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Droxidopa HCl (L-DOPS hydrochloride) is an orally bioactive norepinephrine precursor with the potential to be used for neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder). Droxidopa hydrochloride increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability.
| ln Vivo |
Droxidopa hydrochloride (200 mg/kg; i.p.) changes dopamine neuronal and prefrontal cortical activity and improves attention-deficit/hyperactivity disorder-like behavior in rats [2]. Droxidopa hydrochloride (10, 20 mg/kg; intraperitoneal injection) significantly enhanced the paw withdrawal latency at 5 weeks postoperatively and decreased mechanical hypersensitivity to thermal stimulation in rats with 6-OHDA damage [3].
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| Animal Protocol |
Animal/Disease Models: 250-380g male SD (SD (Sprague-Dawley)) rats [2]
Doses: 200 mg/kg (10 mg/kg, intraperitoneal (ip) injection of benserazide 20 or 30 minutes before injection of L-DOPS) Route of Administration: intraperitoneal (ip) injection Experimental Results: At 30 minutes (P < 0.01) and 40 minutes (P < 0.05) after injection, the hyperactivity of BZ-pretreated SHR/NCrl was Dramatically diminished, the inattentive behavior of SHR/NCrl was improved, and the inattentive behavior of SHR/NCrl was improved. and SHR/NCrl's impulsive behavior improved. Wistar rat. |
| References |
[1]. Horacio Kaufmann, et al. Droxidopa for neurogenic orthostatic hypotension. Neurology, 2014; 83(4).
[2]. Dela Peña I, et al. Droxidopa alters dopamine neuron and prefrontal cortex activity and improves attention-deficit/hyperactivity disorder-like behaviors in rats. Eur J Pharmacol. 2021 Feb 5;892:173826. [3]. Cao LF, et al. Restoring Spinal Noradrenergic Inhibitory Tone Attenuates Pain Hypersensitivity in a Rat Model of Parkinson's Disease. Neural Plast. 2016;2016:6383240. [4]. Kaufmann H. L-dihydroxyphenylserine (Droxidopa): a new therapy for neurogenic orthostatic hypotension: the US experience. Clin Auton Res. 2008 Mar;18 Suppl 1:19-24. |
| Molecular Formula |
C9H11NO5
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|---|---|
| Molecular Weight |
213.187342882156
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| CAS # |
1260173-94-1
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| Related CAS # |
Droxidopa;23651-95-8
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| SMILES |
O[C@H](C1C=CC(=C(C=1)O)O)[C@@H](C(=O)O)N
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6907 mL | 23.4533 mL | 46.9065 mL | |
| 5 mM | 0.9381 mL | 4.6907 mL | 9.3813 mL | |
| 10 mM | 0.4691 mL | 2.3453 mL | 4.6907 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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