Nepikastat
Nepikastat (INN) (SYN117, RS-25560-197) je enzimski inhibitor dopaminske beta hidroksilaze, enzima koji katalizuje konverziju dopamina u norepinefrin.[3]
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| Nazivi | |
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| IUPAC naziv
5-(aminometil)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahidronaftalen-2-il]-1,3-dihidro-2H-imidazol-2-tion
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| Drugi nazivi
SYN-117
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| Identifikacija | |
3D model (Jmol)
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| ChemSpider | |
| MeSH | Nepicastat |
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| 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). | |
 verifikuj (šta je   ?)
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| Reference infokutije | |
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]
Sinteza
уредиJedan od mogućih sintetičkih puteva je[7]:
Reference
уреди- ^ 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.
- ^ 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.
- ^ 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 1564872
. PMID 9283721. doi:10.1038/sj.bjp.0701315.
- ^ 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.
- ^ „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.
- ^ „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.
- ^ U.S. Patent 5.719.280
