Droxidopa

Catalog No.S3041 Synonyms: L-DOPS

Droxidopa Chemical Structure

Molecular Weight(MW): 213.19

Droxidopa is a psychoactive drug and acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline).

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Biological Activity

Description Droxidopa is a psychoactive drug and acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline).
Features An artificial amino acid.
Targets
Adrenergic Receptor [1]
In vitro

Droxidopa is a pro-drug which has a structure similar to noradrenaline, but with a carboxyl group. Droxidopa can be administered orally, unlike noradrenaline, and after absorption is converted by the enzyme dopa decarboxylase into noradrenaline thus increasing levels of the neurotransmitter which is identical to endogenous noradrenaline. [1] Droxidopa is well tolerated. [2] Droxidopa could exert its pressor effect in three different ways: a) as a central stimulator of sympathetic activity; b) as a peripheral sympathetic neurotransmitter; c) as a circulating hormone. Droxidopa taken alone increases standing blood pressure. [3] Droxidopa can also cross the blood–brain barrier (BBB) where it is converted to norepinephrine and epinephrine from within the brain. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 cells M{LXZ2Z2dmO2aX;uJIF{e2G7 M1X1bVI1KGh? M2K4NWFkfGm4YYTpc44hd2ZiaIXtZY4hWFiUIHX4dJJme3OnZDDpckBpfW2jbjDI[ZBIOiBqRGDYMVIqKGOnbHzzJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjDDXXA{STRiYX\0[ZIhOjRiaILzJIJ6KGy3bXnu[ZNk\W62IHHuZYx6e2m|LDDFR|UxRTBwMEC0JO69VQ>? MlvjNlA6PjZyNEO=

... Click to View More Cell Line Experimental Data

In vivo The acute administration of droxidopa in PVL and BDL rats caused a significant and maintained increase in arterial pressure and mesenteric arterial resistance, with a significant decrease of mesenteric arterial and portal blood flow, without changing portal pressure and renal blood flow. Droxidopa-treated rats also showed a decreased ratio of p-eNOS/eNOS and p-AKT/AKT and increased activity of RhoK in SMA[5].

Protocol

Animal Research:

[5]

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  • Animal Models: biliary duct-ligated (BDL) rats
  • Formulation: 1% carboxymetylcellulose solution and 0.2% Tween 80 emulsifier
  • Dosages: 25-50 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO Insoluble
Water Insoluble
Ethanol 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 213.19
Formula

C9H11NO5

CAS No. 23651-95-8
Storage powder
Synonyms L-DOPS

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02897063 Recruiting Autonomic Failure|Pure Autonomic Failure|Multiple System Atrophy|Parkinson Disease|Orthostatic Hypotension Vanderbilt University Medical Center September 2016 Phase 1
NCT02812147 Recruiting Parkinson Disease St. Josephs Hospital and Medical Center, Phoenix|Arizona State University, Tempe May 2016 Phase 2
NCT02586623 Recruiting Symptomatic Neurogenic Orthostatic Hypotension Lundbeck Northera Ltd. February 2016 Phase 4
NCT02624310 Withdrawn HSAN Type IV New York University School of Medicine January 2016 Phase 2
NCT02558972 Recruiting Postural Tachycardia Syndrome (POTS)|Vasovagal Syncope (VVS)|Fainting New York Medical College|Lundbeck LLC September 2015 Phase 2
NCT02066571 Enrolling by invitation Parkinsons Disease|Freezing of Gait|Cognitive Ability, General Henry Ford Health System March 2015 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Adrenergic Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID