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Prochlorperazine Maleate

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Chemical Structure| 84-02-6 同义名 : -
CAS号 : 84-02-6
货号 : A123783
分子式 : C28H32ClN3O8S
纯度 : 95%
分子量 : 606.09
MDL号 : MFCD00069330
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

生物活性
靶点

  • D2 receptor
描述 Prochlorperazine (Dimaleate) is a D(2) antagonist. Prochlorperazine (1-2 mg/kg s.c./i.p.) produced an increase of the pain threshold in the mouse hot-plate test. Prochlorperazine also elicited a dose-dependent increase in ACh release from rat cerebral cortex. In the antinociceptive dose-range, prochlorperazine did not impair mouse performance evaluated by the rota-rod and hole-board tests. Thus, prochlorperazine exerted an antinociceptive effect mediated by a central cholinergic mechanism[3]. Prochlorperazine is a phenothiazine-class antipsychotic drug and induces concentration-dependent loss in cell viability with EC50 value of 18.49 μM. Prochlorperazine in a concentration of 0.001 μM stimulated melanogenesis, while in concentrations 1.0 and 10.0 μM melanization process was inhibited. Furthermore, the drug in concentrations of 0.1, 1.0 and 10.0 μM caused changes in cellular antioxidant defense system, what indicated the induction of oxidative stress[4]. Prochlorperazine is recommended for adults with breakthrough or refractory chemotherapy-induced nausea and vomiting (CINV). The most common AEs (adverse effects) reported with the pediatric use of prochlorperazine are EPS (extrapyramidal symptoms) and sedation. Fatalities, life-threatening, and persistent AEs have also been reported[5]. IV hydromorphone is substantially less effective than IV prochlorperazine for the treatment of acute migraine in the ED (emergency department) and should not be used as first-line therapy[6]. Buccally absorbed prochlorperazine (BAP) is an effective, non-invasive treatment for migraine headaches when compared to intravenous prochlorperazine (IVP)[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.65mL

0.33mL

0.16mL

8.25mL

1.65mL

0.82mL

16.50mL

3.30mL

1.65mL
参考文献

[1]Huang L, Zhao S, et al. An integrated bioinformatics approach identifies elevated cyclin E2 expression and E2F activity as distinct features of tamoxifen resistant breast tumors. PLoS One. 2011;6(7):e22274.

[2]Ghelardini C, Galeotti N, et al. Prochlorperazine induces central antinociception mediated by the muscarinic system. Pharmacol Res. 2004 Sep;50(3):351-8.

[3]Ghelardini C, Galeotti N, Uslenghi C, Grazioli I, Bartolini A. Prochlorperazine induces central antinociception mediated by the muscarinic system. Pharmacol Res. 2004;50(3):351‐358

[4]Otręba M, Wrześniok D, Rok J, Beberok A, Buszman E. Prochlorperazine interaction with melanin and melanocytes. Pharmazie. 2017;72(3):171‐176

[5]Lau Moon Lin M, Robinson PD, Flank J, Sung L, Dupuis LL. The Safety of Prochlorperazine in Children: A Systematic Review and Meta-Analysis. Drug Saf. 2016;39(6):509‐516

[6]Friedman BW, Irizarry E, Solorzano C, et al. Randomized study of IV prochlorperazine plus diphenhydramine vs IV hydromorphone for migraine. Neurology. 2017;89(20):2075‐2082

[7]Fernando T, Lumanauw DD, Youn S, et al. Buccally absorbed vs intravenous prochlorperazine for treatment of migraines headaches. Acta Neurol Scand. 2019;140(1):72‐77