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Droperidol Dopamine Receptor antagonist

Name: Droperidol
Brand: Selleck Chemicals
SKU: S4096
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S4096

Droperidol (NSC 169874,Dehydrobenzperidol) is a potent antagonist of dopamine subtype 2 receptors in the limbic system.

Chemical Structure

Molecular Weight: 379.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.66%

99.66

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Chemical Information, Storage & Stability

Molecular Weight	379.43	Formula	C₂₂H₂₂FN₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	548-73-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 169874,Dehydrobenzperidol			Smiles	C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F

Solubility

In vitro
Batch:

DMSO : 76 mg/mL (200.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.800mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 76 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.450mg/ml (1.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro	Droperidol produces mild α-adrenergic blockade and peripheral vascular dilation. This compound has been shown to block potassium efflux in the myocardium in isolated animal ventricular myocytes, resulting in a dose-dependent delay in repolarization. It has also been shown to induce early depolarizations in isolated animal Purkinje fibers. ^[1]
In vivo	Droperidol (0.01 mM-0.3 mM) increases in a dose-dependent fashion action potential duration (APD) without altering the other parameters in rabbit Purkinje fibers stimulated at 60 pulses/min. This compound (1 mM-3 mM) leads to the reversal of the prolonging effect in rabbit Purkinje fibers. It (10 mM-30 mM) produces shortening in APD at 50% repolarization concomitantly with a significant decrease in Vmax, action potential amplitude and resting membrane potential in rabbit Purkinje fibers. This chemical exerts a dual effect on repolarization, prolongation with low concentrations with development of EADs and subsequent triggered activity in rabbit Purkinje fibers. ^[2] It (3 mg/kg, single dose) decreases dose dependently not only locomotion and rearing frequencies in the open-field but also the apomorphine effects of rats. This compound (3 mg/kg, long term administration) induces significant tolerance to all parameters of activity recorded in the open-field in rats. This chemical withdrawn produces an augmented responsiveness to apomorphine-induced stereotyped behavior. ^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/12658255/ [2] https://pubmed.ncbi.nlm.nih.gov/8355214/ [3] https://pubmed.ncbi.nlm.nih.gov/1775558/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05759481	Recruiting	Post-operative Nausea and Vomiting	Milton S. Hershey Medical Center	February 1 2024	Phase 2
NCT05244460	Recruiting	Cannabis Hyperemesis Syndrome	Mercy Health Ohio\|Lake Erie College of Osteopathic Medicine	December 2 2021	Phase 3

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