Konivaptan
Konivaptan (YM 087, Vaprisol) je nepeptidni inhibitor antidiuretskog hormona (antagonist vazopresinskog receptora). On je odobren 2004 za hiponatremiju (niske nivoe krvnog natrijuma) uzrokovane sindromom neodgovarajućeg izlučivanja antidiuretskog hormona (SIADH), i postoji evidencija da je efektivan u lečenju zatajenja srca.
(IUPAC) ime | |||
---|---|---|---|
N-(4-(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin- 6(1H)-yl)carbonyl)phenyl)- (1,1'-biphenyl)-2-carboxamide | |||
Klinički podaci | |||
Identifikatori | |||
CAS broj | 210101-16-9 | ||
ATC kod | C03XA02 [1] | ||
PubChem[2][3] | 151171 | ||
ChemSpider[4] | 133239 | ||
UNII | 0NJ98Y462X | ||
ChEMBL[5] | CHEMBL1755 | ||
Hemijski podaci | |||
Formula | C32H26N4O2 | ||
Mol. masa | 498.583 | ||
SMILES | eMolekuli & PubHem | ||
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Farmakokinetički podaci | |||
Bioraspoloživost | N/A | ||
Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status | |||
Način primene | intravenous |
Konivaptan inhibira dva od tri podtipa vazopresinskog receptora (V1a i V2).
FDA nije odobrila konivaptan za lečenje dekompenziranog kongestivnog zatajenja srca. U teoriji antagonisti vazopresinskog receptora bi trebalo da budu posebno korisni kod takvog oboljenja, i inicijalne studije ukazuju da je to moguća oblast primene.[6]
Reference
uredi- ↑ WHO International Working Group for Drug Statistics Methodology (27. 08. 2008.). „ATC/DDD Classification (FINAL): New ATC 5th level codes”. WHO Collaborating Centre for Drug Statistics Methodology. Arhivirano iz originala na datum 2008-05-06. Pristupljeno 05. 09. 2008.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ Udelson JE, Smith WB, Hendrix GH, et al. (November 2001). „Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure”. Circulation 104 (20): 2417–23. DOI:10.1161/hc4501.099313. PMID 11705818.