Page last updated: 2024-12-06

proxicromil

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

Description

Proxicromil is a synthetic cromone derivative with anti-inflammatory and anti-allergic properties. It is thought to work by inhibiting the release of histamine and other inflammatory mediators from mast cells. Proxicromil is used to treat allergic rhinitis, a condition that causes inflammation of the nasal passages. It is also used to prevent asthma attacks. Proxicromil is available as a nasal spray and oral tablet. Research on proxicromil focuses on its potential to treat other inflammatory conditions, such as inflammatory bowel disease and rheumatoid arthritis.'

proxicromil: RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65493
CHEMBL ID42641
SCHEMBL ID371474
MeSH IDM0074235

Synonyms (22)

Synonym
60400-92-2
D05645
proxicromil (usan/inn)
proxicromil
4h-naphtho(2,3-b)pyran-2-carboxylic acid, 6,7,8,9-tetrahydro-5-hydroxy-4-oxo-10-propyl-
proxicromilum [inn-latin]
6,7,8,9-tetrahydro-5-hydroxy-4-oxo-10-propyl-4h-naphtho(2,3-b)pyran-2-carboxylic acid
CHEMBL42641
proxicromilum
proxicromil [usan:inn:ban]
8wwz0e633p ,
unii-8wwz0e633p
proxicromil [mart.]
6,7,8,9-tetrahydro-5-hydroxy-4-oxo-10-propyl-4h-naphtho[2,3-b]pyran-2-carboxylic acid
proxicromil [usan]
proxicromil [inn]
VFFTVZUIDYJUQS-UHFFFAOYSA-N
5-hydroxy-4-oxo-10-propyl-6,7,8,9-tetrahydro-4h-naphtho[2,3-b]pyran-2-carboxylic acid
SCHEMBL371474
DTXSID10209163
5-hydroxy-4-oxo-10-propyl-6,7,8,9-tetrahydro-4h-benzo[g]chromene-2-carboxylic acid
Q27271143

Research Excerpts

Overview

Proxicromil is a compound shown in biological tests to have anti-allergic properties.

ExcerptReferenceRelevance
"Proxicromil is a compound shown in biological tests to have anti-allergic properties. "( The effect of proxicromil, a new oral chromone derivative, in antigen challenge tests is asthmatic patients.
Girard, JP; Sullivan, TJ, 1980
)
2.06

Effects

ExcerptReferenceRelevance
"Proxicromil has not direct activity on the development of immune responsiveness but appear to suppress the expression of delayed hypersensitivity and immune complex mediated hypersensitivity reactions by virtue and its anti-inflammatory properties."( The activity of an anti-allergic compound, proxicromil, on models of immunity and inflammation.
Blackham, A; Bundick, RV; Cunnington, PG; Jenkins, SN; Keogh, RW; Orr, TS, 1981
)
1.25

Bioavailability

ExcerptReferenceRelevance
" It is well absorbed in humans after oral administration."( The effect of proxicromil, a new oral chromone derivative, in antigen challenge tests is asthmatic patients.
Girard, JP; Sullivan, TJ, 1980
)
0.62

Dosage Studied

ExcerptRelevanceReference
" Proxicromil was administered for two consecutive 3-week periods using a dosage regimen of 18 mg twice per day for the first period followed by 18 mg four times per day for the second period."( Clinical study of a new orally active chromone in asthma-proxicromil (FPL 57787).
Dahl, R, 1980
)
1.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)30.00000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID76735Percent inhibition of bronchospasm in vivo for a dose of 5 mg/kg in guinea pig1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Antiallergy agents. 1. Substituted 1,8-naphthyridin-2(1H)-ones as inhibitors of SRS-A release.
AID76732Percent inhibition of bronchospasm administered intravenously at a dose of 5 mg/kg in guinea pig1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Antiallergy agents. 1. Substituted 1,8-naphthyridin-2(1H)-ones as inhibitors of SRS-A release.
AID1123018Antiallergic activity in po dosed human assessed as concentration required to inhibit antigen-induced clinical asthma1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Development of ethyl 3,4-dihydro-4-oxopyrimido[4,5-b]quinoline-2-carboxylate, a new prototype with oral antiallergy activity.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1123017Antiallergic activity in po dosed rat assessed as inhibition of antigen-induced passive cutaneous anaphylaxis relative to DSCG1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Development of ethyl 3,4-dihydro-4-oxopyrimido[4,5-b]quinoline-2-carboxylate, a new prototype with oral antiallergy activity.
AID1123012Antiallergic activity in po dosed rat assessed as inhibition of antigen-induced passive cutaneous anaphylaxis1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Development of ethyl 3,4-dihydro-4-oxopyrimido[4,5-b]quinoline-2-carboxylate, a new prototype with oral antiallergy activity.
AID78133In vitro Schultz-Dale Test against isolated guinea pig lung strips repeatedly challenged with antigen in the presence of an antihistamine (H1) at a concentration 30 uM.1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Acidic furo[3,2-b]indoles. A new series of potent antiallergy agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-199024 (85.71)18.7374
1990's3 (10.71)18.2507
2000's0 (0.00)29.6817
2010's1 (3.57)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 (%)
Trials7 (24.14%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (75.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]