Nepicastat
| Nepicastat | |
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5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1,3-dihydro-2H-imidazole-2-thione |
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Other names
SYN-117 |
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| Identifiers | |
| CAS number | 173997-05-2  |
| PubChem | 9796181 |
| ChemSpider | 7971947 |
| MeSH | Nepicastat |
| Jmol-3D images | Image 1 |
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| Properties | |
| Molecular formula | C14H15F2N3S |
| Molar mass | 295.35 g/mol |
 (verify) (what is:  / ?)Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) |
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| Infobox references |
Nepicastat (INN, codenamed SYN117, RS-25560-197) is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.[1]
It has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated as such.[2] As of 2012, clinical trials to assess nepicastat as a treatment for post-traumatic stress disorder (PTSD) and cocaine dependence have been completed.[3][4]
[edit] Synthesis
[edit] References
- ^ 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. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1564872.
- ^ 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.
- ^ "Pharmacogenetic Clinical Trial of Nepicastat for Post Traumatic Stress Disorder (PTSD)". ClinicalTrials.gov. U.S. National Institutes of Health. June 4, 2008. http://www.clinicaltrials.gov/ct2/show/NCT00641511. 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. August 15, 2008. http://www.clinicaltrials.gov/ct2/show/NCT00656357. Retrieved on February 1, 2012.
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