Tasosartan

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Tasosartan
(IUPAC) ime
2,4-dimetil-8[2'-(1H-tetrazol-5-il)bifenil-4-il]metil5,8-dihidropirido[2,3-d]pirimidin-7(6H)-on
Klinički podaci
Identifikatori
CAS broj 145733-36-4
ATC kod C09CA05
PubChem[1][2] 60919
DrugBank DB01349
ChemSpider[3] 54890
UNII 48G92V856H YesY
Hemijski podaci
Formula C23H21N7O 
Mol. masa 411,459 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Withdrawn

Tasosartan je antagonist angiotenzin II receptora.

Proizvođač je ovaj lek povukao sa FDA pregleda nakon što su klinička ispitivanja faze III pokazala povišene transaminaze (znak moguće hepatotoksičnosti) kod znatnog broja učestnika.[4][5]

Osobine[uredi - уреди | uredi izvor]

Osobina Vrednost
Broj akceptora vodonika 6
Broj donora vodonika 1
Broj rotacionih veza 4
Particioni koeficijent[6] (ALogP) 3,1
Rastvorljivost[7] (logS, log(mol/L)) -5,9
Polarna površina[8] (PSA, Å2) 100,6

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. Atkinson AJ et al. (2007). Principles of clinical pharmacology. Amsterdam: Elsevier. str. 515. ISBN 0-12-369417-5. 
  5. Dina R, Jafari M (July 2000). "Angiotensin II-receptor antagonists: an overview". Am J Health Syst Pharm 57 (13): 1231–41. PMID 10902066. 
  6. Ghose, A.K., Viswanadhan V.N., and Wendoloski, J.J. (1998). "Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods". J. Phys. Chem. A 102: 3762–3772. doi:10.1021/jp980230o. 
  7. Tetko IV, Tanchuk VY, Kasheva TN, Villa AE. (2001). "Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices". Chem Inf. Comput. Sci. 41: 1488–1493. PMID 11749573. doi:10.1021/ci000392t.  edit
  8. Ertl P., Rohde B., Selzer P. (2000). "Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties". J. Med. Chem. 43: 3714–3717. PMID 11020286. doi:10.1021/jm000942e.  edit

Literatura[uredi - уреди | uredi izvor]

Spoljašnje veze[uredi - уреди | uredi izvor]

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