Nepicastat (SYN-117) HCl

Catalog No.S2695

Nepicastat (SYN-117) HCl Chemical Structure

Molecular Weight(MW): 331.81

Nepicastat (SYN-117) HCl is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Phase 2.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Nepicastat (SYN-117) HCl is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Phase 2.
Targets
Bovine dopamine-beta-hydroxylase [1] Human dopamine-beta-hydroxylase [1]
8.5 nM 9 nM
In vitro

In vitro, Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity with IC50 of 8.5 nM and 9.0 nM, respectively. While Nepicastat hydrochloride has negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. [1]

In vivo In the artery, left ventricle and cerebral cortex of spontaneously hypertensive rats (SHRs), Nepicastat hydrochloride reduces noradrenaline content, and increases dopamine content and dopamine/noradrenaline ratio in a dose-dependent manner. In addition, Nepicastat hydrochloride also produces the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. [1] In inactin-anesthetized SHRs, Nepicastat hydrochloride (3 mg/kg, i.v.) produces the antihypertensive effects and causes a significant decrease in renal vascular resistance (38%) and an increase in renal blood flow (22%). [2] In dogs with chronic heart failure, low-dose Nepicastat hydrochloride (0.5 mg/kg) prevents left ventricular (LV) dysfunction and remodeling, and combination therapy of Nepicastat hydrochloride and enalapril results in additional improvements in all morphological features. [3] In rat brain, Nepicastat hydrochloride at a dose of 50 mg/kg ( i.p.) leads to the reduction of norepinephrine (NE) and blocks cocaine-primed reinstatement of cocaine seeking. [4]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Spontaneously hypertensive rats (SHRs).
  • Formulation: Nepicastat hydrochloride is dissolved in distilled water.
  • Dosages: ≤100 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (198.9 mM)
Water <1 mg/mL
Ethanol <1 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 331.81
Formula

C14H15F2N3S.HCl

CAS No. 170151-24-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01704196 Completed Cocaine Dependence National Institute on Drug Abuse (NIDA) April 2013 Phase 2
NCT00659230 Completed Posttraumatic Stress Disorder Tuscaloosa Research & Education Advancement Corporation|Biotie Therapies Inc.|Ralph H. Johnson VA Medical Center|Baylor College of Medicine|VA Office of Research and Development|San Diego Veterans Healthcare System April 2009 Phase 2
NCT00656357 Completed Cocaine Dependence Biotie Therapies Inc.|National Institute on Drug Abuse (NIDA) June 2008 Phase 1|Phase 2
NCT00641511 Completed Post Traumatic Stress Disorder (PTSD) Michael Debakey Veterans Affairs Medical Center|Lori Davis, MD Tuscaloosa VA Medical Center|Ralph H. Johnson VA Medical Center|Biotie Therapies Inc. June 2008 Phase 2

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Hydroxylase Signaling Pathway Map

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