Page last updated: 2024-12-05

furegrelate

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

Description

furegrelate: structure given in UD 35:175:d [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3437
CHEMBL ID1204948
CHEBI ID103833
SCHEMBL ID10953582
MeSH IDM0119203

Synonyms (46)

Synonym
BRD-K55529781-236-02-0
DIVK1C_000255
KBIO1_000255
SPECTRUM_000041
SPECTRUM5_001141
BSPBIO_002492
IDI1_000255
KBIO2_005557
KBIO2_002989
KBIOSS_000421
KBIOGR_001266
KBIO2_000421
KBIO3_001712
NINDS_000255
SPECTRUM2_001444
SPECTRUM4_000793
SPECTRUM3_000786
SPBIO_001307
LOPAC0_000515
furegrelate
85666-24-6
2-benzofurancarboxylic acid, 5-(3-pyridinylmethyl)-
5-(pyridin-3-ylmethyl)-1-benzofuran-2-carboxylic acid
CHEBI:103833
furegrelato
unii-kx4d9bza6x
kx4d9bza6x ,
furegrelato [spanish]
furegarelatum
furegarelatum [latin]
furegrelate [inn]
5-(pyridin-3-ylmethyl)benzofuran-2-carboxylic acid
5-(3-pyridylmethyl)-2-benzofurancarboxylate
5-(3-pyridylmethyl)-2-benzofurancarboxylic acid
CHEMBL1204948
DTXSID7046960
SCHEMBL10953582
5-(3-pyridinylmethyl)-2-benzofurancarboxylic acid
VHWFITPGPFLBGT-UHFFFAOYSA-N
Q27180995
AKOS030555586
FT-0768019
u-63557a (free acid)
SDCCGSBI-0050499.P003
HY-106080
CS-0024808

Research Excerpts

Overview

Furegrelate sodium is a thromboxane synthetase inhibitor with potential for the treatment of various diseases including hypertension, thrombosis, and renal disorders.

ExcerptReferenceRelevance
"Furegrelate sodium is a thromboxane synthetase inhibitor with potential for the treatment of various diseases including hypertension, thrombosis, and renal disorders. "( Pharmacokinetics of furegrelate after oral administration to normal humans.
Friis, JM; Lakings, DB; Lunan, CM; Mohrland, JS; VanderLugt, JT, 1989
)
2.04

Treatment

ExcerptReferenceRelevance
"Furegrelate treatment starting in an established stage of nephritis had no effect."( Changes in glomerular thromboxane A2 receptor expression and ligand binding following immune injury.
Bresnahan, BA; Dufek, S; Lianos, EA; Wu, S, 1999
)
1.02

Toxicity

ExcerptReferenceRelevance
" Indomethacin alone had no adverse effect on glomerular function; however, when coadministered with CsA an exaggerated decrease in renal function was observed."( Modulation of experimental cyclosporine nephrotoxicity by inhibition of thromboxane synthesis.
Freeman, D; Keown, P; McDonald, J; Petric, R; Stiller, C; Wallace, C, 1990
)
0.28

Pharmacokinetics

ExcerptReferenceRelevance
" Preliminary pharmacokinetic and bioavailability evaluations in the dog indicate that 1 was rapidly distributed and had a terminal half-life of 132 min after an intravenous dose."( Liquid chromatographic-ultraviolet methods for furegrelate in serum and urine: preliminary pharmacokinetic evaluation in the dog.
Friis, JM; Lakings, DB, 1985
)
0.53

Bioavailability

ExcerptReferenceRelevance
" Preliminary pharmacokinetic and bioavailability evaluations in the dog indicate that 1 was rapidly distributed and had a terminal half-life of 132 min after an intravenous dose."( Liquid chromatographic-ultraviolet methods for furegrelate in serum and urine: preliminary pharmacokinetic evaluation in the dog.
Friis, JM; Lakings, DB, 1985
)
0.53

Dosage Studied

ExcerptRelevanceReference
" Furegrelate (800 or 1600 mg) significantly inhibited thromboxane synthesis throughout the dosing interval as assessed by thromboxane B2 generation from platelet-rich plasma challenged with arachidonic acid or from serum."( Multiple dose trial of the thromboxane synthase inhibitor furegrelate in normal subjects.
Lakings, DB; Mohrland, JS; Vander Lugt, JT, 1990
)
1.43
" A study of the dose-response relationship for CsA at 3, 6, and 24 mg/kg/day for 5 days indicated that maximal blood pressure responses were attained with 6 mg/kg/day."( Cyclosporine-induced hypertension in sheep. The role of thromboxanes.
Bennett, WM; Scoggins, BA; Tresham, JJ; Whitworth, JA, 1990
)
0.28
" dosing regimen, no apparent change in the absorption, disposition, and elimination kinetics is detected and only a slight potential for drug accumulation is observed."( Pharmacokinetics of furegrelate after oral administration to normal humans.
Friis, JM; Lakings, DB; Lunan, CM; Mohrland, JS; VanderLugt, JT, 1989
)
0.6
" Thus, these experiments suggest that thromboxane synthetase inhibition, within a narrow dosage range, potentiates furosemide-induced renin release while cyclooxygenase inhibition suppresses it."( Effect of cyclooxygenase and thromboxane synthetase inhibition on furosemide-stimulated plasma renin activity.
Datar, S; McCauley, FA; Wilson, TW, 1987
)
0.27
" Treatment involved oral dosing (10 mg/kg bid) of TSI or placebo, combined with local treatment of the graft with TSI or placebo (papavarine) at the time of implantation."( Effect of selective thromboxane synthetase inhibitor on vein grafts.
Askins, R; Cargile, M; Hebeler, RF; Neyman, SL; O'Leary, JP, 1987
)
0.27
" Fasted dogs dosed orally with the drug in solution or capsule had similar absorption and elimination kinetics and agreed favorably with the intravenous results."( Liquid chromatographic-ultraviolet methods for furegrelate in serum and urine: preliminary pharmacokinetic evaluation in the dog.
Friis, JM; Lakings, DB, 1985
)
0.53
" The observed increase in time to occlusion was abolished when celecoxib was administered to animals dosed with HDA-ER (80."( Effects of selective cyclooxygenase-2 inhibition on vascular responses and thrombosis in canine coronary arteries.
Barrett, TD; Crofford, LJ; Driscoll, EM; Hennan, JK; Huang, J; Lucchesi, BR; Park, AM; Willens, DE, 2001
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzofurans
[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]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (105)

TimeframeStudies, This Drug (%)All Drugs %
pre-199041 (39.05)18.7374
1990's27 (25.71)18.2507
2000's27 (25.71)29.6817
2010's8 (7.62)24.3611
2020's2 (1.90)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 14.75

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 Index14.75 (24.57)
Research Supply Index4.72 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (14.75)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (1.83%)5.53%
Reviews1 (0.92%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other106 (97.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]