Page last updated: 2024-11-06

fosfedil

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

Description

fosfedil: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID53421
CHEMBL ID39516
SCHEMBL ID612913
MeSH IDM0109825

Synonyms (42)

Synonym
PDSP1_001081
phosphonic acid, ((4-(2-benzothiazolyl)phenyl)methyl)-, diethyl ester
fostedilum [latin]
fostedil [usan:inn]
diethyl (p-2-benzothiazolylbenzyl)phosphonate
brn 3626546
diethyl 4-(benzothiazol-2-yl)benzylphosphonate
phosphonic acid, (p-(2-benzothiazolyl)benzyl)-, diethyl ester
fosfedil
(p-(2-benzothiazolyl)benzyl)phosphonic acid diethyl ester
a 53986
kb 944
fostedil (usan/inn)
D04260
75889-62-2
PDSP2_001065
fostedil
kb-944
CHEMBL39516
a-53986
2-[4-(diethoxyphosphorylmethyl)phenyl]-1,3-benzothiazole
nsc_53421
cas_53421
bdbm82059
diethyl ((4-(2-benzothiazolyl)phenyl)methyl)phosphonate
fostedilum
d41ws786ul ,
unii-d41ws786ul
phosphonic acid,p-[[4-(2-benzothiazolyl)phenyl]methyl]-, diethyl ester
phosphonic acid, p-((4-(2-benzothiazolyl)phenyl)methyl)-, diethyl ester
fostedil [usan]
fostedil [inn]
SCHEMBL612913
DTXSID70226811
FVYRUSCZCWSFLT-UHFFFAOYSA-N
1-(benzothiazol-2-yl)-4-diethoxyphosphinylmethylbenzene
AKOS027379634
2-[4-(diethoxyphosphorylmethyl)phenyl]benzothiazole
diethyl [4-(1,3-benzothiazol-2-yl)benzyl]phosphonate
2-[4-(diethoxyphosphorylmethyl)phenyl]benzo[d]thiazole
Q15408402
diethyl (4-(benzo[d]thiazol-2-yl)benzyl)phosphonate

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"The acute toxicity of diethyl 4-(benzothiazol-2-yl)benzylphosphonate (KB-944) was studied in mice, rats and dogs: In mice and rats, toxic symptoms such as deceleration of spontaneous movement, ataxic gait, disappearance of righting reflex, reduction in body temperature and suppression of breathing appeared following administration of a single dose of KB-944."( Acute toxicity study of KB-944, a new calcium antagonist.
Hirakawa, K; Iino, T; Nose, T; Ogino, F; Takebe, H; Unno, T, 1982
)
0.26
" There were no further findings, even histopathologically, which showed any toxic effect of the drug."( 1-month subacute oral toxicity study of KB-944, a new calcium antagonist, in beagles.
Hirakawa, K; Iino, T; Nose, T; Ogino, F; Takebe, H; Unno, T, 1982
)
0.26

Pharmacokinetics

ExcerptReferenceRelevance
" The plasma levels and urinary excretion of intact fostedil were measured, and the pharmacokinetic parameters of the drug were defined."( Pharmacokinetics of fostedil, a new calcium antagonist, in beagle dogs following oral and intravenous administration.
Bopp, BA; Thomas, EW, 1984
)
0.27

Bioavailability

ExcerptReferenceRelevance
" Furthermore, KB-944 is well absorbed from the intestinal tract, and produces a long-acting increase in the coronary blood flow."( Vasodilator action of KB-944, a new calcium antagonist.
Ito, K; Kanazawa, T; Morita, T; Nose, T; Yoshino, K, 1982
)
0.26

Dosage Studied

ExcerptRelevanceReference
" In plasma there was a decrease in alkaline phosphatase activity, creatinine level and cholinesterase activity and an increase in GPT activity and total cholesterol level in rats given a higher dosage of the drug."( 1-month subacute oral toxicity study of KB-944, a new calcium antagonist, in rats.
Hirakawa, K; Iino, T; Nose, T; Ogino, F; Takebe, H; Unno, T, 1982
)
0.26
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID56273Change in the mean blood pressure and hypotensive action was measured in dogs at 10 mg/kg dose, 60 min after id administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID78076Maximum increase in the coronary flow of isolated guinea pig heart when a dose of 10 ug/heart is administered1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Organic phosphorus compounds. 2. Synthesis and coronary vasodilator activity of (benzothiazolylbenzyl) phosphonate derivatives.
AID77144Maximum increase in coronary flow in isolated guinea pig heart at a dose of 10 ug.1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID55904Coronary vasodilatory activity as increase in coronary blood flow was determined in dogs after i.v. administration of the compound1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators.
AID59550Compound was tested for max increase in blood flow through cicumflex branch of left coronary artery, 60 min after administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID211999Lethal effect after per os administration in mouse for 7 days1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators.
AID56266Change in the heart rate and hypotensive action was measured in dogs at 10 mg/kg dose, 120 min after id administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID59547Compound was tested for max increase in blood flow through cicumflex branch of left coronary artery, 120 min after administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID59583Coronary vasodilatory activity as increase in coronary flow was determined in dogs after 0.1 mg/kg i.v. administration of the compound; (SE +/- 5)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators.
AID79484Calcium antagonistic activity in isolated guinea pig Tenia coli specimens; (SE +/- 0.08)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators.
AID56272Change in the mean blood pressure and hypotensive action was measured in dogs at 10 mg/kg dose, 5 min after id administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID56270Change in the mean blood pressure and hypotensive action was measured in dogs at 10 mg/kg dose, 120 min after id administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID56267Change in the heart rate and hypotensive action was measured in dogs at 10 mg/kg dose, 30 min after id administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID59683Compound was tested for max increase in blood flow through circumflex branch of left coronary artery, 5 min after administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID56271Change in the mean blood pressure and hypotensive action was measured in dogs at 10 mg/kg dose, 30 min after id administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID134575LD50 value in mouse was calculated after the drug was administered intraperitoneally by Weil method1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID79656pA2 was measured as Calcium antagonistic activity 30 min after administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID56269Change in the heart rate and hypotensive action was measured in dogs at 10 mg/kg dose, 60 min after id administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID56268Change in the heart rate and hypotensive action was measured in dogs at 10 mg/kg dose, 5 min after id administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID59548Compound was tested for max increase in blood flow through cicumflex branch of left coronary artery, 30 min after administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator.
AID60139Ability to increase coronary blood flow after intra duodenal administration at 3 mg/kg in dog; (SE +/- 27)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-199023 (82.14)18.7374
1990's5 (17.86)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)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 (%)
Trials1 (3.33%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other29 (96.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]