Konivaptan |
(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 |
Klinički podaci |
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Identifikatori |
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CAS broj | 210101-16-9 |
ATC kod | C03XA02[1] |
PubChem[2][3] | 151171 |
ChemSpider[4] | 133239 |
UNII | 0NJ98Y462X Y |
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ChEMBL[5] | CHEMBL1755 |
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Hemijski podaci |
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Formula | C32H26N4O2 |
Mol. masa | 498.583 |
SMILES | eMolekuli &PubHem |
InChI |
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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 | N/A |
Farmakoinformacioni podaci |
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Trudnoća | ? |
Pravni status | |
Način primene | intravenous |
Konivaptan (YM 087,Vaprisol) je nepeptidni inhibitorantidiuretskog hormona (antagonistvazopresinskog receptora). On je odobren2004 zahiponatremiju (niske nivoe krvnognatrijuma) uzrokovanesindromom neodgovarajućeg izlučivanja antidiuretskog hormona (SIADH), i postoji evidencija da je efektivan u lečenju zatajenja srca.
Konivaptan inhibira dva od tri podtipavazopresinskog receptora (V1a iV2).
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]
- ↑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 izoriginala 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.
Šablon:DiureticiŠablon:Neuropeptidni ligandi