Nepikastat

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Nepikastat
IUPAC ime
Drugi nazivi SYN-117
Identifikacija
CAS registarski broj 173997-05-2
PubChem[1][2] 9796181
ChemSpider[3] 7971947 DaY
MeSH Nepicastat
Jmol-3D slike Slika 1
Svojstva
Molekulska formula C14H15F2N3S
Molarna masa 295.35 g/mol

 DaY (šta je ovo?)   (verifikuj)

Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje (25 °C, 100 kPa) materijala

Infobox references

Nepikastat (INN) (SYN117, RS-25560-197) je enzimski inhibitor dopaminske beta hidroksilaze, enzima koji katalizuje konverziju dopamina u norepinefrin.[4]

On je je ispitan kao potencijalni lek kongestivno zatajenje srca, i pokazano je da je dobro tolerisan u toj ulozi.[5] 2012, Klinička ispitivanja koja su istraživala moguću primenu nepikastata u lečenju posttraumatskog stresnog poremećaja (PTSD) i kokainske zavisnosti su završena 2012.[6][7]

Sinteza[uredi | uredi kod]

Jedan od mogućih sintetičkih puteva je[8]:

Reference[uredi | uredi kod]

  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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  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. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Stanley WC, Li B, Bonhaus DW, et al. (August 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. DOI:10.1038/sj.bjp.0701315. PMC 1564872. PMID 9283721. 
  5. Hegde SS, Friday KF (December 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. 
  6. „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.
  7. „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.
  8. U.S. Patent 5.719.280

Spoljašnje veze[uredi | uredi kod]