Catalog number: 73220-03-8
Category: Inhibitor
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Dopamine Receptor
Remoxipride is a selective dopamine D2 receptor antagonist. It shows selectivity over D3 and D4 receptors with Ki values are ~ 300nM for D2 receptor, ~ 1600nM for D3 receptor and ~ 2800 nM for D4 receptor. Remoxipride shows antipsychotic activity in vivo with no extrapyramidal side effects. In Jul 1995, treatment for Psychotic disorders in USA was discontinued.
White solid
Remoxipride Hydrochloride; Remoxipride HCl; Roxiam; A 33547 hydrochloride; UNII-QS4S72U30K; QS4S72U30K; Remoxipride Hydrochloride Anhydrous ; Remoxipride Monohydrochloride; Remoxipride Monohydrochloride Monohydrate; Remoxipride Monohydrochloride;3-bromo-N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-2,6-dimethoxybenzamide;hydrochloride
water to 100 mM
-20℃ Freezer
Psychotic disorders
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
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Current Developer:
Originator AstraZeneca
1.Online solid phase extraction with liquid chromatography-tandem mass spectrometry to analyze remoxipride in small plasma-, brain homogenate-, and brain microdialysate samples.
Stevens J1, van den Berg DJ, de Ridder S, Niederländer HA, van der Graaf PH, Danhof M, de Lange EC. J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Apr 15;878(13-14):969-75. doi: 10.1016/j.jchromb.2010.02.024. Epub 2010 Feb 26.
Remoxipride is a selective dopamine D(2) receptor antagonist, and useful as a model compound in mechanism-based pharmacological investigations. To that end, studies in small animals with serial sampling over time are needed. For these small volume samples currently no suitable analytical methods are available. We propose analytical methods for the detection of low concentrations remoxipride in small sample volumes of plasma, brain homogenate, and brain microdialysate, using online solid phase extraction with liquid chromatography-tandem mass spectrometry. Method development, optimization and validation are described in terms of calibration curves, extraction yield, lower limit of quantification (LLOQ), precision, accuracy, inter-day- and intra-day variability. The 20 microl plasma samples showed an extraction yield of 76%, with a LLOQ of 0.5 ng/ml. For 0.6 ml brain homogenate samples the extraction yield was 45%, with a LLOQ of 1.8 ng/ml.
2.The dopaminergic stabilizers pridopidine and ordopidine enhance cortico-striatal Arc gene expression.
Waters S1, Ponten H, Edling M, Svanberg B, Klamer D, Waters N. J Neural Transm (Vienna). 2014 Nov;121(11):1337-47. doi: 10.1007/s00702-014-1231-1. Epub 2014 May 11.
The dopaminergic stabilizers pridopidine [4-(3-(methylsulfonyl)phenyl)-1-propylpiperidine] and ordopidine [1-ethyl-4-(2-fluoro-3-(methylsulfonyl)phenyl)piperidine] inhibit psychostimulant-induced hyperactivity, and stimulate behaviour in states of hypoactivity. While both compounds act as dopamine D2 receptor antagonists in vitro, albeit with low affinity, their specific state-dependent behavioural effect profile is not shared by D2 receptor antagonists in general. To further understand the neuropharmacological effects of pridopidine and ordopidine, and how they differ from other dopaminergic compounds in vivo, we assessed the expression of activity-regulated cytoskeleton-associated protein/activity-regulated gene 3.1 (Arc), an immediate early gene marker associated with synaptic activation, in the frontal cortex and striatum. Furthermore, monoamine neurochemistry and locomotor activity were assessed. The effects of pridopidine and ordopidine were compared to reference dopamine D1 and D2 receptor agonists and antagonists, as well as the partial dopamine D2 agonist aripiprazole.
3.Systemic and direct nose-to-brain transport pharmacokinetic model for remoxipride after intravenous and intranasal administration.
Stevens J1, Ploeger BA, van der Graaf PH, Danhof M, de Lange EC. Drug Metab Dispos. 2011 Dec;39(12):2275-82. doi: 10.1124/dmd.111.040782. Epub 2011 Sep 8.
Intranasal (IN) administration could be an attractive mode of delivery for drugs targeting the central nervous system, potentially providing a high bioavailability because of avoidance of a hepatic first-pass effect and rapid onset of action. However, controversy remains whether a direct transport route from the nasal cavity into the brain exists. Pharmacokinetic modeling is proposed to identify the existence of direct nose-to-brain transport in a quantitative manner. The selective dopamine-D2 receptor antagonist remoxipride was administered at different dosages, in freely moving rats, by the IN and intravenous (IV) route. Plasma and brain extracellular fluid (ECF) concentration-time profiles were obtained and simultaneously analyzed using nonlinear mixed-effects modeling. Brain ECF/plasma area under the curve ratios were 0.28 and 0.19 after IN and IV administration, respectively. A multicompartment pharmacokinetic model with two absorption compartments (nose-to-systemic and nose-to-brain) was found to best describe the observed pharmacokinetic data.
4.Mechanism-based PK-PD model for the prolactin biological system response following an acute dopamine inhibition challenge: quantitative extrapolation to humans.
Stevens J1, Ploeger BA, Hammarlund-Udenaes M, Osswald G, van der Graaf PH, Danhof M, de Lange EC. J Pharmacokinet Pharmacodyn. 2012 Oct;39(5):463-77. doi: 10.1007/s10928-012-9262-4. Epub 2012 Jul 12.
The aim of this investigation was to develop a mechanism-based pharmacokinetic-pharmacodynamic (PK-PD) model for the biological system prolactin response following a dopamine inhibition challenge using remoxipride as a paradigm compound. After assessment of baseline variation in prolactin concentrations, the prolactin response of remoxipride was measured following (1) single intravenous doses of 4, 8 and 16 mg/kg and (2) following double dosing of 3.8 mg/kg with different time intervals. The mechanistic PK-PD model consisted of: (i) a PK model for remoxipride concentrations in brain extracellular fluid; (ii) a pool model incorporating prolactin synthesis, storage in lactotrophs, release into- and elimination from plasma; (iii) a positive feedback component interconnecting prolactin plasma concentrations and prolactin synthesis; and (iv) a dopamine antagonism component interconnecting remoxipride brain extracellular fluid concentrations and stimulation of prolactin release.
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