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Nepikastat

С Википедије, слободне енциклопедије
Nepikastat
Nazivi
IUPAC naziv
5-(aminometil)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahidronaftalen-2-il]-1,3-dihidro-2H-imidazol-2-tion
Drugi nazivi
SYN-117
Identifikacija
3D model (Jmol)
ChemSpider
MeSH Nepicastat
  • Fc1cc3c(c(F)c1)CC[C@H](N2/C(=C\NC2=S)CN)C3
Svojstva
C14H15F2N3S
Molarna masa 295,35 g/mol
Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje materijala (na 25 °C [77 °F], 100 kPa).
ДаY verifikuj (šta je ДаYНеН ?)
Reference infokutije

Nepikastat (INN) (SYN117, RS-25560-197) je enzimski inhibitor dopaminske beta hidroksilaze, enzima koji katalizuje konverziju dopamina u norepinefrin.[3]

On je je ispitan kao potencijalni lek kongestivno zatajenje srca, i pokazano je da je dobro tolerisan u toj ulozi.[4] 2012, Klinička ispitivanja koja su istraživala moguću primenu nepikastata u lečenju posttraumatskog stresnog poremećaja (PTSD) i kokainske zavisnosti su završena 2012.[5][6]

Jedan od mogućih sintetičkih puteva je[7]:

  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.  уреди
  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. ^ Stanley WC; Li B; Bonhaus DW; et al. (1997). „Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase”. Br J Pharmacol. 121 (8): 1803—9. PMC 1564872Слободан приступ. PMID 9283721. doi:10.1038/sj.bjp.0701315. 
  4. ^ Hegde SS, Friday KF (1998). „Dopamine-beta-hydroxylase inhibition: a novel sympatho-modulatory approach for the treatment of congestive heart failure”. Current pharmaceutical design. 4 (6): 469—79. PMID 10197057. 
  5. ^ „Pharmacogenetic Clinical Trial of Nepicastat for Post Traumatic Stress Disorder (PTSD)”. ClinicalTrials.gov. U.S. National Institutes of Health. 4. 6. 2008.  Retrieved on February 1, 2012.
  6. ^ „Study of Safety and Potential Efficacy of SYN117 in Cocaine Dependent Volunteers”. ClinicalTrials.gov. U.S. National Institutes of Health. 15. 8. 2008.  Retrieved on February 1, 2012.
  7. ^ U.S. Patent 5.719.280

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