Droxidopa

Catalog No.S3041 Synonyms: L-DOPS

For research use only.

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

Droxidopa Chemical Structure

CAS No. 23651-95-8

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Biological Activity

Description Droxidopa (L-DOPS) 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 MlvRSpVv[3Srb36gZZN{[Xl? NWP1PYZoOjRiaB?= M1rIcWFkfGm4YYTpc44hd2ZiaIXtZY4hWFiUIHX4dJJme3OnZDDpckBpfW2jbjDI[ZBIOiBqRGDYMVIqKGOnbHzzJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjDDXXA{STRiYX\0[ZIhOjRiaILzJIJ6KGy3bXnu[ZNk\W62IHHuZYx6e2m|LDDFR|UxRTBwMEC0JO69VQ>? NULKV|J[OjB7Nk[wOFM>
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 (from reference)

Animal Research:

[5]

  • Animal Models: biliary duct-ligated (BDL) rats
  • Dosages: 25-50 mg/kg
  • Administration: oral administration

Solubility (25°C)

In vitro

DMSO Insoluble
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 213.19
Formula

C9H11NO5

CAS No. 23651-95-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C=C1C(C(C(=O)O)N)O)O)O

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03446807 Not yet recruiting Drug: Droxidopa|Drug: Placebo Oral Tablet Parkinson Disease|Multiple System Atrophy|Progressive Supranuclear Palsy Loma Linda University|H. Lundbeck A/S December 2021 Phase 2
NCT04977388 Recruiting Drug: Droxidopa|Other: Placebo Menkes Disease|Occipital Horn Syndrome Stephen G. Kaler MD|Nationwide Children''s Hospital July 12 2021 Phase 1|Phase 2
NCT03173781 Completed Drug: droxidopa|Drug: Placebo Parkinson''s Disease Colorado Springs Neurological Associates|H. Lundbeck A/S April 2016 Not Applicable
NCT01331122 Withdrawn Drug: droxidopa Gait Disorders Neurologic Chelsea Therapeutics April 2012 Phase 1|Phase 2
NCT01370512 Completed Drug: Droxidopa|Drug: Pyridostigmine Bromide Orthostatic Hypotension Mayo Clinic|National Institute of Neurological Disorders and Stroke (NINDS) November 2011 Phase 2
NCT01354158 Completed Drug: Droxidopa Spinal Cord Injury|Hypotension Bronx VA Medical Center|Chelsea Therapeutics May 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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