Bromperidol - CAS 10457-90-6
Catalog number: 10457-90-6
Category: Inhibitor
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Molecular Formula:
C21H23BrFNO2
Molecular Weight:
420.32
COA:
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Targets:
5-HT Receptor | Dopamine Receptor
Description:
Bromperidol, a derivative of butyrophenone, is an antipsychotic commonly used in the treatment of schizophrenia as it could bind to the D2 dopamine and 5-HT2A serotonin receptor.
Purity:
98%
Appearance:
Tan to Pale Brown Solid
Synonyms:
4-[4-(4-Bromophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone; 4-[4-(p-Bromophenyl)-4-hydroxypiperidino]-4'-fluoro-butyrophenone; Azurene; Impromen; R 11333; R11333; R-11333; Tesoprel
Solubility:
DMSO: 34 mg/mL
Storage:
-20ºC Freeze
MSDS:
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Application:
Bromperidol is an antipsychotic commonly used in the treatment of schizophrenia as it could bind to the D2 dopamine and 5-HT2A serotonin receptor.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Grams-Kilos
Melting Point:
156-158˚C
Density:
1.366 g/cm3
InChIKey:
RKLNONIVDFXQRX-UHFFFAOYSA-N
InChI:
InChI=1S/C21H23BrFNO2/c22-18-7-5-17(6-8-18)21(26)11-14-24(15-12-21)13-1-2-20(25)16-3-9-19(23)10-4-16/h3-10,26H,1-2,11-15H2
Canonical SMILES:
C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F
1.Bromperidol decanoate (depot) for schizophrenia.
Purgato M1, Adams CE. Cochrane Database Syst Rev. 2012 Nov 14;11:CD001719. doi: 10.1002/14651858.CD001719.pub4.
BACKGROUND: Antipsychotic drugs are the mainstay treatment for schizophrenia. Long-acting depot injections of drugs such as bromperidol decanoate are extensively used as a means of long-term maintenance treatment.
2.The pharmacokinetics of long-acting antipsychotic medications.
Spanarello S, La Ferla T1. Curr Clin Pharmacol. 2014;9(3):310-7.
The depot antipsychotics are synthesized by esterification of the active drug to a long chain fatty acid and the resultant compound is then dissolved in a vegetable oil, with the exception of some molecules of new generation characterized by microcrystalline technologies. The absorption rate constant is slower than the elimination rate constant and therefore, the depot antipsychotics exhibit 'flip-flop' kinetics where the time to steady-state is a function of the absorption rate, and the concentration at steady-state is a function of the elimination rate. The pharmacokinetics of depot antipsychotic medications are such that an intramuscular injection given at intervals from 1 to 4 weeks will produce adequate plasma concentrations that are sufficient to prevent relapse over the dosage interval. Such medication is useful in patients who do not reliably take their oral medication. The pharmacokinetics and clinical actions of various depot formulations of antipsychotic drugs have been extensively studied.
3.The use of dried blood spots for quantification of 15 antipsychotics and 7 metabolites with ultra-high performance liquid chromatography - tandem mass spectrometry.
Patteet L1,2, Maudens KE1, Stove CP3, Lambert WE3, Morrens M4, Sabbe B4, Neels H1,2. Drug Test Anal. 2015 Jun;7(6):502-11. doi: 10.1002/dta.1698. Epub 2014 Jul 31.
Therapeutic drug monitoring of antipsychotics is important in optimizing individual therapy. In psychiatric populations, classical venous blood sampling is experienced as frightening. Interest in alternative techniques, like dried blood spots (DBS), has consequently increased. A fast and easy to perform DBS method for quantification of 16 antipsychotics (amisulpride, aripiprazole, asenapine, bromperidol, clozapine, haloperidol, iloperidone, levosulpiride, lurasidone, olanzapine, paliperidone, pipamperone, quetiapine, risperidone, sertindole and zuclopenthixol) and 8 metabolites was developed. DBS were prepared using 25 μL of whole blood and extraction of complete spots was performed using methanol: methyl-t-butyl-ether (4:1). After evaporation, the extract was reconstituted in the mobile phase and 10 μL were injected on an ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). Separation using a C18 column and gradient elution with a flow rate of 0.
4.Withdrawal versus continuation of chronic antipsychotic drugs for behavioural and psychological symptoms in older people with dementia.
Declercq T1, Petrovic M, Azermai M, Vander Stichele R, De Sutter AI, van Driel ML, Christiaens T. Cochrane Database Syst Rev. 2013 Mar 28;3:CD007726. doi: 10.1002/14651858.CD007726.pub2.
BACKGROUND: Antipsychotic agents are often used to treat neuropsychiatric symptoms (NPS) in dementia, although the literature is sceptical about their long-term use for this indication. Their effectiveness is limited and there is concern about adverse effects, including higher mortality with long-term use. When behavioural strategies have failed and drug therapy is instituted, regular attempts to withdraw these drugs are recommended. Physicians, nurses and families of older people with dementia are often reluctant to try to stop antipsychotics, fearing deterioration of NPS. Strategies to reduce antipsychotic use have been proposed, but a systematic review of interventions aimed at withdrawal of antipsychotic agents in older people with dementia has not yet been performed.
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CAS 10457-90-6 Bromperidol

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