Proadifen

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Proadifen
Proadifen.png
Names
IUPAC name
2-Diethylaminoethyl 2,2-diphenylpentanoate
Other names
SKF 525-A
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
UNII
Properties
C23H31NO2
Molar mass 353.51 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

Proadifen (SKF-525A) is a non-selective inhibitor of cytochrome P450 enzymes, preventing some types of drug metabolism.[1] 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.[2]

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.[3]

Proadifen has been demonstrated to inhibit the nicotinic acetylcholine receptor (NAChR) and muscarinic acetylcholine receptor (MAChR) in rats.[4]

References[edit]

  1. ^ Marshall, FN; Williamson, HE (1964). "Natruretic Response During Infusion of Beta-Diethylaminoethyl-Diphenylpropyl Acetate Hydrocloride (Skf 525-A)". The Journal of Pharmacology and Experimental Therapeutics. 143: 395–400. PMID 14161153. 
  2. ^ "Santa Cruz Biotech". 
  3. ^ University in Košice, Slovakia; Institute of Biology and Ecology: Rastislav Jendzelovsky, Jan Koval, Jaromír Mikeš, Zuzana Jendzelovska, Jana Plsikova, and Peter Fedoročko (June 2012). "Inhibition of GSK-3β reverses the pro-apoptotic effect of proadifen (SKF-525A) in HT-29 colon adenocarcinoma cells". Toxicology in Vitro. 
  4. ^ "Santa Cruz Biotech".