Fluspirilene - CAS 1841-19-6
Catalog number:
1841-19-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C29H31F2N3O
Molecular Weight:
475.57
COA:
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Targets:
Calcium Channel | Dopamine Receptor
Description:
Fluspirilene, with antipsychotic activity, is a non-competitive antagonist of agonist-activated L-type calcium channels (IC50 = 0.03 µM). Fluspirilene is also a dopamine inhibitor.
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Purity:
>98%
Appearance:
Light yellow solid powder
Synonyms:
FLUSPIRILENE;8-(4,4-BIS[P-FLUOROPHENYL]BUTYL)-1-PHENYL-1,3,8-TRIAZINO(4,5)DECAN-4-ONE;R 6218;1-phenyl-4-oxo-8-(4,4-bis(4-fluorophenyl)butyl)-1,3,8-triazaspiro(4,5)decane;8-(4,4-bis(p-fluorophenyl)butyl)-1-phenyl-1,3,8-triazaspiro(4,5)decan-4-one;8-triaza
MSDS:
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InChIKey:
QOYHHIBFXOOADH-UHFFFAOYSA-N
InChI:
1S/C29H31F2N3O/c30-24-12-8-22(9-13-24)27(23-10-14-25(31)15-11-23)7-4-18-33-19-16-29(17-20-33)28(35)32-21-34(29)26-5-2-1-3-6-26/h1-3,5-6,8-15,27H,4,7,16-21H2,(H,32,35)
Canonical SMILES:
FC1=CC=C(C(C2=CC=C(F)C=C2)CCCN3CCC4(C(NCN4C5=CC=CC=C5)=O)CC3)C=C1
1.Chronic deep brain stimulation in patients with tardive dystonia without a history of major psychosis.
Capelle HH1, Blahak C, Schrader C, Baezner H, Kinfe TM, Herzog J, Dengler R, Krauss JK. Mov Disord. 2010 Jul 30;25(10):1477-81. doi: 10.1002/mds.23123.
Tardive dystonia usually occurs with a delay after neuroleptic exposure in patients with major psychosis. A subgroup of patients, however, is given such medication for "mild depression" or "neurasthenia." Tardive dystonia, in general, may respond favorably to pallidal deep brain stimulation (DBS). Nevertheless, it remains unclear thus far whether or not similar beneficial outcome is achieved with pallidal DBS in different subgroups of patients with tardive dystonia. Four women (mean age 59 years at surgery) underwent stereotactic pallidal DBS in the frame of an observational study. Tardive dystonia occurred secondary to medication with fluspirilene and haloperidol, and injection of long-acting depot neuroleptics prescribed for mild depression or "nervousness." Assessment included the Burke-Fahn-Marsden (BFM) scale preoperatively and at 12 months follow-up. Extended follow-up was available at a mean of 27.3 months postoperatively (range 16-36 months).
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.[Trichoma (Plica polonica) - a contemporary case with a historical disease].
Wolf F1, Scherr M, Scherthöffer D, Bäuml J, Förstl H. Neuropsychiatr. 2008;22(2):124-6.
We describe a 62-year-old patient with a chronic delusional disorder who presented with severely matted hair ("plica polonica"). Until the late 19th century such dreadlocks were considered as cause, consequence and treatment of mental disease. The historical development of "plica polonica" is briefly reviewed as an example of early and once popular psychiatric disease concepts.
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 1841-19-6 Fluspirilene

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