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proadifen
Sign in to saveProadifen (SKF-525A) is a non-selective inhibitor of cytochrome P450 enzymes, preventing some types of drug metabolism. It is also an inhibitor of neuronal nitric oxide synthase (NOS), CYP-dependent (cytochrome P450-dependent) arachidonate metabolism, transmembrane calcium influx, and platelet thromboxane synthesis. Further documented effects include the blockade of ATP-sensitive inward rectifier potassium channel 8 (KIR6.1), and stimulation of endothelial cell prostacyclin production.
In the Vinony graph
Vinony's link graph records 321 inbound references to proadifen, and connects out to valproic acid, conotoxin and Hypericum perforatum.
It sits within the topics Carboxylate esters, Cytochrome P450 inhibitors and Diethylamino compounds.
Vinony links it to 5 Wikipedia language editions.
Chemical data
- Formula
- C23H31NO2
- Molecular weight
- 353.5 g/mol
- IUPAC name
- 2-(diethylamino)ethyl 2,2-diphenylpentanoate
via PubChem
Drug data · ChEMBL
- Max clinical phase
- Phase 2
- Molecule type
- Small molecule
via ChEMBL · EBI
Research
1,586 papers- Proadifen sensitizes resistant ovarian adenocarcinoma cells to cisplatin.Toxicology letters · 2016
- The local anaesthetics proadifen and adiphenine inhibit nicotinic receptors by different molecular mechanisms.British journal of pharmacology · 2009
- Proadifen-induced production of prostacyclin by equine peritoneal macrophages.American journal of veterinary research · 1989
- Inhibition of GSK-3β reverses the pro-apoptotic effect of proadifen (SKF-525A) in HT-29 colon adenocarcinoma cells.Toxicology in vitro : an international journal published in association with BIBRA · 2012
- Retrorsine.IARC monographs on the evaluation of the carcinogenic risk of chemicals to man · 1976
via PubMed
Wikidata facts
- Mass
- 353.235
Show 3 more facts
- chemical formula
- C₂₃H₃₁NO₂
- canonical SMILES
- CCCC(C1=CC=CC=C1)(C2=CC=CC=C2)C(=O)OCCN(CC)CC
- Commons category
- Proadifen
Sources (2)
via Wikidata · CC0
~1 min read
Encyclopedic overview
2 sectionsContents
- References
- External links
Proadifen (SKF-525A) is a non-selective inhibitor of cytochrome P450 enzymes, preventing some types of drug metabolism. It is also an inhibitor of neuronal nitric oxide synthase (NOS), CYP-dependent (cytochrome P450-dependent) arachidonate metabolism, transmembrane calcium influx, and platelet thromboxane synthesis. Further documented effects include the blockade of ATP-sensitive inward rectifier potassium channel 8 (KIR6.1), and stimulation of endothelial cell prostacyclin production.
Proadifen exerts apoptotic/anti-proliferate (tumour suppressing) effects in certain forms of cancer (HT-29 colon adenocarcinoma), believed to be caused by mediation of glycogen synthase kinase 3 β (GSK-3β). In the same study administration of proadifen was demonstrated to produce time- and dose-dependent phosphatidylserine externalization, caspase-3 activation and PARP cleavage. Intense upregulation of NAG-1 and ATF3 and downregulation of Mcl-1 and Egr-1 were also observed.
Excerpted from Wikipedia’s “proadifen” article, available under the CC BY-SA 4.0 licence.