Droperidol

Catalog No.S4096 Synonyms: NSC 169874

For research use only.

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

Droperidol Chemical Structure

CAS No. 548-73-2

Selleck's Droperidol has been cited by 1 Publication

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Biological Activity

Description Droperidol (NSC 169874) is a potent antagonist of dopamine subtype 2 receptors in the limbic system.
In vitro

Droperidol produces mild α-adrenergic blockade and peripheral vascular dilation. Droperidol has been shown to block potassium efflux in the myocardium in isolated animal ventricular myocytes, resulting in a dose-dependent delay in repolarization. Droperidol 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. Droperidol (1 mM-3 mM) leads to the reversal of the prolonging effect in rabbit Purkinje fibers. Droperidol (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. Droperidol exerts a dual effect on repolarization, prolongation with low concentrations with development of EADs and subsequent triggered activity in rabbit Purkinje fibers. [2] Droperidol (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. Droperidol (3 mg/kg, long term administration) induces significant tolerance to all parameters of activity recorded in the open-field in rats. Droperidol withdrawn produces an augmented responsiveness to apomorphine-induced stereotyped behavior. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 379.43
Formula

C22H22FN3O2

CAS No. 548-73-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05244460 Recruiting Drug: Droperidol Injectable Product|Drug: Diphenhydramine Cannabis Hyperemesis Syndrome Mercy Health Ohio|Lake Erie College of Osteopathic Medicine December 2 2021 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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