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Chemical Compound Review

Amperozida     4-[4,4-bis(4- fluorophenyl)butyl]-N- ethyl...

Synonyms: Amperozide, Amperozidum, Lopac-A-6976, Hogpax vet., SureCN340961, ...
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Disease relevance of Amperozide


Psychiatry related information on Amperozide


High impact information on Amperozide

  • Interaction of the novel antipsychotic drug amperozide and its metabolite FG5620 with central nervous system receptors and monoamine uptake sites: relation to behavioral and clinical effects [9].
  • In the present study amperozide displayed low affinity for several serotonin receptor subtypes as well as for the dopamine D4 receptor transfected in COS7 cells (Ki D4.2 = 769 nmol/L and Ki D4.4 = 384 nmol/L) [9].
  • In addition, after amperozide the number of Fos-positive nuclei was higher in the nucleus accumbens than in the dorsolateral striatum, a characteristic that is common to all known atypical antipsychotic agents [10].
  • The putative atypical antipsychotic drug amperozide preferentially increases c-fos expression in rat medial prefrontal cortex and lateral septum [10].
  • With the exception of the nucleus accumbens-shell, where amperozide failed to produce statistically significant increases, the regional distribution of Fos immunoreactivity following amperozide was similar to that induced by atypical, but not by typical, antipsychotic drugs [10].

Chemical compound and disease context of Amperozide


Biological context of Amperozide

  • Food intake was also suppressed by amperozide at higher doses, whereas it was increased by FG 5974 [7].
  • Amperozide 4-[4,4-bis(4-fluorophenyl)butyl]-N-ethylpiperazine-1- carboxamide) is used in veterinary medicine because of its sedative effect on pigs [12].
  • The suppressive effect of DOI was antagonized by treatment with amperozide, a selective 5-HT2 receptor antagonist, in doses which did not by themselves affect sexual activity [13].
  • Immediately after the experimental treatment, the highest PBL reactivity was found for the amperozide-treated animals and for the non-transported animals, with no differences in reactivity between Hal genotypes [14].
  • Because serotonergic neurons are implicated in both the central mechanisms underlying thermoregulation and the reinforcing effects of alcohol, this study was undertaken to determine whether the poikilothermic effects of alcohol on body temperature (Tb) would be altered by amperozide [15].

Anatomical context of Amperozide

  • Amperozide (2-10 mg/kg, s.c.) significantly increased extracellular levels of DA in both the striatum and nucleus accumbens in a dose-dependent manner [16].
  • Amperozide significantly increased the number of Fos-immunoreactive nuclei in the medial prefrontal cortex and the lateral septum but not in the nucleus accumbens (shell or core), the striatum, or the amygdala [10].
  • The effects of acute, systemic administration of the putative atypical antipsychotic drug amperozide on c-fos expression in the rat forebrain were studied by means of Fos immunohistochemistry [10].
  • The highest dose of amperozide inhibited the activity in substantia nigra pars compacta, showing a liability to induce extrapyramidal side-effects [17].
  • Because amperozide acts centrally on the synaptic activity of dopaminergic and serotonergic neurons in limbic system structures, it is envisaged that the drug ameliorates the aberrant drinking of alcohol by virtue of a direct effect on either one or both of these classes of neurons.(ABSTRACT TRUNCATED AT 250 WORDS)[18]

Associations of Amperozide with other chemical compounds


Gene context of Amperozide


Analytical, diagnostic and therapeutic context of Amperozide


  1. Suppression of alcohol preference in high alcohol drinking rats: efficacy of amperozide versus naltrexone. Myers, R.D., Lankford, M.F. Neuropsychopharmacology (1996) [Pubmed]
  2. Effects of amperozide on biting behavior and performance in restricted-fed pigs following regrouping. Björk, A., Olsson, N.G., Christensson, E., Martinsson, K., Olsson, O. J. Anim. Sci. (1988) [Pubmed]
  3. Antiarrhythmic effect of amperozide, a novel psychotropic compound with class III antiarrhythmic properties, on digoxin-induced arrhythmias in the guinea-pig. Höglund, P., Eriksson, M., Christensson, E.G. J. Pharm. Pharmacol. (1986) [Pubmed]
  4. Amperozide--a new putatively antipsychotic drug with a limbic mode of action on dopamine mediated behaviour. Gustafsson, B., Christensson, E. Pharmacol. Toxicol. (1990) [Pubmed]
  5. The effects of amperozide on cocaine-induced social withdrawal in rats. Rademacher, D.J., Kuppinger, H.E., Thompson, K.J., Harrington, A., Kaczmarek, H.J., Kopish, A.J., Steinpreis, R.E. Behav. Brain Res. (1999) [Pubmed]
  6. Effect of antipsychotic drugs on extracellular serotonin levels in rat medial prefrontal cortex and nucleus accumbens. Ichikawa, J., Kuroki, T., Dai, J., Meltzer, H.Y. Eur. J. Pharmacol. (1998) [Pubmed]
  7. Selective inhibition of alcohol intake in diverse alcohol-preferring rat strains by the 5-HT2A antagonists amperozide and FG 5974. Overstreet, D.H., McArthur, R.A., Rezvani, A.H., Post, C. Alcohol. Clin. Exp. Res. (1997) [Pubmed]
  8. New drugs for the treatment of experimental alcoholism. Myers, R.D. Alcohol (1994) [Pubmed]
  9. Interaction of the novel antipsychotic drug amperozide and its metabolite FG5620 with central nervous system receptors and monoamine uptake sites: relation to behavioral and clinical effects. Svartengren, J., Pettersson, E., Björk, A. Biol. Psychiatry (1997) [Pubmed]
  10. The putative atypical antipsychotic drug amperozide preferentially increases c-fos expression in rat medial prefrontal cortex and lateral septum. Nomikos, G.G., Tham, C.S., Fibiger, H.C., Svensson, T.H. Neuropsychopharmacology (1997) [Pubmed]
  11. Synthesis of dopamine and 5-HT in anatomical regions of the rat's brain is unaffected by sustained infusion of amperozide. Adell, A., Myers, R.D. Pharmacol. Toxicol. (1995) [Pubmed]
  12. Determination of amperozide residues in swine liver using liquid chromatography-mass spectrometry. Balizs, G., Börner, S., Wennemar, A. The Analyst. (1994) [Pubmed]
  13. The selective 5-HT2 receptor antagonist amperozide attenuates 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane-induced inhibition of male rat sexual behavior. Klint, T., Dahlgren, I.L., Larsson, K. Eur. J. Pharmacol. (1992) [Pubmed]
  14. Influence of the Hal locus and standardized stress on antibody response and in vitro reactivity of peripheral blood lymphocytes in pigs. Edfors-Lilja, I., Lundström, K., Nyberg, L., Rundgren, M. Vet. Immunol. Immunopathol. (1987) [Pubmed]
  15. Action of the 5-HT2A antagonist amperozide on alcohol-induced poikilothermia in rats. Myers, R.D., Lankford, M. Pharmacol. Biochem. Behav. (1998) [Pubmed]
  16. Amperozide, a novel antipsychotic drug, inhibits the ability of d-amphetamine to increase dopamine release in vivo in rat striatum and nucleus accumbens. Ichikawa, J., Meltzer, H.Y. J. Neurochem. (1992) [Pubmed]
  17. Differential effects of repeated administration of novel antipsychotic drugs on the activity of midbrain dopamine neurons in the rat. Skarsfeldt, T. Eur. J. Pharmacol. (1995) [Pubmed]
  18. Selective reduction by the 5-HT antagonist amperozide of alcohol preference induced in rats by systemic cyanamide. Myers, R.D., Lankford, M., Björk, A. Pharmacol. Biochem. Behav. (1992) [Pubmed]
  19. BIMG 80, a novel potential antipsychotic drug: evidence for multireceptor actions and preferential release of dopamine in prefrontal cortex. Volonté, M., Monferini, E., Cerutti, M., Fodritto, F., Borsini, F. J. Neurochem. (1997) [Pubmed]
  20. Amperozide and clozapine but not haloperidol or raclopride increase the secretion of oxytocin in rats. Uvnäs-Moberg, K., Alster, P., Svensson, T.H. Psychopharmacology (Berl.) (1992) [Pubmed]
  21. Effects of amperozide, 8-OH-DPAT, and FG 5974 on operant responding for ethanol. Roberts, A.J., McArthur, R.A., Hull, E.E., Post, C., Koob, G.F. Psychopharmacology (Berl.) (1998) [Pubmed]
  22. Dopamine D1, D2 and serotonin2 receptor occupation by typical and atypical antipsychotic drugs in vivo. Matsubara, S., Matsubara, R., Kusumi, I., Koyama, T., Yamashita, I. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  23. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. Roth, B.L., Craigo, S.C., Choudhary, M.S., Uluer, A., Monsma, F.J., Shen, Y., Meltzer, H.Y., Sibley, D.R. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  24. Alcohol intake in high alcohol drinking (HAD) rats is suppressed by FG5865, a novel 5-HT1A agonist/5-HT2 antagonist. Long, T.A., Kalmus, G.W., Björk, A., Myers, R.D. Pharmacol. Biochem. Behav. (1996) [Pubmed]
  25. Effects of amperozide in schizophrenia. An open study of a potent 5-HT2 receptor antagonist. Axelsson, R., Nilsson, A., Christensson, E., Björk, A. Psychopharmacology (Berl.) (1991) [Pubmed]
  26. Involvement of the 5-HT2 receptor in the 5-HT receptor-mediated stimulation of prolactin release. Albinsson, A., Palazidou, E., Stephenson, J., Andersson, G. Eur. J. Pharmacol. (1994) [Pubmed]
  27. The limbic functional selectivity of amperozide is not mediated by dopamine D2 receptors as assessed by in vitro and in vivo binding. Svartengren, J., Celander, M. Eur. J. Pharmacol. (1994) [Pubmed]
  28. High frequency oral movements induced by long-term administration of amperozide but not FG5803 in rats. Liminga, U., Andren, P.E., Ohlund, L.S., Gunne, L.M. Psychopharmacology (Berl.) (1996) [Pubmed]
  29. Effects of amperozide in two animal models of anxiety. Engel, J.A., Egbe, P., Liljequist, S., Söderpalm, B. Pharmacol. Toxicol. (1989) [Pubmed]
  30. Observations on the action of amperozide: are there social influences on sow-litter productivity? Kyriakis, S.C., Olsson, N.G., Martinsson, K., Björk, A.K. Res. Vet. Sci. (1991) [Pubmed]
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