Nelivaptan

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Nelivaptan
(IUPAC) ime
(2S,4R)-1-[(3R)-5-chloro-1-(2,4-dimethoxyphenyl)sulfonyl-3-(2-met​hoxyphenyl)-2-oxo-indolin-3-yl]-4-hydroxy-N,N-dimethyl-pyrrolidin​e-2-carboxamide
Klinički podaci
Identifikatori
CAS broj 439687-69-1
ATC kod  ?
PubChem[1][2] 9895468
ChemSpider[3] 8071134
Hemijski podaci
Formula C30H32ClN3O8S 
Mol. masa 630.11 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status
Način primene Oralno

Nelivaptan (INN[4]), kod SSR-149,415, je selektivni i oralno aktivni ne-peptidni antagonist vazopresinskog receptora koji je selektivan za V1b podtip.[5] Lek je bio u kliničkim ispitivanjima za tretman anksioznosti i depresija.[6] Jula 2008, Sanofi-Aventis je objavio da je dalji razvoj ovog leka obustavljen.[7]

Literatura[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. World Health Organization (2007). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 98" (PDF). WHO Drug Information 21 (4): 341. 
  5. Griebel G, Simiand J, Serradeil-Le Gal C, Wagnon J, Pascal M, Scatton B, Maffrand JP, Soubrie P (2002). "Anxiolytic- and antidepressant-like effects of the non-peptide vasopressin V1b receptor antagonist, SSR149415, suggest an innovative approach for the treatment of stress-related disorders". Proc. Natl. Acad. Sci. U.S.A. 99 (9): 6370–5. PMC 122955. PMID 11959912. doi:10.1073/pnas.092012099. 
  6. Serradeil-Le Gal C, Wagnon J, Tonnerre B, Roux R, Garcia G, Griebel G, Aulombard A (2005). "An overview of SSR149415, a selective nonpeptide vasopressin V(1b) receptor antagonist for the treatment of stress-related disorders". CNS drug reviews 11 (1): 53–68. PMID 15867952. doi:10.1111/j.1527-3458.2005.tb00035.x. 
  7. "Second-quarter 2008 results". Press Release. Sanofi-Aventis. 31. 07. 2008.. http://en.sanofi-aventis.com/binaries/20080731_results2008_Q2_CP_EN_tcm28-20271.pdf. pristupljeno 10. 06. 2009.. "It has been decided to discontinue the development of amibegron and SSR 149415 (a V1B receptor antagonist)." 

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