Konivaptan

Konivaptan
(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
PubChem	151171
ChemSpider	133239
UNII	0NJ98Y462X
ChEMBL	CHEMBL1755
Hemijski podaci
Formula	C32H26N4O2
Mol. masa	498.583
SMILES	eMolekuli & PubHem
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) ; Key: IKENVDNFQMCRTR-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	N/A
Farmakoinformacioni podaci
Trudnoća	?
Pravni status
Način primene	intravenous

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 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. 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.

Spoljašnje veze uredi

	Portal Medicina
	Portal Hemija

Šablon:Diuretici Šablon:Neuropeptidni ligandi

[1] 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.

[2] 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

[3] 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.

[4] 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

[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] 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.

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