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picumast

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

Description

picumast: RN & NM refer to di-HCl [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID431850
CHEMBL ID2106970
SCHEMBL ID18585
MeSH IDM0061105

Synonyms (16)

Synonym
picumast
7-(3-(4-(p-chlorobenzyl)-1-piperazinyl)propoxy)-3,4-dimethylcoumarin
picumast [inn:ban]
7-[3-[4-[(4-chlorophenyl)methyl]piperazin-1-yl]propoxy]-3,4-dimethylchromen-2-one
AKOS005066633
CHEMBL2106970
39577-19-0
unii-125267oauf
125267oauf ,
picumast [mart.]
picumast [mi]
2h-1-benzopyran-2-one, 7-(3-(4-((4-chlorophenyl)methyl)-1-piperazinyl)propoxy)-3,4-dimethyl-
picumast [inn]
SCHEMBL18585
DTXSID20192693
Q27251372

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"A double-masked study was performed to investigate a possible side effect of the antiallergic substance Picumast dihydrochloride on lens transparency."( Lens safety study with Picumast dihydrochloride--a double masked study using the Scheimpflug method.
Goder, G; Hockwin, O; Laser, H; Meinel, U; Messinger, D; Müller-Breitenkamp, U, 1990
)
0.8
" Adverse drug reactions were reported in 14 patients and 5 of them were withdrawn from the trial for only non serious reactions."( Acceptability, safety and efficacy of picumast dihydrochloride on long-term use in patients with perennial bronchial asthma.
Boerner, D; Eberhardt, R; Metz, K, 1989
)
0.55

Pharmacokinetics

ExcerptReferenceRelevance
" After intravenous administration of 10 mg picumast dihydrochloride a peak concentration of 182 ng/ml was achieved at the end of the 1 h infusion."( Pharmacokinetics of picumast dihydrochloride and its active metabolites M1 and M2 in humans.
Besenfelder, E; Dahmen, W; Kaufmann, B; Mosberg, H; Neugebauer, G; Nieder, N; Ponton, T; Wittenbrink-Dix, AM; Woelke-Seidl, E, 1989
)
0.86

Bioavailability

ExcerptReferenceRelevance
" In dogs the bioavailability of the parent compound was 14%, the absorption of radioactivity 68%."( Pharmacokinetics of picumast after administration of 14C-picumast dihydrochloride in dogs, rats, rabbits and monkeys.
Besenfelder, E; Boehm, E; Neubert, P; Roesch, A; Schaumann, W; Sterz, H, 1989
)
0.6
"The pharmacokinetics of picumast dihydrochloride (3,4-dimethyl-7-[4-(4-chlorobenzyl)piperazine-1-yl]propoxycoumarin dihydrochloride) and the pharmacodynamically active metabolites M1 and M2 as well as the absolute bioavailability of picumast dihydrochloride have been studied in healthy volunteers after oral administration of the drug in doses which were considerably higher than therapeutically used."( Pharmacokinetics of picumast dihydrochloride and its active metabolites M1 and M2 in humans.
Besenfelder, E; Dahmen, W; Kaufmann, B; Mosberg, H; Neugebauer, G; Nieder, N; Ponton, T; Wittenbrink-Dix, AM; Woelke-Seidl, E, 1989
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (19)

Assay IDTitleYearJournalArticle
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079931Moderate 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]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079935Cytolytic 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]
AID1079933Acute 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
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079938Chronic 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]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079936Choleostatic 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]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (26)

TimeframeStudies, This Drug (%)All Drugs %
pre-199020 (76.92)18.7374
1990's6 (23.08)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 (%)
Trials9 (33.33%)5.53%
Reviews2 (7.41%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (59.26%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]