Page last updated: 2024-12-11
bemoradan
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Description
bemoradan: RN & structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 5362399 |
| CHEMBL ID | 46765 |
| SCHEMBL ID | 121664 |
| MeSH ID | M0172862 |
Synonyms (33)
| Synonym |
|---|
| bemoradan |
| rwj-22867 |
| orf-22867 |
| bemoradan (usan/inn) |
| D03075 |
| 112018-01-6 |
| orf 22867 |
| CHEMBL46765 |
| AKOS000279097 |
| 7-(4-methyl-6-oxo-4,5-dihydro-1h-pyridazin-3-yl)-4h-1,4-benzoxazin-3-one |
| 2h-1,4-benzoxazin-3(4h)-one, 7-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)- |
| bemoradanum [inn-latin] |
| bemoradanum |
| 7-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)-2h-1,4-benzoxazin-3(4h)-one |
| g2s2v1etbq , |
| unii-g2s2v1etbq |
| bemoradan [usan:inn] |
| 6-(3,4-dihydo-3-oxo-1,4(2h)-benzoxazin-7-yl)-2,3,4,5-tetrahydro-5-methylpyridazin-3-one |
| 2h-1,4-benzoxazin-3(4h)-one, 7-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)-, (+-)- |
| 123169-88-0 |
| bemoradan [usan] |
| bemoradan [inn] |
| SCHEMBL121664 |
| 6-(3,4-dihydro-3-oxo-1,4(2h)-benzoxazin-7-yl)-2,3,4,5-tetrahydro-5-methylpyridazin-3-one |
| XZPGINPFWXLYNW-UHFFFAOYSA-N |
| 7-[(1,4,5,6-tetrahydro-4-methyl-6-oxopyridazin)-3-yl]-4h-1,4-benzoxazin-3(2h)-one |
| bdbm50228430 |
| Q27278659 |
| 7-(4-methyl-6-oxo-1,4,5,6-tetrahydropyridazin-3-yl)-2h-1,4-benzoxazin-3(4h)-one |
| DTXSID50869548 |
| AKOS040764860 |
| HY-153168 |
| CS-0653058 |
Research Excerpts
Overview
Bemoradan is a potent, long-acting orally active inodilator.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Bemoradan is a potent, long-acting orally active inodilator. " | ( Pharmacokinetics and bioavailability of bemoradan, a long-acting inodilator in healthy males. Abrams, LS; Brusser, L; Chien, SC; Huang, SM; Lasseter, K; Simon, D; Smith, IL, 1994) | 2 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " The pharmacokinetics and bioavailability of bemoradan were studied in twelve normal males following oral administration of single, ascending doses of the bemoradan HCL salt in capsules." | ( Pharmacokinetics and bioavailability of bemoradan, a long-acting inodilator in healthy males. Abrams, LS; Brusser, L; Chien, SC; Huang, SM; Lasseter, K; Simon, D; Smith, IL, 1994) | 0.82 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (2)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) | IC50 (µMol) | 0.3000 | 0.0000 | 2.0724 | 10.0000 | AID159204; AID159206 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) | IC50 (µMol) | 0.3000 | 0.0003 | 1.9901 | 10.0000 | AID159204; AID159206 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (24)
Molecular Functions (9)
Ceullar Components (5)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| endoplasmic reticulum | cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) |
| Golgi apparatus | cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) |
| cytosol | cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) |
| membrane | cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) |
| guanyl-nucleotide exchange factor complex | cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) |
| cytosol | cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) |
| membrane | cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) |
| cytosol | cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (14)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID229994 | Index of contractility was determined as the ratio of % of dP/dtmax in conscious dog after (po) administration of 0.10 mg/kg | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID59676 | Effective dose required to increase the myocardial contractile force (CF) 50% above base line when administered intravenously. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID57021 | Mean arterial blood pressure (MAP) in dog after intravenous dose of 0.075 mg/kg | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID59626 | Percent change in activity 8 hr after peroral administration in conscious dog at 0.10 mg/kg | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID59624 | Percent change in activity 8 hr after peroral administration in conscious dog at 0.01 mg/kg (Not determined) | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID220557 | 50% increase in cardiac force in dog by intravenous dose | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Heteroatom analogues of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones. |
| AID220555 | 50% increase in cardiac force in dog by id dose | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Heteroatom analogues of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones. |
| AID159204 | Inhibition of cardiac phosphodiesterase-3 isolated from canine heart. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID59627 | Percent change in activity 8 hr after peroral administration in conscious dog at 0.30 mg/kg | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID229996 | Index of contractility was determined as the ratio of % of dP/dtmax in conscious dog after (po) administration of a dose of 0.01 mg/kg | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID57016 | Heart rate (HR) in dog after intravenous dose of 0.075 mg/kg | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID229995 | Index of contractility was determined as the ratio of % of dP/dtmax in conscious dog after (po) administration of 0.30 mg/kg | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID57027 | Myocardial contractile force (CF) in dog after intravenous dose of 0.075 mg/kg | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents. |
| AID159206 | Inhibition of canine cardiac Phosphodiesterase 3 | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | Heteroatom analogues of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (7)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (100.00) | 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 | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 8 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||