product name Prochlorperazine dimaleate
Description: Prochlorperazine dimaleate (also known as Prochlorperazin, Compazine, Capazine, Stemetil), the dimaleate salt of Prochlorperazine, is a dopamine (D2) receptor antagonist that belongs to the phenothiazine class of antipsychotic agents that are used for the antiemetic treatment of nausea and vertigo. It is also a highly potent typical antipsychotic, 10–20 times more potent than chlorpromazine. Prochlorperazine dimaleate is also used to treat migraine headaches.
References: Pharmacol Res. 2004 Sep;50(3):351-8; PLoS One. 2011;6(7):e22274.
606.09
Formula
C20H24ClN3S.C8H8O8
CAS No.
84-02-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 74 mg/mL (122.1 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (3.3 mM)
Solubility (In vivo)
Synonyms
Prochlorperazin, Compazine, Capazine, Stemetil
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19414746
| In Vitro |
In vitro activity: Prochlorperazine down-regulates cyclin E2 and reduces cell proliferation in MCF-7 cells that are resistant to tamoxifen. It has the potential to impact on estrogen receptor (ER) function and alter response to endocrine therapy. Kinase Assay: Perphenazine is a typical antipsychotic drug, inhibits 5-HT2A receptor (5-HT2A), Alpha-1A adrenergic receptor (α1A), Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor (H1) with Ki of 5.6, 10, 0.765/0.13, 3.4, and 8 nM. IC50 value: 5.6 nM (Ki, 5-HT2A) 10 nM (Ki,α1A), 0.765/0.13 nM (Ki,D2/D3), 3.4 nM (Ki,D2L receptor), 8 nM (Ki,H1); Target: 5-HT2A,α1A,D2/D3, D2L receptor,H1 Cell Assay: Cells are treated 5 μM of prochlorperazine for 5 days and cell proliferation is measured by methylene blue staining or for 2 days and cyclin E2 mRNA levels are measured by qPCR. |
|---|---|
| In Vivo | Prochlorperazine is showed to be able to induce antinociception in mice. prochlorperazine-treated mice show a complete integrity of motor co-ordination on the rota-rod test, normal spontaneous motility, as well as exploratory behaviour as revealed by the hole-board test. The antinociceptive effect of prochlorperazine appears to be due to the antagonism of D2 receptors since the increase of the pain threshold induced by the investigated compound is prevented by pretreatment with the D2 agonist quinpirole. |
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| Formulation & Dosage | |
| References | Pharmacol Res. 2004 Sep;50(3):351-8; PLoS One. 2011;6(7):e22274. |
