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MedKoo Cat#: 317756 | Name: Droperidol
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Droperidol is a D1DR and D2DR inhibitor, an antidopaminergic drug used as an antiemetic and antipsychotic. Droperidol is also often used for neuroleptanalgesic anesthesia and sedation in intensive-care treatment. It has also been used as an antipsychotic in doses ranging from 5 to 10 mg given as an intramuscular injection, generally in cases of severe agitation in a psychotic patient who is refusing oral medication. Its use in intramuscular sedation has been replaced by intramuscular preparations of haloperidol, midazolam, clonazepam and olanzapine.

Chemical Structure

Droperidol
Droperidol
CAS#548-73-2

Theoretical Analysis

MedKoo Cat#: 317756

Name: Droperidol

CAS#: 548-73-2

Chemical Formula: C22H22FN3O2

Exact Mass: 379.1696

Molecular Weight: 379.44

Elemental Analysis: C, 69.64; H, 5.84; F, 5.01; N, 11.07; O, 8.43

Price and Availability

Size Price Availability Quantity
100mg USD 250.00 2 Weeks
500mg USD 650.00 2 Weeks
1g USD 950.00 2 Weeks
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Related CAS #
No Data
Synonym
Droperidol; Droleptan; Inapsine; Dridol; Dehydrobenzperidol; Properidol; DHBP; NSC 169874; NSC169874; NSC-169874; McN-JR-4749; McN-JR 4749; R4749; R 4749; R-4749;
IUPAC/Chemical Name
3-[1-[4-(4-fluorophenyl)-4-oxobutyl]-3,6-dihydro-2H-pyridin-4-yl]-1H-benzimidazol-2-one
InChi Key
RMEDXOLNCUSCGS-UHFFFAOYSA-N
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)
SMILES Code
C1CN(CC=C1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Droperidol is a Dopamine-2 Receptor Antagonist.
In vitro activity:
Droperidol produces the inhibition of K+ channels in cardiac myocytes. Droperidol (3 x 10(-8) M to 10(-7) M) augmented vasorelaxation and hyperpolarization produced by levcromakalim, whereas phentolamine (3 x 10(-9) M) did not alter this vasorelaxation. These results suggest that droperidol augments vasodilator activity via ATP-sensitive K+ channels. Reference: Anesth Analg. 2006 Mar;102(3):786-91. https://pubmed.ncbi.nlm.nih.gov/16492829/
In vivo activity:
Droperidol attenuates airway smooth muscle contraction. The IC(50) of droperidol on CCh-induced tracheal ring contraction was 13 +/- 2 micromol/l. Droperidol attenuated CCh and aluminum fluoride stimulated inositol monophosphate accumulation. These results suggest that droperidol inhibits G protein coupled phospholipase C, resulting in attenuation of CCh-induced phosphatidylinositol response and subsequent attenuation of contractions of the rat trachea. Reference: Pharmacology. 2003 May;68(1):24-8. https://pubmed.ncbi.nlm.nih.gov/12660476/
Solvent mg/mL mM
Solubility
DMF 20.0 52.71
DMSO 67.0 176.58
DMSO:PBS (pH 7.2) (1:4) 0.2 0.53
Ethanol 0.3 0.66
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 379.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Kinoshita H, Dojo M, Nakahata K, Kimoto Y, Kakutani T, Mizumoto K, Hatano Y. Augmented activity of adenosine triphosphate-sensitive K+ channels induced by droperidol in the rat aorta. Anesth Analg. 2006 Mar;102(3):786-91. doi: 10.1213/01.ane.0000195441.14929.6d. PMID: 16492829. 2. Radke PW, Frenkel C, Urban BW. Molecular actions of droperidol on human CNS ion channels. Eur J Anaesthesiol. 1998 Jan;15(1):89-95. doi: 10.1046/j.1365-2346.1998.00221.x. PMID: 9522147. 3. Shibata O, Saito M, Makita T, Morooka H, Sumikawa K. Droperidol attenuates contractile and phosphatidylinositol responses of rat trachea. Pharmacology. 2003 May;68(1):24-8. doi: 10.1159/000068729. PMID: 12660476. 4. Olschewski A, Bräu ME, Hempelmann G, Vogel W, Safronov BV. Differential block of fast and slow inactivating tetrodotoxin-sensitive sodium channels by droperidol in spinal dorsal horn neurons. Anesthesiology. 2000 Jun;92(6):1667-76. doi: 10.1097/00000542-200006000-00026. PMID: 10839918.
In vitro protocol:
1. Kinoshita H, Dojo M, Nakahata K, Kimoto Y, Kakutani T, Mizumoto K, Hatano Y. Augmented activity of adenosine triphosphate-sensitive K+ channels induced by droperidol in the rat aorta. Anesth Analg. 2006 Mar;102(3):786-91. doi: 10.1213/01.ane.0000195441.14929.6d. PMID: 16492829. 2. Radke PW, Frenkel C, Urban BW. Molecular actions of droperidol on human CNS ion channels. Eur J Anaesthesiol. 1998 Jan;15(1):89-95. doi: 10.1046/j.1365-2346.1998.00221.x. PMID: 9522147.
In vivo protocol:
1. Shibata O, Saito M, Makita T, Morooka H, Sumikawa K. Droperidol attenuates contractile and phosphatidylinositol responses of rat trachea. Pharmacology. 2003 May;68(1):24-8. doi: 10.1159/000068729. PMID: 12660476. 2. Olschewski A, Bräu ME, Hempelmann G, Vogel W, Safronov BV. Differential block of fast and slow inactivating tetrodotoxin-sensitive sodium channels by droperidol in spinal dorsal horn neurons. Anesthesiology. 2000 Jun;92(6):1667-76. doi: 10.1097/00000542-200006000-00026. PMID: 10839918.
1: Tracz K, Owczuk R. Small doses of droperidol do not present relevant torsadogenic actions: a double-blind, ondansetron-controlled study. Br J Clin Pharmacol. 2015 Apr;79(4):669-76. doi: 10.1111/bcp.12527. PubMed PMID: 25293524; PubMed Central PMCID: PMC4386951. 2: Toyoda T, Terao Y, Oji M, Okada M, Araki H, Fukusaki M. [The Interaction of Low-dose Droperidol, Propofol, and Sevoflurane on QTc Prolongation]. Masui. 2015 Jun;64(6):580-5. Japanese. PubMed PMID: 26437544. 3: Thomas MC, Musselman ME, Shewmaker J. Droperidol for the treatment of acute migraine headaches. Ann Pharmacother. 2015 Feb;49(2):233-40. doi: 10.1177/1060028014554445. Epub 2014 Nov 21. Review. PubMed PMID: 25416184. 4: Calver L, Drinkwater V, Gupta R, Page CB, Isbister GK. Droperidol v. haloperidol for sedation of aggressive behaviour in acute mental health: randomised controlled trial. Br J Psychiatry. 2015 Mar;206(3):223-8. doi: 10.1192/bjp.bp.114.150227. Epub 2014 Nov 13. PubMed PMID: 25395689. 5: Fang L, Lin CX, Zhu ZW, Zhao LS, Zhang SY. Elucidation of in vitro phase I metabolites of droperidol using UPLC-QTOF MS. Eur J Drug Metab Pharmacokinet. 2015 Mar;40(1):111-4. doi: 10.1007/s13318-014-0185-x. Epub 2014 Mar 5. PubMed PMID: 24590313. 6: Storrar J, Hitchens M, Platt T, Dorman S. Droperidol for treatment of nausea and vomiting in palliative care patients. Cochrane Database Syst Rev. 2014 Nov 27;11:CD006938. doi: 10.1002/14651858.CD006938.pub3. Review. PubMed PMID: 25429434. 7: Scott JP, Stuth EA, Stucke AG, Cava JR, Berens RJ. Droperidol transiently prolongs the QT interval in children undergoing single ventricle palliation. Pediatr Cardiol. 2015 Jan;36(1):196-204. doi: 10.1007/s00246-014-0985-4. Epub 2014 Aug 3. PubMed PMID: 25087057. 8: Macht M, Mull AC, McVaney KE, Caruso EH, Johnston JB, Gaither JB, Shupp AM, Marquez KD, Haukoos JS, Colwell CB. Comparison of droperidol and haloperidol for use by paramedics: assessment of safety and effectiveness. Prehosp Emerg Care. 2014 Jul-Sep;18(3):375-80. doi: 10.3109/10903127.2013.864353. Epub 2014 Jan 24. PubMed PMID: 24460451. 9: Calver L, Isbister GK. High dose droperidol and QT prolongation: analysis of continuous 12-lead recordings. Br J Clin Pharmacol. 2014 May;77(5):880-6. doi: 10.1111/bcp.12272. PubMed PMID: 24168079; PubMed Central PMCID: PMC4004408. 10: Bērziņš A, Hodgkinson P. Solid-state NMR and computational investigation of solvent molecule arrangement and dynamics in isostructural solvates of droperidol. Solid State Nucl Magn Reson. 2015 Feb;65:12-20. doi: 10.1016/j.ssnmr.2014.09.001. Epub 2014 Sep 17. PubMed PMID: 25282618. 11: Toyoda T, Terao Y, Oji M, Okada M, Fukusaki M, Sumikawa K. The interaction of antiemetic dose of droperidol with propofol on QT interval during anesthetic induction. J Anesth. 2013 Dec;27(6):885-9. doi: 10.1007/s00540-013-1625-5. Epub 2013 May 10. PubMed PMID: 23660990. 12: Kasagi Y, Hayashida M, Sugasawa Y, Kikuchi I, Yamaguchi K, Okutani R, Takeda S, Inada E. Antiemetic effect of naloxone in combination with dexamethasone and droperidol in patients undergoing laparoscopic gynecological surgery. J Anesth. 2013 Dec;27(6):879-84. doi: 10.1007/s00540-013-1630-8. Epub 2013 May 11. PubMed PMID: 23666451. 13: Agámez Medina GL, González-Arévalo A, Gómez-Arnau JI, García del Valle S, Rubio JA, Esteban E, Pérez E. Effects of droperidol and ondansetron on dispersion of ventricular repolarization: A randomized double-blind clinical study in anesthetized adult patients. Rev Esp Anestesiol Reanim. 2015 Nov;62(9):495-501. doi: 10.1016/j.redar.2015.01.017. Epub 2015 Apr 14. English, Spanish. PubMed PMID: 25887095. 14: Nuttall GA, Malone AM, Michels CA, Trudell LC, Renk TD, Marienau ME, Oliver WC, Ackerman MJ. Does low-dose droperidol increase the risk of polymorphic ventricular tachycardia or death in the surgical patient? Anesthesiology. 2013 Feb;118(2):382-6. doi: 10.1097/ALN.0b013e31827dde8d. PubMed PMID: 23291623. 15: Perkins J, Ho JD, Vilke GM, DeMers G. American Academy of Emergency Medicine Position Statement: Safety of Droperidol Use in the Emergency Department. J Emerg Med. 2015 Jul;49(1):91-7. doi: 10.1016/j.jemermed.2014.12.024. Epub 2015 Mar 30. PubMed PMID: 25837231. 16: Chen FC, Fang BX, Li P, Yang JG, Zhou BH. Compatibility of butorphanol and droperidol in 0.9% sodium chloride injection. Am J Health Syst Pharm. 2013 Mar 15;70(6):515-9. doi: 10.2146/ajhp120324. PubMed PMID: 23456405. 17: Chan EW, Taylor DM, Knott JC, Phillips GA, Castle DJ, Kong DC. Intravenous droperidol or olanzapine as an adjunct to midazolam for the acutely agitated patient: a multicenter, randomized, double-blind, placebo-controlled clinical trial. Ann Emerg Med. 2013 Jan;61(1):72-81. doi: 10.1016/j.annemergmed.2012.07.118. Epub 2012 Sep 13. PubMed PMID: 22981685. 18: Budiharto L, De Fruyt J. [Droperidol for the treatment of acutely agitated patients: still an option]. Tijdschr Psychiatr. 2013;55(3):183-92. Review. Dutch. PubMed PMID: 23512631. 19: Beppu Y, Asada A, Morishima K, Kurita S, Nakatani K. [Extrapyramidal reactions in three patients due to droperidol infusion for intravenous patient-controlled analgesia]. Masui. 2013 Apr;62(4):426-30. Japanese. PubMed PMID: 23697194. 20: Ahmad-Sabry MH, Shareghi G. Long-term use of intrathecal droperidol as an excellent antiemetic in nonmalignant pain--a retrospective study. Middle East J Anaesthesiol. 2012 Oct;21(6):857-62. PubMed PMID: 23634568.