8-Fenilteofilin

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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 YesY
Hemijski podaci
Formula C13H12N4O2 
Mol. masa 256,259 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
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[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. PMID 20331846. doi:10.1186/1758-2946-2-3.  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. PMID 21948594. doi:10.1093/nar/gkr777.  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. PMID 11465391. doi:10.1080/00498250110043292. 

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