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| 250mg |
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Pimozide (R-6238; NSC-170984; Orap) is an antipsychotic drug of the diphenylbutylpiperidine class discovered y Janssen Pharmaceuticals in 1963. Pimozide is an antagonist of dopamine receptors, with Kis values of 1.4 nM, 2.5 nM, and 588 nM for dopamine D2, D3, and D1 receptors, respectively. It also exhibits affinity at the α1-adrenoceptor, with a Ki of 39 nM. When compared to chlorpromazine, pimozide is much more potent (ratio 50–70:1). It is even more effective than haloperidol when compared weight for weight. Additionally, it has specific neurologic indications for resistant tics and Tourette syndrome. Akathisia, tardive dyskinesia, and, in rarer cases, neuroleptic malignant syndrome and prolongation of the QT interval are among the side effects.
| Targets |
Dopamine D2 receptor ( Ki = 1.4 nM ); Dopamine D3 receptor ( Ki = 2.5 nM ); Dopamine D1 receptor ( Ki = 588 nM ); α1-adrenoceptor ( Ki = 39 nM ); STAT3; STAT5
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| Cell Assay |
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| References |
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| Molecular Formula |
C28H29F2N3O
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| Molecular Weight |
461.55
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| Exact Mass |
461.23
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| Elemental Analysis |
C, 72.86; H, 6.33; F, 8.23; N, 9.10; O, 3.47
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| CAS # |
2062-78-4
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| Related CAS # |
Pimozide-d4-1; Pimozide-d4; 1803193-57-8; Pimozide-d5 N-Oxide; 1794795-40-6
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| Appearance |
White solid powder
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| SMILES |
C1CN(CCC1N2C3=CC=CC=C3NC2=O)CCCC(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F
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| InChi Key |
YVUQSNJEYSNKRX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H29F2N3O/c29-22-11-7-20(8-12-22)25(21-9-13-23(30)14-10-21)4-3-17-32-18-15-24(16-19-32)33-27-6-2-1-5-26(27)31-28(33)34/h1-2,5-14,24-25H,3-4,15-19H2,(H,31,34)
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| Chemical Name |
3-[1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl]-1H-benzimidazol-2-one
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| Synonyms |
R6238; NSC 170984; NSC170984; R-6238; NSC-170984; R 6238
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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 |
| 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) |
DMSO: 16.7~90 mg/mL (36.1~195 mM)
H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.62 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 16.7 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. View More
Solubility in Formulation 3: 1.67 mg/mL (3.62 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1666 mL | 10.8331 mL | 21.6661 mL | |
| 5 mM | 0.4333 mL | 2.1666 mL | 4.3332 mL | |
| 10 mM | 0.2167 mL | 1.0833 mL | 2.1666 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 |
| NCT04529226 | Recruiting | Drug: Clozapine Drug: haloperidol, pimozide, olanzapine, risperidone, amisulpride |
Psychosis Intellectual Disability |
RECORDATI GROUP | June 10, 2013 | Phase 4 |
| NCT05507372 | Not yet recruiting | Drug: Pimozide 1 MG | Tinnitus, Subjective | Applied Biology, Inc. | October 1, 2022 | Not Applicable |
| NCT00158223 | Completed | Drug: Pimozide Drug: Placebo |
Schizophrenia Psychotic Disorders |
Icahn School of Medicine at Mount Sinai |
October 2004 | Phase 4 |
| NCT00374244 | Completed | Drug: Pimozide Drug: placebo |
Schizophrenia | Yale University | January 2004 | Phase 2 |
| NCT00004652 | Completed | Drug: pimozide | Tourette Syndrome | National Center for Research Resources (NCRR) |
February 1993 | Phase 2 |
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