Details
Stereochemistry | ACHIRAL |
Molecular Formula | C23H25F3N2OS |
Molecular Weight | 434.5196 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
c1ccc2c(c1)/C(=C(\[H])/CCN3CCN(CC3)CCO)/c4cc(ccc4S2)C(F)(F)F
InChI
InChIKey=NJMYODHXAKYRHW-DVZOWYKESA-N
InChI=1S/C23H25F3N2OS/c24-23(25,26)17-7-8-22-20(16-17)18(19-4-1-2-6-21(19)30-22)5-3-9-27-10-12-28(13-11-27)14-15-29/h1-2,4-8,16,29H,3,9-15H2/b18-5-
DescriptionCurator's Comment:: Description was created based on several sources, including https://www.medicines.org.uk/emc/PIL.5400.latest.pdf | http://www.lundbeck.com/upload/au/files/pdf/Fluanxol_CMI.pdf
Curator's Comment:: Description was created based on several sources, including https://www.medicines.org.uk/emc/PIL.5400.latest.pdf | http://www.lundbeck.com/upload/au/files/pdf/Fluanxol_CMI.pdf
Flupenthixol is a thioxanthene antipsychotic used in the treatment of schizophrenia and other psychoses, with the exception of mania and psychomotor hyperactivity due to an activating effect associated with this drug. It may also be employed as an antidepressant. Flupenthixol has a wide range of pharmacological actions. Flupenthixol blocks dopaminergic receptors, thus interfering with dopaminergic transmission in the brain. Flupenthixol also inhibits serotonin 5-HT, histamine H1,
muscarinic and alpha-1 adrenergic receptors.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL217 Sources: DOI: 10.1016/B978-008055232-3.61770-2 |
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Target ID: CHEMBL2095200 |
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Target ID: CHEMBL2094251 |
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Target ID: CHEMBL231 |
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Target ID: CHEMBL2094109 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | FLUANXOL Approved UseFlupentixol Decanoate Injection and Flupentixol Dihydrochloride Tablets
Indication: Schizophrenia and allied psychoses, especially with symptoms such as hallucinations, delusions and thought disturbances along with apathy, lowered mood and withdrawal. |
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Primary | FLUANXOL Approved UseFluanxol is used to treat depression in patients who may, or may not, also be showing signs of anxiety. |
PubMed
Title | Date | PubMed |
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[Allergotoxic brain reaction to flupentixol-depot]. | 1976 Mar-Apr |
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A controlled comparison of flupenthixol and amitriptyline in depressed outpatients. | 1976 May 8 |
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Depot injections and tardive dyskinesia. | 1978 Oct |
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Effects of chronic treatment with antidepressants on aggressiveness induced by clonidine in mice. | 1982 |
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Abnormal involuntary movements: a study of dopaminergic receptor interaction. | 1983 |
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The antibacterial effect of selected phenothiazines and thioxanthenes on slow-growing mycobacteria. | 1986 Dec |
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Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. | 1994 Feb 1 |
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Mitochondrial involvement in schizophrenia and other functional psychoses. | 1996 Sep |
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Tolerability of low dose neuroleptics: a case control study of flupenthixol. | 1997 Nov |
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Flupenthixol treatment for cocaine abusers with schizophrenia: a pilot study. | 1998 Aug |
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Effect of flupenthixol on subjective and cardiovascular responses to intravenous cocaine in humans. | 2001 Nov 1 |
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Permanent activation of the human P-glycoprotein by covalent modification of a residue in the drug-binding site. | 2003 Jun 6 |
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Encephalopathy and myoclonus triggered by valproic acid. | 2004 Sep |
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[Trazodone for the treatment of behavioral and psychological symptoms of dementia (BPSD) in Alzheimer's disease: a retrospective study focused on the aggression and negativism in caregiving situations]. | 2006 Jun |
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Post-training intra-striatal scopolamine or flupenthixol impairs radial maze learning in rats. | 2006 Jun 3 |
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Cell specific dopamine modulation of the transient potassium current in the pyloric network by the canonical D1 receptor signal transduction cascade. | 2010 Aug |
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The monoamine oxidase A inhibitor clorgyline is a broad-spectrum inhibitor of fungal ABC and MFS transporter efflux pump activities which reverses the azole resistance of Candida albicans and Candida glabrata clinical isolates. | 2012 Mar |
Patents
Sample Use Guides
Fluanxol® (flupentixol) 0.5 mg and 1 mg film-coated tablets.
The starting dose is usually 1 mg daily taken as a single dose in the morning. This may be increased to 2 mg per day after one week. The maximum daily dose is 3 mg per day.
Fluanxol® (flupenthixol decanoate) Depot 20 mg/mL, Concentrated Depot 100 mg/mL.
Generally, the starting dose is 20 to 40 mg (1 to 2 mL). A second dose of 20 to 40 mg (1 to 2 mL) is usually given 4-10 days after the first injection, and further doses are given every 2 to 4 weeks for the majority of patients.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26945819
Fupentixol inhibited the proton currents in BV2 microglial cells in a concentration-dependent manner (IC50 6.6 uM).
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FA0UYH6QUO
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258-756-4
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5281881
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53772-82-0
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SUBSTANCE RECORD