Description
Droxidopa is a synthetic amino acid precursor of (-)-norepinephrine which is absorbed
from the gut and metabolized to norepinephrine. In Parkinsonian patients, droxidopa
added to existing levodopa/decarboxylase inhibitor therapy produces significant
improvements in retropulsion, dysarthria and muscular rigidity refractory to other
treatments; however, tremor was unaffected.
Description
Droxidopa (L-DOPS) is a synthetic precursor and prodrug of the neurotransmitter norepinephrine. It is transformed into norepinephrine through the action of DOPA decarboxylase. L-DOPS increases norepinephrine levels in the rat heart following intraperitoneal administration and in the brain following intracerebroventricular administration at doses of 125 and 100 μg/animal, respectively. It increases arterial pressure and mesenteric arterial resistance in rats with ligated portal vein or biliary ducts when used at doses of 25-50 mg/kg. L-DOPS crosses the blood brain barrier, however, its effects can be blocked by the peripherally-restricted DOPA decarboxylase inhibitor carbidopa , indicating that the mechanism is peripheral. Formulations containing droxidopa are used in the treatment of neurogenic orthostatic hypotension.
Chemical Properties
Off-White Solid
Originator
Sumitomo (Japan)
Uses
Droxidopa is a psychoactive drug and acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline).
Uses
The L-threo-form Droxidopa. A synthetic amino acid precursor of Norepinephrine (N674500). Antiparkinsonian.
Uses
L-DOPS has been administered for clinical trial studies in mice with amyloid pathology.
Definition
ChEBI: A serine derivative that is L-serine substituted at the beta-position by a 3,4-dihydroxyphenyl group. A prodrug for noradrenalone, it is used for treatment of neurogenic orthostatic hypotension
General Description
L-DOPS, also called L-threo 3,4-Dihydroxyphenylserine or droxidopa is a catecholamine. L-DOPS has many clinical advantages and may be useful for treating norepinephrine deficiency. It is used for treating neurogenic orthostatic hypotension and improves norepinephrine levels. L-DOPS mediates reduction of amyloid plaques and could have a therapeutic potential for treating amyloid pathology.
Biochem/physiol Actions
L-DOPS is a norepinephrine precursor in vivo.
References
[1] J BARTHOLINI. The stereoisomers of 3,4-dihydroxyphenylserine as precursors of norepinephrine.[J]. Journal of Pharmacology and Experimental Therapeutics, 1975, 193 2: 523-532.
[2] MAR COLL. Droxidopa, an oral norepinephrine precursor, improves hemodynamic and renal alterations of portal hypertensive rats[J]. Hepatology, 2012, 56 5: 1849-1860. DOI:
10.1002/hep.25845[3] HORACIO KAUFMANN Jose A P Lucy Norcliffe Kaufmann. Droxidopa in neurogenic orthostatic hypotension.[J]. Expert Review of Cardiovascular Therapy, 2015, 13 8: 875-891. DOI:
10.1586/14779072.2015.1057504
