J; Dahlbom, M; Lazewatsky, J; Maddahi, J; Phelps, M; Schelbert, H; Sparks, R, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID709478Ratio of drug level in heart to liver in Wistar rat after 60 mins2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Effect of the prosthetic group on the pharmacologic properties of 18F-labeled rhodamine B, a potential myocardial perfusion agent for positron emission tomography (PET).
AID709479Biodistribution in Wistar rat liver after 60 mins2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Effect of the prosthetic group on the pharmacologic properties of 18F-labeled rhodamine B, a potential myocardial perfusion agent for positron emission tomography (PET).
AID709480Biodistribution in Sprague-Dawley rat heart after 60 mins2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Effect of the prosthetic group on the pharmacologic properties of 18F-labeled rhodamine B, a potential myocardial perfusion agent for positron emission tomography (PET).
AID709476Ratio of drug level in heart to blood in Sprague-Dawley rat after 60 mins2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Effect of the prosthetic group on the pharmacologic properties of 18F-labeled rhodamine B, a potential myocardial perfusion agent for positron emission tomography (PET).
AID709481Biodistribution in Wistar rat liver after 10 mins2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Effect of the prosthetic group on the pharmacologic properties of 18F-labeled rhodamine B, a potential myocardial perfusion agent for positron emission tomography (PET).
AID709477Ratio of drug level in heart to liver in Sprague-Dawley rat after 60 mins2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Effect of the prosthetic group on the pharmacologic properties of 18F-labeled rhodamine B, a potential myocardial perfusion agent for positron emission tomography (PET).
AID709482Biodistribution in Wistar rat heart after 60 mins2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Effect of the prosthetic group on the pharmacologic properties of 18F-labeled rhodamine B, a potential myocardial perfusion agent for positron emission tomography (PET).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (30)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (16.67)29.6817
2010's20 (66.67)24.3611
2020's5 (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: 11.25

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 Index11.25 (24.57)
Research Supply Index3.76 (2.92)
Research Growth Index5.02 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (16.67%)5.53%
Reviews5 (13.89%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (69.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
ammonium hydroxide
azane : Saturated acyclic nitrogen hydrides having the general formula NnHn+2.		3.5920azane;
gas molecular entity;
mononuclear parent hydride		EC 3.5.1.4 (amidase) inhibitor;
metabolite;
mouse metabolite;
neurotoxin;
NMR chemical shift reference compound;
nucleophilic reagent;
refrigerant
rotenone
Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.		2.0710organic heteropentacyclic compound;
rotenones		antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin
pyridazine
pyridazine: structure given in first source		2.110diazine;
pyridazines
triphenyltetrazolium
triphenyltetrazolium: RN given refers to parent cpd. 2,3,5-triphenyltetrazolium : An organic cation that is tetrazole carrying three phenyl substituents at positions 2, 3 and 5.		2.0710organic cation
dobutamine
Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.. dobutamine : A catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure.		2.0610catecholamine;
secondary amine		beta-adrenergic agonist;
cardiotonic drug;
sympathomimetic agent
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		2.5220adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
technetium tc 99m sestamibi
Technetium Tc 99m Sestamibi: A technetium imaging agent used to reveal blood-starved cardiac tissue during a heart attack.		3.4711
ConditionIndicatedRelationship StrengthStudiesTrials
Arteriosclerosis, Coronary
[description not available]		08.4873
Coronary Artery Disease
Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.		08.4873
Heart Disease, Ischemic
[description not available]		04.230
Myocardial Ischemia
A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).		04.230
Coronary Occlusion
Complete blockage of blood flow through one of the CORONARY ARTERIES, usually from CORONARY ATHEROSCLEROSIS.		02.4920
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2110
Coronary Artery Stenosis
[description not available]		03.0110
Coronary Stenosis
Narrowing or constriction of a coronary artery.		03.0110
Injury, Ischemia-Reperfusion
[description not available]		02.0410
Ischemia
A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.		02.0410
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		02.0410
Cardiovascular Stroke
[description not available]		02.4620
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		02.4620
Chronic Illness
[description not available]		02.0510
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		02.0510
Coronary Heart Disease
[description not available]		02.9810
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.		02.9810
Cerebral Ischemia
[description not available]		02.0710
Brain Ischemia
Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.		02.0710
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)		03.4711