8-Fenilteofilin

Из Википедије, слободне енциклопедије
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[уреди]

  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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