Konivaptan
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(IUPAC) ime
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N-(4-(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin- 6(1H)-yl)carbonyl)phenyl)- (1,1'-biphenyl)-2-carboxamide
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Klinički podaci
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Identifikatori
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CAS broj
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210101-16-9
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ATC kod
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C03XA02 [1]
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PubChem[2][3]
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151171
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ChemSpider[4]
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133239
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UNII
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0NJ98Y462X Y
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ChEMBL[5]
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CHEMBL1755
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Hemijski podaci
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Formula
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C32H26N4O2
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Mol. masa
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498.583
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SMILES
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eMolekuli & PubHem
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InChI |
InChI=1S/C32H26N4O2/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37) Y Key: IKENVDNFQMCRTR-UHFFFAOYSA-N Y |
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Farmakokinetički podaci
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Bioraspoloživost
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N/A
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Farmakoinformacioni podaci
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Trudnoća
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?
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Pravni status
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Način primene
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intravenous
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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.
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
- ↑ 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. edit
- ↑ 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. edit
- ↑ 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
- ↑ 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.
Vanjske veze
Šablon:Diuretici
Šablon:Neuropeptidni ligandi