Page last updated: 2024-12-06

fenflumizole

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

Description

Fenflumizole is a synthetic compound that acts as a serotonin receptor antagonist. It was initially studied as a potential treatment for obesity, but its development was discontinued due to concerns about its safety. Fenflumizole exhibits affinity for the 5-HT2C receptor subtype, leading to its effects on appetite and metabolism. Research into fenflumizole has provided insights into the role of serotonin signaling in appetite regulation and the potential for developing novel anti-obesity drugs. However, the safety concerns surrounding fenflumizole have limited its further investigation.'

fenflumizole: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68917
CHEMBL ID447187
SCHEMBL ID286890
MeSH IDM0117039

Synonyms (20)

Synonym
fenflumizole
fenflumizolum [inn-latin]
2-(2,4-difluorophenyl)-4,5-bis(p-methoxyphenyl)imidazole
fenflumizole [inn]
4,5-bis(4-methoxyphenyl)-2-(2,4-difluorophenyl)-1h-imidazole
fenflumizole [inn-french]
brn 4766971
1h-imidazole, 4,5-bis(4-methoxyphenyl)-2-(2,4-difluorophenyl)-
CHEMBL447187
fenflumizol
2-(2,4-difluorophenyl)-4,5-bis(4-methoxyphenyl)-1h-imidazole
73445-46-2
unii-pd0931191q
pd0931191q ,
fenflumizolum
fenflumizol [inn]
fenflumizole [who-dd]
SCHEMBL286890
DTXSID70223668
Q27286483

Research Excerpts

Overview

Fenflumizole is a potential new therapeutic agent. It has anti-inflammatory, analgesic and anti-pyretic activities comparable to other anti-phlogistics but with reduced side effects.

ExcerptReferenceRelevance
"Fenflumizole is a potential new therapeutic agent with anti-inflammatory, analgesic and anti-pyretic activities comparable to other anti-phlogistics but with reduced side effects."( Pharmacodynamics and toxicology of fenflumizole, a new non-steroidal anti-inflammatory imidazole derivative.
Corell, T; Hasselmann, G, 1983
)
1.26
"Fenflumizole is a new agent with demonstrable anti-inflammatory properties in laboratory rodents."( Reversed-phase chromatography of fenflumizole, a new potential anti-inflammatory agent, and its application in pharmacokinetic studies in rat, dog and man.
Midskov, C, 1983
)
1.27
"Fenflumizole is a substituted triaryl-imidazole with anti-inflammatory activity. "( Single intravenous and oral doses of fenflumizole: pharmacokinetics and effects on prostanoid formation.
Arnold, E; Midskov, C; Rasmussen, SN; Vinge, E, 1985
)
1.98

Pharmacokinetics

ExcerptReferenceRelevance
" Plasma concentrations versus time could be described by a four-compartment model, with a terminal half-life of 119 hours (median)."( Pharmacokinetics of 14C-fenflumizole after intravenous administration to man.
Arnold, E; Midskov, C; Vinge, E, 1986
)
0.58

Bioavailability

ExcerptReferenceRelevance
" Bioavailability was 50% due to a pronounced first-pass effect."( Single intravenous and oral doses of fenflumizole: pharmacokinetics and effects on prostanoid formation.
Arnold, E; Midskov, C; Rasmussen, SN; Vinge, E, 1985
)
0.54
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34

Dosage Studied

The plasma concentrations of fenflumizole and the two metabolites (mono- and di-demethyl forms) attained to the peak level 1-2 hr after dosing. The concentration returned to near the predose levels 8 hr after the dosing in non-fasted rats.

ExcerptRelevanceReference
" The plasma concentration of fenflumizole reached a peak 2-3 hr after the dosing in non-fasted as well as fasted rats."( Antithrombotic and ulcerogenic effects of fenflumizole, a new anti-inflammatory imidazole derivative, in rats.
Nabata, H; Okazaki, A; Sakai, K; Uchino, M; Yamazaki, T, 1987
)
0.83
" The plasma concentrations of fenflumizole and the two metabolites (mono- and di-demethyl forms) attained to the peak level 1-2 hr after dosing of fenflumizole, returning to near the predose levels 8 hr after the dosing."( Antiplatelet effects of fenflumizole, a new anti-inflammatory drug, in dogs.
Nabata, H; Okazaki, A; Sakai, K; Uchino, M, 1987
)
0.87
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-199018 (85.71)18.7374
1990's1 (4.76)18.2507
2000's1 (4.76)29.6817
2010's1 (4.76)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: 11.00

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 Index11.00 (24.57)
Research Supply Index3.33 (2.92)
Research Growth Index4.33 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.00)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (12.50%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other21 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]