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Chemical Compound Review

Fluanxol     2-[4-[(3E)-3-[2- (trifluoromethyl)thioxanth...

Synonyms: Siplaril, Siplarol, Depixol, Fluxanxol, Flupentixol, ...
 
 
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Disease relevance of Emergil

 

Psychiatry related information on Emergil

 

High impact information on Emergil

  • Ten outpatient crack cocaine smokers with poor prognoses were administered flupenthixol decanoate in an open-label, open-ended trial [10].
  • The stereoselective antagonism of the flupenthixol isomers on several putative cellular targets was studied to explore the mechanism of their chemosensitizing activity. cis- and trans-flupenthixol were equally active inhibitors of protein kinase C and calmodulin [11].
  • Drug substrates that either enhance (calcein acetoxymethyl ester, demecolcine, and vinblastine) or inhibit (cyclosporin A and trans-(E)-flupentixol) ATPase activity of Cys-less or untreated mutant I306C P-glycoprotein did not affect the activity of MTS-verapamil-treated mutant I306C [12].
  • The neuroleptic flupenthixol reduces the expression in rats of the gene coding for NADH-cytochrome b5 reductase as measured by in situ hybridisation and its enzymic manifestation [13].
  • Moreover, drug resistance of KB-8-5 epidermoid cancer cells, which express the wild-type MDR1 gene at levels comparable to clinical specimens from multidrug-resistant cancers, was fully overcome in the presence of trans-(E)-flupentixol [14].
 

Chemical compound and disease context of Emergil

 

Biological context of Emergil

 

Anatomical context of Emergil

 

Associations of Emergil with other chemical compounds

 

Gene context of Emergil

  • Flupenthixol treatment initially raised the prolactin levels about two- or threefold, and a subsequent decline during months 3 and 6 occurred [33].
  • We report here that retroviral vectors encoding a mutant P-glycoprotein (MDR1-F983A) protect hematopoietic cells from anticancer drugs even in the presence of trans-(E)-flupentixol, an inhibitor of P-glycoprotein [14].
  • Forty-five patients with acute schizophrenic illnesses (defined by PSE criteria) were assessed in clinical, cognitive and social terms before being entered in a four week study of the isomers of flupenthixol and placebo [34].
  • CONCLUSION: ECT and MECT combined with flupenthixol were effective in improving psychopathology in patients refractory to antipsychotic medication alone [7].
  • Effect of flupenthixol and butaclamol isomers on prolactin secretion in rats [35].
 

Analytical, diagnostic and therapeutic context of Emergil

References

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  2. Efficacy and tolerability of flupenthixol decanoate in the treatment of depression and psychosomatic disorders: a multicenter trial in general practice. Budde, G. Prog. Neuropsychopharmacol. Biol. Psychiatry (1992) [Pubmed]
  3. Sexual-incentive motivation and paced sexual behavior in female rats after treatment with drugs modifying dopaminergic neurotransmission. Ellingsen, E., Agmo, A. Pharmacol. Biochem. Behav. (2004) [Pubmed]
  4. Flupenthixol decanoate and relapse prevention in alcoholics: results from a placebo-controlled study. Wiesbeck, G.A., Weijers, H.G., Lesch, O.M., Glaser, T., Toennes, P.J., Boening, J. Alcohol Alcohol. (2001) [Pubmed]
  5. Flupenthixol in chronic schizophrenic inpatients: a controlled comparison with haloperidol. Ehmann, T.S., Delva, N.J., Beninger, R.J. Journal of clinical psychopharmacology. (1987) [Pubmed]
  6. Comparison of the prophylactic action of flupenthixol with placebo in lithium treated manic-depressive patients. Esparon, J., Kolloori, J., Naylor, G.J., McHarg, A.M., Smith, A.H., Hopwood, S.E. The British journal of psychiatry : the journal of mental science. (1986) [Pubmed]
  7. Acute and maintenance ECT with flupenthixol in refractory schizophrenia: sustained improvements in psychopathology, quality of life, and social outcomes. Chanpattana, W., Kramer, B.A. Schizophr. Res. (2003) [Pubmed]
  8. Behavioral effects produced by long-term administration of a neuroleptic drug (flupenthixol) upon social interaction in a group of eight rats. Hecht, A. Psychopharmacology (Berl.) (1979) [Pubmed]
  9. Effect of flupenthixol on depression with special reference to combination use with tricyclic antidepressants. An uncontrolled pilot study with 45 patients. Fujiwara, J., Ishino, H., Baba, O., Hanaoka, M., Sasaki, K. Acta psychiatrica Scandinavica. (1976) [Pubmed]
  10. Outpatient treatment of 'crack' cocaine smoking with flupenthixol decanoate. A preliminary report. Gawin, F.H., Allen, D., Humblestone, B. Arch. Gen. Psychiatry (1989) [Pubmed]
  11. Cellular and biochemical characterization of thioxanthenes for reversal of multidrug resistance in human and murine cell lines. Ford, J.M., Bruggemann, E.P., Pastan, I., Gottesman, M.M., Hait, W.N. Cancer Res. (1990) [Pubmed]
  12. Permanent activation of the human P-glycoprotein by covalent modification of a residue in the drug-binding site. Loo, T.W., Bartlett, M.C., Clarke, D.M. J. Biol. Chem. (2003) [Pubmed]
  13. Superoxide, neuroleptics and the ubiquinone and cytochrome b5 reductases in brain and lymphocytes from normals and schizophrenic patients. Whatley, S.A., Curti, D., Das Gupta, F., Ferrier, I.N., Jones, S., Taylor, C., Marchbanks, R.M. Mol. Psychiatry (1998) [Pubmed]
  14. Chemoprotection of hematopoietic cells by a mutant P-glycoprotein resistant to a potent chemosensitizer of multidrug-resistant cancers. Hafkemeyer, P., Licht, T., Pastan, I., Gottesman, M.M. Hum. Gene Ther. (2000) [Pubmed]
  15. Amisulpride: a review of its use in the management of schizophrenia. Curran, M.P., Perry, C.M. Drugs (2001) [Pubmed]
  16. A double-blind comparison of flupenthixol, nortriptyline and diazepam in neurotic depression. Johnson, D.A. Acta psychiatrica Scandinavica. (1979) [Pubmed]
  17. Psychosomatic disorders in general practice: comparisons of treatment with flupenthixol, diazepam and sulpiride. Meyers, C., Vranckx, C., Elgen, K. Pharmatherapeutica. (1985) [Pubmed]
  18. Flupenthixol and Melitracen in the management of trigeminal neuralgia. Bin Yaacob, H. Dental journal of Malaysia. (1985) [Pubmed]
  19. Differential regulation of the consummatory, motivational and anticipatory aspects of feeding behavior by dopaminergic and opioidergic drugs. Barbano, M.F., Cador, M. Neuropsychopharmacology (2006) [Pubmed]
  20. Antipsychotic drugs. Clinical pharmacokinetics of potential candidates for plasma concentration monitoring. Balant-Gorgia, A.E., Balant, L. Clinical pharmacokinetics. (1987) [Pubmed]
  21. Comparison of dopamine receptor sites labeled by [3H]-S-sulpiride and [3H]-spiperone in striatum. Zahniser, N.R., Dubocovich, M.L. J. Pharmacol. Exp. Ther. (1983) [Pubmed]
  22. Stereospecific effect of flupenthixol on neuroreceptor gene expression. De La Concha, A., McKie, J., Hodgkinson, S., Mankoo, B.S., Gurling, H.M. Brain Res. Mol. Brain Res. (1991) [Pubmed]
  23. A double-blind study of flupenthixol ('Fluanxol') in general practice. Ovhed, I. Current medical research and opinion. (1976) [Pubmed]
  24. Evidence for cell loss in corpus striatum after long-term treatment with a neuroleptic drug (flupenithixol) in rats. Nielsen, E.B., Lyon, M. Psychopharmacology (Berl.) (1978) [Pubmed]
  25. The actions of flupenthixol upon 5-hydroxytryptamine-induced aggregation and the uptake of 5-hydroxytryptamine and dopamine by human blood platelets. Boullin, D.J., Grimes, R.P., Orr, M.W. Br. J. Pharmacol. (1975) [Pubmed]
  26. Opposite effects of prefrontal cortex and nucleus accumbens infusions of flupenthixol on stimulant-induced locomotion and brain stimulation reward. Duvauchelle, C.L., Levitin, M., MacConell, L.A., Lee, L.K., Ettenberg, A. Brain Res. (1992) [Pubmed]
  27. Microinjection of cis-flupenthixol, a dopamine antagonist, into the medial preoptic area impairs sexual behavior of male rats. Pehek, E.A., Warner, R.K., Bazzett, T.J., Bitran, D., Band, L.C., Eaton, R.C., Hull, E.M. Brain Res. (1988) [Pubmed]
  28. A controlled comparison of flupenthixol decanoate injections and oral amitriptyline in depressed out-patients. Tam, W., Young, J.P., John, G., Lader, M.H. The British journal of psychiatry : the journal of mental science. (1982) [Pubmed]
  29. Depressive and extrapyramidal symptoms and clinical effects: a trial of fluphenazine versus flupenthixol in maintenance of schizophrenic out-patients. Knights, A., Okasha, M.S., Salih, M.A., Hirsch, S.R. The British journal of psychiatry : the journal of mental science. (1979) [Pubmed]
  30. Do neuroleptics impair learning in schizophrenic patients? Cutmore, T.R., Beninger, R.J. Schizophr. Res. (1990) [Pubmed]
  31. 3-Methoxy-4-hydroxyphenylglycol excretion in acutely schizophrenic patients during a controlled clinical trial of the isomers of flupenthixol. Joseph, M.H., Baker, H.F., Johnstone, E.C., Crow, T.J. Psychopharmacology (Berl.) (1979) [Pubmed]
  32. Dopamine receptor antagonists in the nucleus accumbens attenuate analgesia induced by ventral tegmental area substance P or morphine and by nucleus accumbens amphetamine. Altier, N., Stewart, J. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  33. Long-term effects of the substituted benzamide derivative amisulpride on baseline and stimulated prolactin levels. Schlösser, R., Gründer, G., Anghelescu, I., Hillert, A., Ewald-Gründer, S., Hiemke, C., Benkert, O. Neuropsychobiology (2002) [Pubmed]
  34. The outcome of severe acute schizophrenic illnesses after one year. Johnstone, E.C., Frith, C.D., Gold, A., Stevens, M. The British journal of psychiatry : the journal of mental science. (1979) [Pubmed]
  35. Effect of flupenthixol and butaclamol isomers on prolactin secretion in rats. Meltzer, H.Y., Paul, S.M., Fang, V.S. Psychopharmacology (Berl.) (1977) [Pubmed]
  36. Radioimmunoassay for flupenthixol in plasma. Robinson, J.D., Risby, D. Clin. Chem. (1977) [Pubmed]
  37. Effects of flupenthixol and quadazocine on self-administration of speedball combinations of cocaine and heroin by rhesus monkeys. Mello, N.K., Negus, S.S. Neuropsychopharmacology (1999) [Pubmed]
  38. Pharmacotherapy in the prevention of suicidal behavior. Montgomery, S.A., Montgomery, D.B., Green, M., Bullock, T., Baldwin, D. Journal of clinical psychopharmacology. (1992) [Pubmed]
  39. Long-term behavioural and biochemical effects following prolonged treatment with a neuroleptic drug (flupenthixol) in rats. Nielsen, E.B. Psychopharmacology (Berl.) (1977) [Pubmed]
  40. Comparative double-blind study of flupenthixol decanoate and fluphenazine decanoate in the treatment of patients relapsing in a schizophrenic symptomatology. Wistedt, B., Ranta, J. Acta psychiatrica Scandinavica. (1983) [Pubmed]
 
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