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Aliskiren

Izvor: Wikipedija
Aliskiren
(IUPAC) ime
(2S,4S,5S,7S)-5-amino-N-(2-karbamoil-2,2-dimetiletil)-4-hidroksi-7[4-metoksi-3-(3-metoksipropoksi)fenil]metil8-metil-2-(propan-2-il)nonanamid
Klinički podaci
AHFS/Drugs.comMonografija
MedlinePlusa607039
Identifikatori
CAS broj173334-57-1
ATC kodC09XA02
C09XA52 (saHCT)
PubChem[1][2]5493444
DrugBankDB01258
ChemSpider[3]4591452
UNII502FWN4Q32 DaY
KEGG[4]D03208 DaY
ChEBICHEBI:601027 DaY
ChEMBL[5]CHEMBL1639 DaY
Hemijski podaci
FormulaC30H53N3O6 
Mol. masa551,758 g/mol
SMILESeMolekuli &PubHem
InChI
InChI=1S/C30H53N3O6/c1-19(2)22(14-21-10-11-26(38-8)27(15-21)39-13-9-12-37-7)16-24(31)25(34)17-23(20(3)4)28(35)33-18-30(5,6)29(32)36/h10-11,15,19-20,22-25,34H,9,12-14,16-18,31H2,1-8H3,(H2,32,36)(H,33,35)/t22-,23-,24-,25-/m0/s1 DaY
Key: UXOWGYHJODZGMF-QORCZRPOSA-N DaY
Farmakokinetički podaci
Bioraspoloživostniska (oko 2,5%)
MetabolizamHepatički,CYP3A4-posredovano
Poluvreme eliminacije24 sata
IzlučivanjeRenalno
Farmakoinformacioni podaci
Licenca

EU EMEA:link, US FDA:link

Trudnoća?
Pravni statusPOM (UK)℞-only (SAD)
Način primenePO (oralno)

Aliskiren (Tekturna (SAD);Rasilez (UK i druge zemlje)) prvi je u klasi lekova koji se nazivaju direktnimreninskim inhibitorima. Njegova trenutna licencirana indikacija jeprimarna hipertenzija.

Aliskiren su razvila preduzećaNovartis iSpeedel.[6][7] On je odobren u SAD2007. za tretman primarne hipertenzije.

Osobine

[uredi |uredi kod]
OsobinaVrednost
Broj akceptora vodonika7
Broj donora vodonika4
Broj rotacionih veza19
Particioni koeficijent[8] (ALogP)3,3
Rastvorljivost[9] (logS, log(mol/L))-7,5
Polarna površina[10] (PSA,Å2)146,1

Reference

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  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. ↑Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. ↑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
  6. ↑Gradman A, Schmieder R, Lins R, Nussberger J, Chiang Y, Bedigian M (2005). „Aliskiren, a novel orally effectiverenin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients”. Circulation 111 (8): 1012–8. DOI:10.1161/01.CIR.0000156466.02908.ED. PMID 15723979. 
  7. ↑Straessen JA, Li Y, and Richart T (2006). „Oral Renin Inhibitors”. Lancet 368 (9545): 1449–56. DOI:10.1016/S0140-6736(06)69442-7. PMID 17055947. 
  8. ↑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. 
  9. ↑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. DOI:10.1021/ci000392t. PMID 11749573. 
  10. ↑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. DOI:10.1021/jm000942e. PMID 11020286. 

Vanjske veze

[uredi |uredi kod]
Portal Medicina
Portal Hemija
Antihipertenzivi: Lekovi koji deluju narenin-angiotenzin sistem (C09)
AKE inhibitori/
("-pril")
AIIRAi/
("-sartan")
Renin inhibitori/
("-kiren")
Izvor:https://sh.wikipedia.org/w/index.php?title=Aliskiren&oldid=42281163
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