Home GPCR & G Protein Adrenergic Receptor agonist Droxidopa

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Droxidopa Adrenergic Receptor agonist

Cat.No.S3041

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

Chemical Structure

Molecular Weight: 213.19

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Quality Control

Batch: Purity: 99.84%
99.84

Cell Culture, Treatment & Working Concentration

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
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Solubility

In vitro
Batch:

DMSO : 2 mg/mL (9.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 2 mg/mL

Ethanol : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 213.19 Formula

C9H11NO5

 Storage (From the date of receipt)
CAS No. 23651-95-8 Download SDF Storage of Stock Solutions

Synonyms L-DOPS Smiles C1=CC(=C(C=C1C(C(C(=O)O)N)O)O)O

Mechanism of Action

Features
An artificial amino acid.
Targets/IC50/Ki
Adrenergic Receptor
In vitro
Droxidopa is a pro-drug which has a structure similar to noradrenaline, but with a carboxyl group. It 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. This compound is well tolerated. It 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. This chemical taken alone increases standing blood pressure. It can also cross the blood–brain barrier (BBB) where it is converted to norepinephrine and epinephrine from within the brain.
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. This compound-treated rats also showed a decreased ratio of p-eNOS/eNOS and p-AKT/AKT and increased activity of RhoK in SMA.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17214596/
  • [5] https://pubmed.ncbi.nlm.nih.gov/22610782/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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