Nepicastat
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Preferred IUPAC name 5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1,3-dihydro-2H-imidazole-2-thione | |
Other names SYN-117 | |
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MeSH | Nepicastat |
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Properties | |
Chemical formula | C14H15F2N3S |
Molar mass | 295.35 g/mol |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Y verify (what is YN ?) 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] In Phase 2 study treatment with nepicastat was not effective in relieving PTSD-associated symptoms when compared to placebo. The study was funded by the U.S. Department of Defense.[5]
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.
- ^ 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. 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. Retrieved on February 1, 2012.
- ^ Biotie reports top-line data from clinical study with nepicastat (SYN117) in post-traumatic stress disorder BIOTIE THERAPIES CORP. STOCK EXCHANGE RELEASE 27 December 2012.
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(dopamine, epinephrine,
norepinephrine)
PAHTooltip Phenylalanine hydroxylase |
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THTooltip Tyrosine hydroxylase |
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DBHTooltip Dopamine beta-monooxygenase |
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PNMTTooltip Phenylethanolamine N-methyltransferase |
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COMTTooltip Catechol-O-methyl transferase |
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(serotonin, melatonin)
TPHTooltip Tryptophan hydroxylase |
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AANATTooltip Serotonin N-acetyl transferase |
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ASMTTooltip Acetylserotonin O-methyltransferase |
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HDCTooltip Histidine decarboxylase |
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HNMTTooltip Histamine N-methyltransferase |
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DAOTooltip Diamine oxidase |
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This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it. |
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