8-Fenilteofilin

8-Fenilteofilin
(IUPAC) ime
8-fenil-1,3-dimetil-7H-purin-2,6-dion
Klinički podaci
Identifikatori
CAS broj 961-45-5
ATC kod nije dodeljen
PubChem[1][2] 1922
ChemSpider[3] 1846
ChEMBL[4] CHEMBL62350 DaY
Hemijski podaci
Formula C13H12N4O2 
Mol. masa 256,259 g/mol
SMILES eMolekuli & PubHem
InChI
InChI=1S/C13H12N4O2/c1-16-11-9(12(18)17(2)13(16)19)14-10(15-11)8-6-4-3-5-7-8/h3-7H,1-2H3,(H,14,15) DaY
Key: PJFMAVHETLRJHJ-UHFFFAOYSA-N DaY
Farmakoinformacioni podaci
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Pravni status

8-Fenilteofilin (8-fenil-1,3-dimetilksantin, 8-PT) je lek iz ksantinske familije koji deluje kao potentan i selektivan antagonist adenozinskih receptora A1 i A2A, ali za razliku od drugih derivata ksantina on nije inhibitor fosfodiesteraze.[5][6][7] On ima stimulantno dejstvo u životinjskim studijama i sličnu potentnost sa kofeinom.[8] 8-Fenilteofilin je isto tako potentan i selektivan inhibitor jetrenog enzima CYP1A2 zbog čeka je verovatno da uzrokuje nepoželjne interakcije sa drugim lekovima koje CYP1A2 normalno metaboliše.[9]

Reference

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. Scotini E, Carpenedo F, Fassina G (February 1983). „New derivatives of methyl-xanthines: effect of thiocaffeine thiotheophylline and 8-phenyltheophylline on lipolysis and on phosphodiesterase activities”. Pharmacological Research Communications 15 (2): 131–43. PMID 6844374. 
  6. Rabe KF, Magnussen H, Dent G (April 1995). „Theophylline and selective PDE inhibitors as bronchodilators and smooth muscle relaxants”. The European Respiratory Journal : Official Journal of the European Society for Clinical Respiratory Physiology 8 (4): 637–42. PMID 7664866. 
  7. Howell LL, Morse WH, Spealman RD (September 1990). „Respiratory effects of xanthines and adenosine analogs in rhesus monkeys”. The Journal of Pharmacology and Experimental Therapeutics 254 (3): 786–91. PMID 2395111. 
  8. Spealman RD (1988). „Psychomotor stimulant effects of methylxanthines in squirrel monkeys: relation to adenosine antagonism”. Psychopharmacology 95 (1): 19–24. PMID 3133696. 
  9. Murray S, Odupitan AO, Murray BP, Boobis AR, Edwards RJ (March 2001). „Inhibition of human CYP1A2 activity in vitro by methylxanthines: potent competitive inhibition by 8-phenyltheophylline”. Xenobiotica 31 (3): 135–51. DOI:10.1080/00498250110043292. PMID 11465391. 

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Receptorski ligandi
2-(1-Heksinil)-N-metiladenozin • 2-Cl-IB-MECA • 2'-MeCCPA • 5'-N-etilkarboksamidoadenozin • ATL-146e • BAY 60-6583 • CCPA • CGS-21680 • CP-532,903 • GR 79236 • LUF-5835 • LUF-5845 • N6-Ciklopentiladenozin • Regadenoson • SDZ WAG 994 • UK-432,097
Antagonisti
8-Fenil-1,3-dipropilksantin • Acefilin • Aminofilin • Bamifilin • Kofein • CGS-15943 • 8-Hloroteofilin • CPX • CVT-6883 • Dimetazan • DPCPX • Fenetilin • Istradefilin • KF-26777 • MRE3008F20 • MRS-1220 • MRS-1334 • MRS-1706 • MRS-1754 • MRS-3777 • Paraksantin • Pentoksifilin • Preladenant • Propentofilin • PSB-10 • PSB-11 • PSB 36 • PSB-603 • PSB-788 • PSB-1115 • Rolofilin • SCH-442,416 • SCH-58261 • Teobromin • Teofilin • VUF-5574 • ZM-241,385
Inhibitori preuzimanja
ENT inhibitori
VNT inhibitori