flestolol: short-acting beta blockader [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 55885 |
| CHEMBL ID | 7467 |
| SCHEMBL ID | 611921 |
| MeSH ID | M0137965 |
| Synonym |
|---|
| flestolol |
| flestololum [latin] |
| flestolol [french,spanish] |
| benzoic acid, 2-fluoro-, 3-((2-((aminocarbonyl)amino)-1,1-dimethylethyl)amino)-2-hydroxypropyl ester |
| flestolol [inn] |
| CHEMBL7467 |
| [3-[[1-(carbamoylamino)-2-methylpropan-2-yl]amino]-2-hydroxypropyl] 2-fluorobenzoate |
| 87721-62-8 |
| unii-li02075e1w |
| flestololum |
| li02075e1w , |
| benzoic acid, 2-fluoro-, 3-((2-((aminocarbonyl)amino)-1,1-dimethylethyl)amino)-2-hydroxypropyl ester, (+/-)- |
| o-fluorobenzoic acid, 3-ester with (+/-)-(2-((2,3-dihydroxypropyl)amino)-2-methylpropyl)urea |
| 91697-99-3 |
| SCHEMBL611921 |
| Q15634013 |
| benzoic acid, 2-fluoro-, 3-((2-((aminocarbonyl)amino)-1,1-dimethylethyl)amino)-2-hydroxypropyl ester, (+)- |
| 100511-22-6 |
| V8FW2XAC43 |
| 39WX8P569M , |
| (-)-3-((2-((aminocarbonyl)amino)-1,1-dimethylethyl)amino)-2-hydroxypropyl 2-fluorobenzoate |
| benzoic acid, 2-fluoro-, 3-((2-((aminocarbonyl)amino)-1,1-dimethylethyl)amino)-2-hydroxypropyl ester, (-)- |
| flestolol, (-)- |
| flestolol, (+)- |
| unii-39wx8p569m |
| DTXSID60868981 |
| 3-{[1-(carbamoylamino)-2-methylpropan-2-yl]amino}-2-hydroxypropyl 2-fluorobenzoate |
Flestolol (ACC-9089) is a nonselective, competitive, ultra-short-acting beta-adrenergic blocking agent, without any intrinsic sympathomimetic activity. It has a half-life of 6.9 minutes.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Flestolol (ACC-9089) is a nonselective, competitive, ultra-short-acting beta-adrenergic blocking agent, without any intrinsic sympathomimetic activity. " | ( Flestolol: an ultra-short-acting beta-adrenergic blocking agent. Barton, SD; Burge, J; Laddu, AR; Turlapaty, P, 1986) | 3.16 |
| "Flestolol is an ultrashort-acting beta-blocking drug with a half-life of 6.9 minutes. " | ( Electropharmacology of flestolol for supraventricular tachycardia without associated structural heart disease. Blake, K; Franz, MR; Laddu, A; Liem, LB; Peterson, J; Swerdlow, C, 1987) | 2.03 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Flestolol has an extremely short half-life, demonstrated by an 83% loss of effect within 25 min." | ( Effects of flestolol, an ultra-short acting beta-adrenoceptor antagonist, on hemodynamic changes produced by treadmill exercise or isoprenaline stimulation in conscious dogs. Fischer, G; Grohs, JG; Raberger, G, 1990) | 1.39 |
| "Flestolol has an extremely short half-life, demonstrated by an 83% loss of effect within 25 min." | ( Effects of flestolol, an ultra-short acting beta-adrenoceptor antagonist, on hemodynamic changes produced by treadmill exercise or isoprenaline stimulation in conscious dogs. Fischer, G; Grohs, JG; Raberger, G, 1990) | 1.39 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Flestolol did not cause any significant change (P greater than .05) in the heart rate or systolic or diastolic blood pressure from the baseline." | ( Pharmacokinetics and pharmacodynamics of flestolol, a new short-acting, beta-adrenergic receptor antagonist. Achari, R; Bell, V; Drissel, D; Hulse, JD; Laddu, A; Matier, WL; Turlapaty, P, 1987) | 1.26 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with flestolol did not affect the total number of beats, the number of normal and ectopic beats, and the arrhythmic ratio, i.e." | ( Effects of beta-adrenoceptor antagonism upon delayed reperfusion arrhythmias in conscious dogs. Krejcy, K; Krumpl, G; Raberger, G; Todt, H, 1991) | 0.62 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The only adverse effect seen was hypotension in 2 patients." | ( Safety and efficacy of flestolol, a new ultrashort-acting beta-adrenergic blocking agent, for supraventricular tachyarrhythmias. Burge, J; Katz, RJ; Keefe, D; Laddu, AR; Somberg, JC; Steinberg, JS, 1986) | 0.58 |
Flestolol shifted the dose-response curves of isoprenaline-induced changes in heart rate, positive left ventricular dp/dtmax, and diastolic arterial pressure dose dependently to the right. Its main effect during exercise was a decrease in positive left Ventricular dP/dt max.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Flestolol shifted the dose-response curves of isoprenaline-induced changes in heart rate, positive left ventricular dp/dtmax, and diastolic arterial pressure dose dependently to the right, while its main effect during exercise was a decrease in positive left ventricular dP/dtmax." | ( Effects of flestolol, an ultra-short acting beta-adrenoceptor antagonist, on hemodynamic changes produced by treadmill exercise or isoprenaline stimulation in conscious dogs. Fischer, G; Grohs, JG; Raberger, G, 1990) | 1.58 |
| " Second, if adverse effects are experienced, reducing the dosage or terminating the infusion results in rapid reversal of its pharmacological effects." | ( Controlled beta-receptor blockade with esmolol and flestolol. Frishman, WH; Murthy, VS, 1988) | 0.53 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Beta-2 adrenergic receptor | Homo sapiens (human) | Kd | 0.0079 | 0.0000 | 0.6288 | 8.9130 | AID41154 |
| Beta-1 adrenergic receptor | Homo sapiens (human) | Kd | 0.0079 | 0.0001 | 0.8039 | 10.0000 | AID41154 |
| Beta-3 adrenergic receptor | Homo sapiens (human) | Kd | 0.0079 | 0.0001 | 0.7631 | 8.9130 | AID41154 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID58407 | Time taken for 80% recovery at a dose of 1 microg (3-h infusion period) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID22765 | t1/2 in canine liver | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID41156 | In vitro blocking of beta adrenergic receptor in guinea pig trachea | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
| AID60894 | Percent inhibition of isoproterenol induced tachycardia at a dose of 1 microg (3-h infusion period) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID41154 | In Vitro inhibition of the beta adrenergic receptor in guinea pig atria | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID22764 | T1/2 in canine blood | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID233866 | Selectivity determined by expression 10[pA2(atria) - pA2 (trachea)] in guinea pig | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 18 (81.82) | 18.7374 |
| 1990's | 4 (18.18) | 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] | ||
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.
| This Compound (11.00) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (8.33%) | 5.53% |
| Reviews | 2 (8.33%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 20 (83.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||