Page last updated: 2024-11-06

torbafylline

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

Description

Torbafylline is a synthetic compound with a chemical structure similar to theophylline. It is a selective phosphodiesterase 4 (PDE4) inhibitor. PDE4 inhibitors have been studied for their potential therapeutic effects in treating inflammatory and respiratory diseases. Torbafylline has been shown to exhibit anti-inflammatory effects in animal models, suggesting potential for treating conditions like asthma and chronic obstructive pulmonary disease (COPD). The mechanism of action involves inhibiting the breakdown of cyclic adenosine monophosphate (cAMP), leading to increased cAMP levels within cells, which in turn modulate various cellular processes involved in inflammation. Despite promising preclinical results, torbafylline has not yet been approved for clinical use. Ongoing research aims to evaluate its safety and efficacy in human trials.'

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

Cross-References

ID SourceID
PubMed CID65888
CHEMBL ID2104934
SCHEMBL ID93832
MeSH IDM0169987

Synonyms (18)

Synonym
torbafylline
7-(ethoxymethyl)-1-(5-hydroxy-5-methylhexyl)-3-methylpurine-2,6-dione
105102-21-4
unii-65o78f9t1w
torbafilina [spanish]
torbafylline [inn]
7-(ethoxymethyl)-1-(5-hydroxy-5-methylhexyl)-3-methylxanthine
torbafilina
torbafyllinum
65o78f9t1w ,
torbafyllinum [latin]
CHEMBL2104934
SCHEMBL93832
7-ethoxymethyl-1-(5-hydroxy-5-methylhexyl)-3-methylxanthine
QSXXLDDWVCEBFP-UHFFFAOYSA-N
2-(3-(trifluoromethyl)anilino)nicotinicacid
DTXSID00146952
Q27263900

Research Excerpts

Treatment

Torbafylline treatment had little further effect on ischemic muscles subjected to mild stimulation. It did significantly increase the capillary per fibre ratio in extensor digitorum longus.

ExcerptReferenceRelevance
"Torbafylline treatment had little further effect on ischemic muscles subjected to mild stimulation, which on its own improved functional hyperemia, resistance to fatigue, and the capillaries per fibre ratio in tibialis anterior, although it did significantly increase the capillary per fibre ratio in extensor digitorum longus."( Effect of torbafylline on muscle blood flow, performance, and capillary supply in ischemic muscles subjected to varying levels of activity.
Brown, MD; Egginton, S; Hudlicka, O; Okyayuz-Baklouti, I, 1994
)
1.41
"Torbafylline treatment nearly doubled perfusion in the glycolytic regions (Cp:Ct = 0.216 +/- 0.137) and nearly quadrupled it in oxidative (Cp:Ct = 0.121 +/- 0.151) regions of ischaemic muscles."( Regional capillary perfusion in muscles with limited blood supply: effects of torbafylline.
Egginton, S; Hudlicka, O, 1992
)
1.23
"3. Torbafylline treatment caused an increased LDH activity in intact fast muscles and decreased it in soleus, although the relative capacity for anaerobic and aerobic metabolism (indicated by the ratio of LDH and CS activities) remained unchanged in all cases."( The effect of torbafylline on enzyme activities in fast and slow muscles with limited blood supply.
Egginton, S; Hudlická, O, 1991
)
1.16
"Treatment with torbafylline for one week did not change the weight of the vascular casts."( Collateral circulation in skeletal muscles: effect of pentoxifylline and torbafylline.
Hudlicka, O; Torres, SH, 1990
)
0.85

Dosage Studied

ExcerptRelevanceReference
" Similarly, 14-day dosing of torbafylline resulted in a 3-fold decrease in urinary protein excretion."( Role of neutrophils and macrophages in experimental nephrosis of the rat.
Berens, KL; Luke, DR; Verani, RR, 1998
)
0.59
[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)304.90000.11007.190310.0000AID1449628
[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 (1)

Assay IDTitleYearJournalArticle
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (32)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (9.38)18.7374
1990's24 (75.00)18.2507
2000's3 (9.38)29.6817
2010's2 (6.25)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 (%)
Trials1 (3.13%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other31 (96.88%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]