Nepikastat

Iz Wikipedije, slobodne enciklopedije
Idi na navigaciju Idi na pretragu
Nepikastat
Nepicastat.png
IUPAC ime
Drugi nazivi SYN-117
Identifikacija
CAS registarski broj 173997-05-2
PubChem[1][2] 9796181
ChemSpider[3] 7971947 YesY
MeSH Nepicastat
Jmol-3D slike Slika 1
Svojstva
Molekulska formula C14H15F2N3S
Molarna masa 295.35 g/mol

 YesY (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 - уреди | uredi izvor]

Jedan od mogućih sintetičkih puteva je[8]:

Nepicastat scheme.png

Reference[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. 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. PMC 1564872. PMID 9283721. doi:10.1038/sj.bjp.0701315. 
  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.. http://www.clinicaltrials.gov/ct2/show/NCT00641511.  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.. http://www.clinicaltrials.gov/ct2/show/NCT00656357.  Retrieved on February 1, 2012.
  8. U.S. Patent 5.719.280

Spoljašnje veze[uredi - уреди | uredi izvor]