| 词条 | Proadifen |
| 释义 |
| ImageFile=Proadifen.png | ImageSize= | IUPACName=2-Diethylaminoethyl 2,2-diphenylpentanoate | OtherNames=SKF 525-A |Section1={{Chembox Identifiers | CASNo=302-33-0 | PubChem=4910 | ChemSpiderID = 4741 | ChEMBL = 282567 | SMILES = O=C(OCCN(CC)CC)C(c1ccccc1)(c2ccccc2)CCC | StdInChI = 1S/C23H31NO2/c1-4-17-23(20-13-9-7-10-14-20,21-15-11-8-12-16-21)22(25)26-19-18-24(5-2)6-3/h7-16H,4-6,17-19H2,1-3H3 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = A510CA4CBT |Section2={{Chembox Properties | C=23 | H=31 | N=1 | O=2 | Appearance= | Density= | MeltingPt= | BoilingPt= | Solubility= |Section3={{Chembox Hazards | MainHazards= | FlashPt= | AutoignitionPt = }}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.[2] References1. ^{{cite journal | pmid = 14161153 | year = 1964 | last1 = Marshall | first1 = FN | last2 = Williamson | first2 = HE | title = Natruretic Response During Infusion of Beta-Diethylaminoethyl-Diphenylpropyl Acetate Hydrocloride (Skf 525-A) | volume = 143 | pages = 395–400 | journal = The Journal of Pharmacology and Experimental Therapeutics}} {{Navboxes2. ^1 {{cite web|url=http://www.scbt.com/datasheet-200492-skf-525a-hcl-proadifen.html|author= |title = Proadifen hydrochloride (CAS 62-68-0) |website=Santa Cruz Biotech}} 3. ^{{cite journal | vauthors = Jendželovský R, Koval J, Mikeš J, Papčová Z, Plšíková J, Fedoročko P | title = Inhibition of GSK-3β reverses the pro-apoptotic effect of proadifen (SKF-525A) in HT-29 colon adenocarcinoma cells | journal = Toxicol In Vitro | volume = 26 | issue = 6 | pages = 775–82 | date = September 2012 | pmid = 22683934 | doi = 10.1016/j.tiv.2012.05.014 }} | title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Acetylcholine receptor modulators}}{{Ion channel modulators}}{{Nitric oxide signaling modulators}}{{Sigma receptor modulators}}{{Xenobiotic-sensing receptor modulators}} }} 2 : Valerates|Cytochrome P450 inhibitors |
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