Page last updated: 2024-11-08

desmethylazelastine

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

Description

desmethylazelastine: azelastine metabolite [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID162558
CHEMBL ID2074921
CHEBI ID197264
SCHEMBL ID2820100
MeSH IDM0152997

Synonyms (27)

Synonym
desmethylazelastine
47491-38-3
1(2h)-phthalazinone, 4-((4-chlorophenyl)methyl)-2-(hexahydro-1h-azepin-4-yl)-
FT-0666081
CHEBI:197264
2-(azepan-4-yl)-4-[(4-chlorophenyl)methyl]phthalazin-1-one
4-(4-chlorobenzyl)-2-(perhydroazepinyl-(4))-1(2h)-phthalazinone
8w9sob28q4 ,
unii-8w9sob28q4
bdbm50420234
CHEMBL2074921 ,
4-[(4-chlorophenyl)methyl]-2-(hexahydro-1h-azepin-4-yl)-1(2h)-phthalazinone
n-desmethyl azelastine
demethylazelastine
4-(4-chlorobenzyl)-2-(hexahydroazepin-4-yl)-1-(2h)-phthalazinone
4-[(4-chlorophenyl)methyl]-2-(hexahydro-1h-azepin-4-yl)-l (2h)-phthalazinone
WRYCMIFVXDQIKN-UHFFFAOYSA-N
SCHEMBL2820100
2-(azepan-4-yl)-4-(4-chlorobenzyl)phthalazin-1(2h)-one
n-desmethylazelastine
AKOS030254511
DTXSID10963859
2-(azepan-4-yl)-4-[(4-chlorophenyl)methyl]phthalazin-1(2h)-one
Q27271119
4-[(4-chlorophenyl)methyl]-2-(hexahydro-1h-azepin-4-yl)-1(2h)-phthalazinone;demethylazelastine
HY-147336
CS-0566420

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" For pharmacokinetic modeling, the mean concentrations of AZ and DAZ in plasma were converted to those in blood."( Pharmacokinetics of azelastine and its active metabolite, desmethylazelastine, in guinea pigs.
Adusumalli, VE; Kucharczyk, N; Sofia, RD; Wong, KK,
)
0.38
" The peak concentration (Cmax) of AZ, especially after the first dose, was significantly higher in pediatric dogs than that in adult dogs, whereas following the multiple AZ administrations, the bioavailability parameters for the last dose were similar in the two age groups."( Pharmacokinetics of the new antiasthma and antiallergy drug, azelastine, in pediatric and adult beagle dogs.
Adusumalli, VE; Kucharczyk, N; Sofia, RD; Wichmann, JK; Wong, KK, 1993
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
phthalazines
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)26.80000.00022.318510.0000AID679131; AID679132
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (17)

Processvia Protein(s)Taxonomy
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID679132TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells2001European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Feb, Volume: 12, Issue:4
Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport.
AID679131TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.025 uM) in MDR1-expressing LLC-PK1 cells2001European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Feb, Volume: 12, Issue:4
Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport.
[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-19901 (14.29)18.7374
1990's3 (42.86)18.2507
2000's2 (28.57)29.6817
2010's1 (14.29)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.35

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.

MetricThis Compound (vs All)
Research Demand Index12.35 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.35)

All Compounds (24.57)

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%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]