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Purity: ≥98%
Perphenazine (also known as Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties. Perphenazine has a somewhat strong potency and primarily blocks dopamine 2 (D2) receptors, but it may also have antagonistic effects at histamine 1 (H1), cholinergic M1, and alpha 1 adrenergic receptors in the vomiting center, which would lessen nausea and vomiting. Treatment for specific mental/emotional disorders (e.g., schizophrenia, manic phase of bipolar disorder, schizoaffective disorder) has been implemented.
| Targets |
D2 Receptor ( Ki = 0.56 nM ); D3 Receptor ( Ki = 0.43 nM ); D4 Receptor ( Ki = 28.5 nM ); 5-HT2A Receptor ( Ki = 5.6 nM ); 5-HT6 Receptor ( Ki = 17 nM ); 5-HT7 Receptor ( Ki = 23 nM ); H2 Receptor ( Ki = 132 nM ); 5-HT1A Receptor ( Ki = 421 nM )
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| Enzyme Assay |
Perphenazine Is a common antipsychotic medication that inhibits the α1A adrenergic receptor, the 5-HT2A receptor, the D2/D3 dopamine receptor, the D2L receptor, and the histamine H1 receptor (H1) with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM. Ki, 5-HT2A: 5.6 nM; Ki,α1A: 10 nM; Ki,D2/D3): 0.765/0.13 nM; Ki,D2L receptor: 3.4 nM; Ki,H1: 8 nM. As for the IC50 values, they are as follows.
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| Cell Assay |
On 96-well plates, cells are plated, and medications are applied for varied lengths of time. After that, the cells are incubated for one hour with the MTS assay reagent. After that, a microplate reader is used to read the plates at 490 nm.
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| References |
| Molecular Formula |
C21H26CLN3OS
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| Molecular Weight |
403.97
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| Exact Mass |
403.15
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| Elemental Analysis |
C, 62.44; H, 6.49; Cl, 8.78; N, 10.40; O, 3.96; S, 7.94
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| CAS # |
58-39-9
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| Related CAS # |
Perphenazine-d4; 155593-75-2; Perphenazine dihydrochloride; 2015-28-3; Perphenazine-d8 dihydrochloride; 2070015-23-3
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| Appearance |
White to off-white crystalline powder
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| SMILES |
OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(Cl)C=C24)CC1
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| InChi Key |
RGCVKNLCSQQDEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H26ClN3OS/c22-17-6-7-21-19(16-17)25(18-4-1-2-5-20(18)27-21)9-3-8-23-10-12-24(13-11-23)14-15-26/h1-2,4-7,16,26H,3,8-15H2
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| Chemical Name |
2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.19 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4754 mL | 12.3772 mL | 24.7543 mL | |
| 5 mM | 0.4951 mL | 2.4754 mL | 4.9509 mL | |
| 10 mM | 0.2475 mL | 1.2377 mL | 2.4754 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05762146 | Recruiting | Drug: Perphenazine Drug: Propylthiouracil |
Ischemic Stroke, Acute | Maastricht University | September 5, 2022 | Phase 2 |
| NCT00480246 | Completed | Drug: BL 1020 Drug: Perphenazine |
Healthy | BioLineRx, Ltd. | May 2007 | Phase 1 |
| NCT02199743 | Completed | Drug: Perphenazine Drug: Haloperidol |
Schizoaffective Disorder Schizophrenia |
University of Texas Southwestern Medical Center |
February 2013 | Phase 4 |
| NCT00806234 | Completed | Drug: Aripiprazole or Perphenazine | Psychotic Disorders |
Johns Hopkins University | January 2009 | Phase 4 |
| NCT00802100 | Completed | Drug: Perphenazine Drug: Aripiprazole |
Schizophrenia | National Institute of Mental Health (NIMH) |
December 2008 | Phase 4 |
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