Home GPCR & G Protein Adrenergic Receptor agonist Droxidopa For research use only.

Droxidopa

Synonyms: L-DOPS

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

Droxidopa Chemical Structure

Droxidopa Chemical Structure

CAS No. 23651-95-8

Purity & Quality Control

Droxidopa Related Products

Signaling Pathway

Adrenergic Receptor Signaling Pathways

Adrenergic Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 cells Function assay 24 h Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis, EC50=0.004 μM 20966043
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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
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]
In Vivo
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].
Animal Research Animal Models biliary duct-ligated (BDL) rats
Dosages 25-50 mg/kg
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03446807 Withdrawn
Parkinson Disease|Multiple System Atrophy|Progressive Supranuclear Palsy
Loma Linda University|H. Lundbeck A/S
 December 2021 Phase 2
NCT04977388 Recruiting
Menkes Disease|Occipital Horn Syndrome
Stephen G. Kaler MD|Nationwide Children''s Hospital
 July 12 2021 Phase 1|Phase 2
NCT03173781 Completed
Parkinson''s Disease
Colorado Springs Neurological Associates|H. Lundbeck A/S
 April 2016 Not Applicable
NCT01331122 Withdrawn
Gait Disorders Neurologic
Chelsea Therapeutics
 April 2012 Phase 1|Phase 2
NCT01354158 Completed
Spinal Cord Injury|Hypotension
Bronx VA Medical Center|Chelsea Therapeutics
 May 2011 Phase 1
NCT01327066 Completed
QTc Interval
Chelsea Therapeutics
 March 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 213.19 Formula

C9H11NO5
CAS No. 23651-95-8 SDF Download Droxidopa SDF
Smiles C1=CC(=C(C=C1C(C(C(=O)O)N)O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 2 mg/mL ( (9.38 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 2 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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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