Page last updated: 2024-11-11

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 SourceID
PubMed CID5362399
CHEMBL ID46765
SCHEMBL ID121664
MeSH IDM0172862

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.

ExcerptReferenceRelevance
"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

ExcerptReferenceRelevance
" 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

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC50 (µMol)0.30000.00002.072410.0000AID159204; AID159206
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC50 (µMol)0.30000.00031.990110.0000AID159204; AID159206
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesioncGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cellular response to insulin stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesion mediated by integrincGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of lipid catabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
oocyte maturationcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
lipid metabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
response to xenobiotic stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of meiotic nuclear divisioncGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of apoptotic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
steroid hormone mediated signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of oocyte developmentcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of ribonuclease activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to cGMPcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to transforming growth factor beta stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
apoptotic signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein kinase B bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
nuclear estrogen receptor activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
estrogen bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
endoplasmic reticulumcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
Golgi apparatuscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
guanyl-nucleotide exchange factor complexcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID229994Index of contractility was determined as the ratio of % of dP/dtmax in conscious dog after (po) administration of 0.10 mg/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID59676Effective dose required to increase the myocardial contractile force (CF) 50% above base line when administered intravenously.1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID57021Mean arterial blood pressure (MAP) in dog after intravenous dose of 0.075 mg/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID59626Percent change in activity 8 hr after peroral administration in conscious dog at 0.10 mg/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID59624Percent change in activity 8 hr after peroral administration in conscious dog at 0.01 mg/kg (Not determined)1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID22055750% increase in cardiac force in dog by intravenous dose1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Heteroatom analogues of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones.
AID22055550% increase in cardiac force in dog by id dose1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Heteroatom analogues of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones.
AID159204Inhibition of cardiac phosphodiesterase-3 isolated from canine heart.1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID59627Percent change in activity 8 hr after peroral administration in conscious dog at 0.30 mg/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID229996Index of contractility was determined as the ratio of % of dP/dtmax in conscious dog after (po) administration of a dose of 0.01 mg/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID57016Heart rate (HR) in dog after intravenous dose of 0.075 mg/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID229995Index of contractility was determined as the ratio of % of dP/dtmax in conscious dog after (po) administration of 0.30 mg/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID57027Myocardial contractile force (CF) in dog after intravenous dose of 0.075 mg/kg1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
AID159206Inhibition of canine cardiac Phosphodiesterase 31992Journal 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)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (100.00)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 (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]