Disease relevance of Flupentixol

• VE increased significantly after 10 min of hypoxia in the piglets that received flupentixol independent of whether the carotid bodies were intact or denervated [1].
• A 51-year-old man treated for 2 years with flupentixol, an incisive neuroleptic, developed severe dyspnea due to intermittent, rhythmic, and dystonic movements of the vocal cords and upper airway [2].
• The mixed D1/D2 dopaminergic antagonists chlorpromazine, haloperidol and flupentixol inhibited 3H-Thymidine incorporation into adult BALB/c mouse spleen cells stimulated by concanavalin A, lipopolysaccharide from Escherichia coli, and allogenic cells in a mixed lymphocyte reaction [3].

Psychiatry related information on Flupentixol

• Biochemical measures in patients with a somatoform pain disorder, before, during, and after treatment with amitriptyline with or without flupentixol [4].
• Objective and subjective assessments of the effects of flupentixol and benzodiazepines on human psychomotor performance [5].
• The results can be taken as evidence that flupentixol has an impairing effect on human information processing resources; in particular functions related to motor preparation, perceptual analysis, and memory retrieval are affected [6].
• Flupentixol (0.5 mg/kg) had a slight inhibitory effect on exploratory behavior and no effect on nonsexual interaction with a female [7].

High impact information on Flupentixol

• In summary, the data demonstrate that in the nucleotide-trapped low affinity state of Pgp, the allosteric site remains accessible and responsive to modulation by flupentixol (and its closely related analogs), which can reset the high affinity state for [(125)I]IAAP binding without any further nucleotide hydrolysis [8].
• Only structure analogues of flupentixol and fluphenazine with a lipophilic side chain were potent antagonists against 5-HT-evoked Na(+) and Ca(2+) currents [9].
• The inhibitory effects of selected phenothiazines and two geometric stereoisomers of the thioxanthene flupentixol were studied using strains of S. aureus possessing unique efflux-related MDR phenotypes [10].
• This indicates that F983 contributes to inhibition of drug transport by both isomers of flupentixol and plays an important role in stimulation and inhibition of ATP hydrolysis and [125I]IAAP labeling by cis(Z)- and trans(E)-flupentixol, respectively [11].
• The aim of this study was to evaluate the effect of two neuroleptics, flupentixol and trifluperidol, on the release of pro-apoptotic TNF-alpha and NO by LPS-activated rat microglial cells [12].

Biological context of Flupentixol

• The protection by flupentixol is abolished in the Pgp F983A mutant that is impaired in modulation by flupentixols, indicating involvement of the allosteric site in generating the conformational change [13].

Anatomical context of Flupentixol

• A venous blood sample and an umbilical cord blood sample were obtained from five young women treated with the neuroleptic drug, cis(Z)-flupentixol decanoate in Viscoleo (intramuscularly) or flupentixol (orally) at the time of giving birth [14].
• The chemosensitizing effects of flupentixol were produced by increasing intracellular drug accumulation via a mechanism unrelated to the binding of the plasma membrane P-glycoprotein [15].
• Oral movements induced by the injection of carbachol (1 microgram/0.2 microliter) into the ventral striatum were enhanced by previous injection of this combination of dopamine receptor agonists into the same site and were inhibited by flupentixol [16].
• Flupentixol at 20 and 2 muM reduced IL-1beta by mixed glial cell cultures after 3 days of exposure [17].

Associations of Flupentixol with other chemical compounds

• In this study we demonstrate that substitution of a single phenylalanine residue at position 983 (F983) with alanine (F983A) in putative transmembrane (TM) region 12 selectively affects inhibition of Pgp-mediated drug transport by both isomers of flupentixol [11].
• The present report is a refined analysis of a published double-blind study on the D2/D3-selective antagonist amisulpride (ASP) versus the mixed D1-5/5-HT2 antagonist flupentixol (FPX) [18].
• Seven phenothiazine derivatives, perazine, perphenazine, prochlorperazine, propericiazine, thioproperazine, trifluoperazine, and flupentixol, have been found to be extractable from human plasma and urine samples using disk solid-phase extraction (SPE) with an Empore C18 cartridge [19].
• The non-specific binding of [3H]SCH 39166 in both nucleus caudatus and cerebellum was lower after the addition of SCH 23390 or SCH 39166 than after flupentixol (10 microM) [20].

Gene context of Flupentixol

• Flupentixol at 20 and 2 muM reduced IL-2 release after 1 day of incubation [17].
• In two studies with putative anti-craving agents (the dopamine D2 receptor agonist lisuride and the D2 receptor antagonist flupentixol) we treated alcohol-addicted and non-addicted rats and observed the effects on alcohol taking, alcohol seeking and brain neurotransmission [21].

Analytical, diagnostic and therapeutic context of Flupentixol

• In a double-blind crossover study, patients were treated with amitriptyline combined with a low dose of flupentixol or placebo [4].
• Flupentixol 2 mg proved nearly inert objectively and on visual analogue scales [5].
• A comparison of flupentixol concentrations measured with radioimmunoassay (RIA) and GC was undertaken on 100 plasma samples obtained from 50 schizophrenic patients [22].
• A new method of measuring flupentixol in plasma was developed using gas chromatography (GC) with a nitrogen-phosphorus detector [22].
• The data obtained after oral administration of perazine or flupentixol to a male subject are presented [23].

References