Droxidopa (hydrochloride) CAS#: 1260173-94-1

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Uses

Droxidopa (L-DOPS) hydrochloride is a potent, orally active norepinephrine precursor. Droxidopa hydrochloride increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa hydrochloride has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder)[1][2][3][4].

Definition

ChEBI: Droxidopa is 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 It has a role as a prodrug, a vasoconstrictor agent and an antihypertensive agent. It is a L-tyrosine derivative and a member of catechols.

in vivo

Droxidopa hydrochloride (200 mg/kg;i.p.) alters dopamine neuron and prefrontal cortex activity and improves attention-deficit/hyperactivity disorder-like behaviors in rats^[2]. Droxidopa hydrochloride (10, 20 mg/kg; i.p.) significantly increases the paw withdrawal latency and inhibits mechanical hypersensitivity to thermal stimulation in 6-OHDA-lesioned rats at the 5th week after surgery^[3].

Animal Model:	250-380g male Sprague-Dawley rats^[2]
Dosage:	200 mg/kg (10 mg/kg, i.p. benserazide was given to the animals at 20 or 30 min prior to L-DOPS injection)
Administration:	I.p.
Result:	Significantly decreased hyperactivity of BZ-pretreated SHR/NCrl at 30 (P < 0.01) and 40 min (P < 0.05) post-injection, improved inattention-like behavior of SHR/NCrl, and ameliorated impulsive-like behavior of SHR/NCrl and Wistar rats.

References

[1] Horacio Kaufmann, et al. Droxidopa for neurogenic orthostatic hypotension. Neurology, 2014; 83(4).
[2] Dela Pea 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. DOI:10.1016/j.ejphar.2020.173826
[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. DOI:10.1155/2016/6383240
[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. DOI:10.1007/s10286-007-1002-2

Droxidopa (hydrochloride)

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