| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| Other Sizes |
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Droperidol (Dridol; Properidol; Dehydrobenzperidol; Inapsine) is a novel and potent D1DR and D2DR inhibitor with anti-emetic, sedative and anti-anxiety activities. It is also an antidopaminergic medication with antipsychotic and antiemetic properties. In the context of intensive care, droperidol is also frequently used for sedation and neuroleptanalgesic anesthesia.
| ln Vitro |
Droperidol causes peripheral vascular dilatation and mild α-adrenergic blockade. Droperidol has been shown to block potassium efflux in the myocardium in isolated animal ventricular myocytes, resulting in a dose-dependent delay in repolarization. In isolated animal Purkinje fibers, droperidol has also been demonstrated to cause early depolarizations. [1]
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| ln Vivo |
Droperidol (0.01 mM-0.3 mM) increases the action potential duration (APD) in a dose-dependent manner while leaving the other parameters unchanged in rabbit Purkinje fibers stimulated at 60 pulses/min. In rabbit Purkinje fibers, droperidol (1 mM–3 mM) causes the prolonging effect to reverse. In rabbit Purkinje fibers, droperidol (10 mM–30 mM) causes a considerable reduction in Vmax, action potential amplitude, and resting membrane potential in addition to a 50% repolarization in APD shortening. Droperidol has a dual effect on rabbit Purkinje fiber repolarization, prolongation at low concentrations with EAD development, and subsequent triggered activity.[2] Droperidol (3 mg/kg, single dose) reduces the apomorphine effects of rats as well as their locomotion and rearing frequencies in an open field in a dose-dependent manner. Rats given droperidol (3 mg/kg) over an extended period of time develop a notable tolerance to all activity parameters observed in the open environment. Withdrawing from droperidol increases reactivity to apomorphine-induced stereotyped behavior.[3]
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| References |
| Molecular Formula |
C22H22FN3O2
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|---|---|
| Molecular Weight |
379.43
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| Exact Mass |
379.17
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| Elemental Analysis |
C, 69.64; H, 5.84; F, 5.01; N, 11.07; O, 8.43
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| CAS # |
548-73-2
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| Appearance |
Solid powder
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| SMILES |
C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F
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| InChi Key |
RMEDXOLNCUSCGS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22FN3O2/c23-17-9-7-16(8-10-17)21(27)6-3-13-25-14-11-18(12-15-25)26-20-5-2-1-4-19(20)24-22(26)28/h1-2,4-5,7-11H,3,6,12-15H2,(H,24,28)
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| Chemical Name |
3-[1-[4-(4-fluorophenyl)-4-oxobutyl]-3,6-dihydro-2H-pyridin-4-yl]-1H-benzimidazol-2-one
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| Synonyms |
Inapsine; Dridol; Dehydrobenzperidol; Properidol; Droperidol; Droleptan; Inapsine; Janssen Brand of Droperidol; Kern Brand of Droperidol; Taylor Brand of Droperidol;
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: ~76 mg/mL (~200.3 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.59 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 (6.59 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6355 mL | 13.1777 mL | 26.3553 mL | |
| 5 mM | 0.5271 mL | 2.6355 mL | 5.2711 mL | |
| 10 mM | 0.2636 mL | 1.3178 mL | 2.6355 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 |
| NCT05244460 | Recruiting | Drug: Diphenhydramine Drug: Droperidol Injectable Product |
Cannabis Hyperemesis Syndrome | Mercy Health Ohio | December 2, 2021 | Phase 3 |
| NCT05401058 | Recruiting | Drug: Droperidol Injection Drug: Saline |
Digestive System Disease Urologic Diseases |
RenJi Hospital | November 21, 2022 | Not Applicable |
| NCT00702442 | Completed | Drug: Droperidol Drug: Saline solution |
Vomiting | Aristotle University Of Thessaloniki |
June 2008 | Phase 4 |
| NCT04411069 | Completed | Drug: Droperidol | Postoperative Nausea Postoperative Vomiting |
Instituto do Cancer do Estado de São Paulo |
February 20, 2019 | Phase 2 |
| NCT02744495 | Completed | Drug: Betamethasone Drug: Droperidol |
Postoperative Vomiting Postoperative Nausea |
Hôpital Privé de Parly II - Le Chesnay |
February 2016 | Phase 3 |
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