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| | PROCHLORPERAZINE MALEATE Basic information |
| | PROCHLORPERAZINE MALEATE Chemical Properties |
| Melting point | 1750C | | storage temp. | 2-8°C | | solubility | Very slightly soluble in water and in ethanol (96 per cent). | | pka | pKa 8.1(H2O,t =24±1) (Uncertain) | | form | solid | | color | White | | Water Solubility | H2O: slightly soluble 0.3mg/mL
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 2.3mg/mL
methanol: soluble | | λmax | 313nm(MeOH)(lit.) | | Merck | 14,7761 | | Stability: | Stable for 2 years as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. | | Major Application | pharmaceutical | | InChIKey | DSKIOWHQLUWFLG-SPIKMXEPSA-N | | SMILES | OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.CN1CCN(CCCN2c3ccccc3Sc4ccc(Cl)cc24)CC1 |
| Hazard Codes | Xn | | Risk Statements | 20/21/22 | | Safety Statements | 36 | | WGK Germany | 3 | | RTECS | SO3150000 | | HS Code | 2934302300 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Acute Tox. 4 Oral
Lact.
Repr. 2
STOT SE 3 | | Toxicity | LD50 in mice (mg/kg): 400 s.c.; 120 i.p.; 90 i.v., 400 orally (Courvoisier) |
| | PROCHLORPERAZINE MALEATE Usage And Synthesis |
| Description | Prochlorperazine maleate (84-02-6) inhibits dynamin and clathrin-mediated endocytosis (CME) with an IC50=5.8 μM for CME.1Increases tumor cell antigen presentation enhancing the efficacy of anti-tumor mAbs.2A clinically useful antipsychotic agent3with antimigraine4and antiemetic activity5. | | Chemical Properties | Off-White Powder | | Uses | Antiemetic;Dopamine antagonist | | Uses | Antiemetic. | | Brand name | Compazine (GlaxoSmithKline). | | General Description | Prochlorperazinemaleate, 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazinemaleate (Compazine), is in the piperazine subgroupof the phenothiazines, characterized by high-milligramantipsychotic potency, a high prevalence of EPS, and lowsedative and autonomic effects. Prochlorperazine is more potenton a milligram basis than its alkylamino counterpart,chlorpromazine. Because of the high prevalence of EPS, however,it is used mainly for its antiemetic effect, not for its antipsychoticeffect. | | Biological Activity | D 2 receptor antagonist. Also interacts with 5-HT 3 and nAChR. Displays antipsychotic, antispasmodic, antiemetic and antinociceptive activity in vivo . | | Biochem/physiol Actions | Phenothiazine antipsychotic; D2 dopamine receptor antagonist; antispasmodic | | References | [1] JAMES A DANIEL. Phenothiazine-derived antipsychotic drugs inhibit dynamin and clathrin-mediated endocytosis.[J]. Traffic, 2015, 16 6: 635-654. DOI:10.1111/tra.12272
[2] HUI YI CHEW. Endocytosis Inhibition in Humans to Improve Responses to ADCC-Mediating Antibodies.[J]. Cell, 2020, 180 5: 895-914.e27. DOI:10.1016/j.cell.2020.02.019
[3] M.D. L E H. Clinical use of psychotherapeutic drugs: Current status[J]. Clinical Pharmacology & Therapeutics, 1969, 10 2: 170-198. DOI:10.1002/cpt1969102170
[4] CALLI COOK Brittany N. Emergency Department Use of Intravenous Prochlorperazine for Acute Migraine.[J]. Advanced Emergency Nursing Journal, 2018, 40 3: 148-154. DOI:10.1097/tme.0000000000000203
[5] VAN DEN BERG A A. The prophylactic antiemetic efficacy of prochlorperazine and ondansetron in nasal septal surgery: a randomized double-blind comparison.[J]. Anaesthesia and Intensive Care, 1996, 24 5: 538-545. DOI:10.1177/0310057x9602400505 |
| | PROCHLORPERAZINE MALEATE Preparation Products And Raw materials |
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