Page last updated: 2024-12-06
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 Source | ID |
|---|---|
| PubMed CID | 53421 |
| CHEMBL ID | 39516 |
| SCHEMBL ID | 612913 |
| MeSH ID | M0109825 |
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
| Excerpt | Reference | Relevance |
|---|---|---|
| "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
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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
| Excerpt | Relevance | Reference |
|---|---|---|
| " 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 ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID56273 | Change in the mean blood pressure and hypotensive action was measured in dogs at 10 mg/kg dose, 60 min after id administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID78076 | Maximum increase in the coronary flow of isolated guinea pig heart when a dose of 10 ug/heart is administered | 1989 | Journal of medicinal chemistry, Jul, Volume: 32, Issue:7 | Organic phosphorus compounds. 2. Synthesis and coronary vasodilator activity of (benzothiazolylbenzyl) phosphonate derivatives. |
| AID77144 | Maximum increase in coronary flow in isolated guinea pig heart at a dose of 10 ug. | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID55904 | Coronary vasodilatory activity as increase in coronary blood flow was determined in dogs after i.v. administration of the compound | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators. |
| AID59550 | Compound was tested for max increase in blood flow through cicumflex branch of left coronary artery, 60 min after administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID211999 | Lethal effect after per os administration in mouse for 7 days | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators. |
| AID56266 | Change in the heart rate and hypotensive action was measured in dogs at 10 mg/kg dose, 120 min after id administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID59547 | Compound was tested for max increase in blood flow through cicumflex branch of left coronary artery, 120 min after administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID59583 | Coronary vasodilatory activity as increase in coronary flow was determined in dogs after 0.1 mg/kg i.v. administration of the compound; (SE +/- 5) | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators. |
| AID79484 | Calcium antagonistic activity in isolated guinea pig Tenia coli specimens; (SE +/- 0.08) | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators. |
| AID56272 | Change in the mean blood pressure and hypotensive action was measured in dogs at 10 mg/kg dose, 5 min after id administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID56270 | Change in the mean blood pressure and hypotensive action was measured in dogs at 10 mg/kg dose, 120 min after id administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID56267 | Change in the heart rate and hypotensive action was measured in dogs at 10 mg/kg dose, 30 min after id administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID59683 | Compound was tested for max increase in blood flow through circumflex branch of left coronary artery, 5 min after administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID56271 | Change in the mean blood pressure and hypotensive action was measured in dogs at 10 mg/kg dose, 30 min after id administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID134575 | LD50 value in mouse was calculated after the drug was administered intraperitoneally by Weil method | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID79656 | pA2 was measured as Calcium antagonistic activity 30 min after administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID56269 | Change in the heart rate and hypotensive action was measured in dogs at 10 mg/kg dose, 60 min after id administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID56268 | Change in the heart rate and hypotensive action was measured in dogs at 10 mg/kg dose, 5 min after id administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID59548 | Compound was tested for max increase in blood flow through cicumflex branch of left coronary artery, 30 min after administration | 1986 | Journal of medicinal chemistry, May, Volume: 29, Issue:5 | Organic phosphorus compounds. 1. 4-(Benzothiazol-2-yl)benzylphosphonate as potent calcium antagonistic vasodilator. |
| AID60139 | Ability to increase coronary blood flow after intra duodenal administration at 3 mg/kg in dog; (SE +/- 27) | 1990 | Journal 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)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 23 (82.14) | 18.7374 |
| 1990's | 5 (17.86) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (3.33%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 29 (96.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||