Page last updated: 2024-12-08

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 Source	ID
PubMed CID	431850
CHEMBL ID	2106970
SCHEMBL ID	18585
MeSH ID	M0061105

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

Excerpt	Reference	Relevance
"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" Adverse drug reactions were reported in 14 patients and 5 of them were withdrawn from the trial for only non serious reactions."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

Excerpt	Reference	Relevance
" 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

Excerpt	Reference	Relevance
" 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 ID	Title	Year	Journal	Article
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
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]
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' 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]
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
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]
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
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' 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]
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]
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]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (26)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	20 (76.92)	18.7374
1990's	6 (23.08)	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	9 (33.33%)	5.53%
Reviews	2 (7.41%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	16 (59.26%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
adenine [no description available]	1.95	1	0	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
chlorine chloride : A halide anion formed when chlorine picks up an electron to form an an anion.	1.97	1	0	halide anion; monoatomic chlorine	cofactor; Escherichia coli metabolite; human metabolite
histamine [no description available]	6.97	1	0	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
theophylline [no description available]	8.36	1	1	dimethylxanthine	adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent
astemizole Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.	8.36	1	1	benzimidazoles; piperidines	anti-allergic agent; anticoronaviral agent; H1-receptor antagonist
ketotifen Ketotifen: A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.. ketotifen : An organic heterotricyclic compound that is 4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one which is substituted at position 4 by a 1-methylpiperidin-4-ylidene group. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is used (usually as its hydrogen fumarate salt) for the treatment of asthma, where it may take several weeks to exert its full effect.	5.01	5	2	cyclic ketone; olefinic compound; organic heterotricyclic compound; organosulfur heterocyclic compound; piperidines; tertiary amino compound	anti-asthmatic drug; H1-receptor antagonist
pyrilamine Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.. mepyramine : An ethylenediamine derivative that is ethylenediamine in which one of the amino nitrogens is substituted by two methyl groups and the remaining amino nitrogen is substituted by a 4-methoxybenzyl and a pyridin-2-yl group.	1.97	1	0	aromatic ether; ethylenediamine derivative	H1-receptor antagonist
terfenadine Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.	8.36	1	1	diarylmethane
trifluoperazine [no description available]	1.97	1	0	N-alkylpiperazine; N-methylpiperazine; organofluorine compound; phenothiazines	antiemetic; calmodulin antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor; phenothiazine antipsychotic drug
alpha-aminopyridine alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.	1.97	1	0
barium chloride barium chloride: RN given refers to parent cpd. barium chloride : The inorganic dichloride salt of barium.	6.97	1	0	barium salt; inorganic chloride	potassium channel blocker
cromolyn sodium Cromolyn Sodium: A chromone complex that acts by inhibiting the release of chemical mediators from sensitized MAST CELLS. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack.. disodium cromoglycate : An organic sodium salt that is the disodium salt of cromoglycic acid.	3.07	1	0	organic sodium salt	anti-asthmatic drug; drug allergen
glucose, (beta-d)-isomer beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.	2.37	2	0	D-glucopyranose	epitope; mouse metabolite
p-methoxy-n-methylphenethylamine p-Methoxy-N-methylphenethylamine: A potent mast cell degranulator. It is involved in histamine release.. N,O-dimethyltyramine : A secondary amino compound that is tyramine in which the hydrogen of the phenolic hydroxy group has been replaced by a methyl group.	1.97	1	0	aromatic ether; secondary amino compound	metabolite
1-hexadecyl-2-acetyl-glycero-3-phosphocholine Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.. 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine : A 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has hexadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis.	1.97	1	0	2-acetyl-1-alkyl-sn-glycero-3-phosphocholine	antihypertensive agent; beta-adrenergic antagonist; bronchoconstrictor agent; hematologic agent; vasodilator agent
n-formylmethionine leucyl-phenylalanine N-Formylmethionine Leucyl-Phenylalanine: A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated.. N-formyl-L-methionyl-L-leucyl-L-phenylalanine : A tripeptide composed of L-Met, L-Leu and L-Phe in a linear sequence with a formyl group at the amino terminus. It acts as a potent inducer of leucocyte chemotaxis and macrophage activator as well as a ligand for the FPR receptor.	1.97	1	0	tripeptide
barium Barium: An element of the alkaline earth group of metals. It has an atomic symbol Ba, atomic number 56, and atomic weight 138. All of its acid-soluble salts are poisonous.	6.97	1	0	alkaline earth metal atom; elemental barium
warfarin Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.	9.51	26	9	benzenes; hydroxycoumarin; methyl ketone

Condition	Relationship Strength	Studies	Trials
Anaphylactic Reaction [description not available]	3.29	2	0
Bronchospasm [description not available]	3.29	2	0
Allergic Conjunctivitis [description not available]	2.89	1	0
Eosinophilia, Tropical [description not available]	2.89	1	0
Allergic Reaction [description not available]	3.8	4	0
Anaphylaxis An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death.	3.29	2	0
Bronchial Spasm Spasmodic contraction of the smooth muscle of the bronchi.	3.29	2	0
Conjunctivitis, Allergic Conjunctivitis due to hypersensitivity to various allergens.	2.89	1	0
Eosinophilia Abnormal increase of EOSINOPHILS in the blood, tissues or organs.	2.89	1	0
Hypersensitivity Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.	3.8	4	0
Extravascular Hemolysis [description not available]	1.97	1	0
Hemolysis The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.	1.97	1	0
Asthma, Bronchial [description not available]	5.37	5	3
Cataract, Membranous [description not available]	3.36	1	1
Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).	5.37	5	3
Cataract Partial or complete opacity on or in the lens or capsule of one or both eyes, impairing vision or causing blindness. The many kinds of cataract are classified by their morphology (size, shape, location) or etiology (cause and time of occurrence). (Dorland, 27th ed)	3.36	1	1
Adjuvant Arthritis [description not available]	1.97	1	0
Pink Eye [description not available]	1.97	1	0
Anasarca [description not available]	1.97	1	0
Granulomas [description not available]	1.97	1	0
Conjunctivitis INFLAMMATION of the CONJUNCTIVA.	1.97	1	0
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	1.97	1	0
Granuloma A relatively small nodular inflammatory lesion containing grouped mononuclear phagocytes, caused by infectious and noninfectious agents.	1.97	1	0
Cirrhosis, Liver [description not available]	3.36	1	1
Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.	8.36	1	1
Hay Fever [description not available]	4.97	3	3
Sneezing The sudden, forceful, involuntary expulsion of air from the NOSE and MOUTH caused by irritation to the MUCOUS MEMBRANES of the upper RESPIRATORY TRACT.	3.36	1	1
Rhinitis, Allergic, Seasonal Allergic rhinitis that occurs at the same time every year. It is characterized by acute CONJUNCTIVITIS with lacrimation and ITCHING, and regarded as an allergic condition triggered by specific ALLERGENS.	4.97	3	3
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	1.97	1	0

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