Droxidopa - CAS 23651-95-8
Catalog number: B0046-063644
Category: APIs
Molecular Formula:
C9H11NO5
Molecular Weight:
213.189
COA:
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Description:
Droxidopa is a synthetic amino acid precursor which acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline). It is capable of crossing the protective blood–brain barrier.
Ordering Information
Catalog Number Size Price Stock Quantity
B0046-063644 500 mg $398 In stock
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Purity:
>98%
Synonyms:
L-DOPS; Northera; (2S,3R)-2-amino-3-(3,4-dihydroxyphenyl)-3-hydroxypropanoic acid
MSDS:
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Melting Point:
>170°C (dec.)
InChIKey:
QXWYKJLNLSIPIN-JGVFFNPUSA-N
InChI:
InChI=1S/C9H11NO5/c10-7(9(14)15)8(13)4-1-2-5(11)6(12)3-4/h1-3,7-8,11-13H,10H2,(H,14,15)/t7-,8+/m0/s1
Canonical SMILES:
C1=CC(=C(C=C1C(C(C(=O)O)N)O)O)O
1.L-dihydroxyphenylserine (Droxidopa) in the treatment of orthostatic hypotension
Christopher J. Mathias. Clin Auton Res (2008) 18[Suppl 1]:25–29
L-threo-dihydroxyphenylserine (Droxidopa) has a structure which is similar to noradrenaline but with a carboxyl group. It can be administered orally, and is acted upon by the ubiquitous enzyme L-aromatic amino acid decarboxylase (dopa decarboxylase), which is found all over the body. It is converted directly to noradrenaline. It is likely to have both neuronal and extra neuronal effects, with a direct effect through noradrenaline on target organs. Droxidopa has been highly successful in replacing deficient or absent noradrenaline in patients with dopamine beta hydroxylase deficiency. In Japan, it has been approved since 1989 use for in the treatment of neurogenic OH due to various disorders, that include familial amyloid polyneuropathy, haemodialysis induced hypotension, and MSA and PD. Experience with Droxidopa, especially in primary autonomic failure and PD in Caucasians is limited. Because of its potential value in the management of symptomatic orthostatic hypotension, two Phase II studies were performed in Europe. These were multicentre, multinational studies. An escalating dose of Droxidopa was used in the first study in patients with PAF and MSA. In the second a randomised double blind placebo controlled study was performed using three doses of Droxidopa in patients with MSA or PD. This review will describe key components from each of these studies, and will focus on whether inhibition of the enzyme dopa decarboxylase, which converts Droxidopa to noradrenaline, can influence its ability to reduce orthostatic hypotension.
2. Meta-analysis of the safety and efficacy of droxidopa for neurogenic orthostatic hypotension
Ahmed Elgebaly • Bassant Abdelazeim • Omar Mattar. Clin Auton Res (2016) 26:171–180
The present study provides Class 1 evidence that droxidopa is a safe and effective drug for the short-term management of NOH symptoms. In terms of safety, droxidopa was well tolerated, and none of the reported adverse events, particularly severe adverse events such as hypertension, and supine hypertension, were significantly higher in the droxidopa group than in the placebo group.
3. New Developments in the Management of Neurogenic Orthostatic Hypotension
Italo Biaggioni. Curr Cardiol Rep (2014) 16:542
Droxidopa was originally developed by Sumitomo Pharmaceuticals and has been approved in Japan since 1989 for the treatment of neurogenic orthostatic hypotension and the freezing phenomenon seen in patients with Parkinson disease. The efficacy of droxidopa in restoring norepinephrine is exemplified in patients with dopamine-beta-hydroxylase (DβH) deficiency. These extremely rare patients have a genetic deficiency in dopamine-β-hydroxylase, the enzyme that converts dopamine to norepinephrine (Fig. 2) and therefore accumulate dopamine and are unable to produce norepinephrine. Droxidopa bypasses this enzymatic defect and restores nor- epinephrine in these patients. It not only increases plasma norepinephrine but also restores it in noradrenergic nerve terminals.
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CAS 23651-95-8 Droxidopa

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