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Chemical Compound Review

Remoxipride     3-bromo-N-[[(2S)-1- ethylpyrrolidin-2...

Synonyms: Roxiam, Remoxiprida, Romoxipride, Remoxipridum, Tocris-0916, ...
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Disease relevance of Remoxipride


Psychiatry related information on Remoxipride


High impact information on Remoxipride


Chemical compound and disease context of Remoxipride


Biological context of Remoxipride


Anatomical context of Remoxipride


Associations of Remoxipride with other chemical compounds

  • Sixty-two DSM III chronic schizophrenic inpatients were selected for a double-blind, placebo controlled, multi-centre, relapse prevention study of remoxipride, a selective dopamine (D2)-receptor antagonist [26].
  • We have used 123I-IBZM single photon emission tomography (SPET) to characterize the patterns of striatal D2 receptor binding in vivo in DSMIII-R-diagnosed schizophrenic and schizo-affective patients treated with either risperidone (n = 6) or remoxipride (n = 4) but predominantly EPS free [27].
  • Pretreatment with dopamine receptor blockers [D1 (SCH 39166, 0.1 mg/kg) or D2 (remoxipride, 3.0 mg/kg and nemonapride, 0.003 mg/kg)] and low-efficacy agonists [D1 (SKF 77434; 3.0 mg/kg) or D2 (SDZ 208-911 and SDZ 208-912; 0.01-0.03 mg/kg)] antagonized the discriminative-stimulus effects of methamphetamine [28].
  • This Mg(2+)-free LTP was blocked by dopamine depletion and by the dopamine D-1/D-5 receptor antagonist SCH 23390 but was not blocked by the dopamine D-2 receptor antagonist remoxipride or the GABA(A) antagonist picrotoxin [29].
  • The potential antipsychotic agents BMY 14802, remoxipride, tiospirone and gevotriline (WY 47,384) have a relatively high affinity for sigma binding sites in brain tissue [30].

Gene context of Remoxipride

  • The newer, atypical antipsychotics such as quetiapine, remoxipride, clozapine, olanzapine, sertindole, ziprasidone, and amisulpride all bind more loosely than dopamine to the dopamine D2 receptor and have dissociation constants higher than that for dopamine [31].
  • While 5-HT2A receptors are readily blocked at low dosages of most atypical antipsychotic drugs (with the important exceptions of remoxipride and amisulpride, neither of which is available for use in Canada) the dosages at which this happens are below those needed to alleviate psychosis [31].
  • A further aim was to compare the prolactin response following remoxipride and thyrotropin release hormone (TRH) during the refractory period [32].
  • The effect of remoxipride on prolactin release is probably not due to an interaction with D2 receptors since GH4C1 cells, in contrast to GH3 and GH4ZR7 cells, are completely devoid of D2 receptors; in contrast, we have previously shown that the D2 antagonist haloperidol causes prolactin release from D2 receptor-expressing cells, only [33].
  • MDMA (5 mg kg(-1) i.p.) produced a rapid decrease in rectal temperature in rats at Ta 15 degrees C. This response was blocked by pretreatment with the dopamine D2 receptor antagonist remoxipride (10 mg kg(-1) i.p.), but unaltered by pretreatment with the D1 antagonist SCH23390 (1.1 mg kg(-1) i.p) [34].

Analytical, diagnostic and therapeutic context of Remoxipride


  1. Early phase II clinical trial of remoxipride in treatment of schizophrenia with measurements of prolactin and neuroleptic activity. Chouinard, G. Journal of clinical psychopharmacology. (1987) [Pubmed]
  2. Characterization of glutathione conjugates of the remoxipride hydroquinone metabolite NCQ-344 formed in vitro and detection following oxidation by human neutrophils. Erve, J.C., Svensson, M.A., von Euler-Chelpin, H., Klasson-Wehler, E. Chem. Res. Toxicol. (2004) [Pubmed]
  3. The pharmacology of the acute hyperthermic response that follows administration of 3,4-methylenedioxymethamphetamine (MDMA, 'ecstasy') to rats. Mechan, A.O., Esteban, B., O'Shea, E., Elliott, J.M., Colado, M.I., Green, A.R. Br. J. Pharmacol. (2002) [Pubmed]
  4. Behavioural analysis of changes in nociceptive thresholds produced by remoxipride in sheep and rats. Main, D.C., Waterman, A.E., Kilpatrick, I.C. Eur. J. Pharmacol. (1995) [Pubmed]
  5. Symptomatic relief from treatment-induced psychosis in Parkinson's disease: an open-label pilot study with remoxipride. Mendis, T., Mohr, E., George, A., Rusk, I.N., Gray, P., Grimes, J.D. Mov. Disord. (1994) [Pubmed]
  6. Effects of remoxipride on measures of psychological performance in healthy volunteers. Fagan, D., Scott, D.B., Mitchell, M., Tiplady, B. Psychopharmacology (Berl.) (1991) [Pubmed]
  7. The Australian multicentre double-blind comparative study of remoxipride and thioridazine in schizophrenia. Keks, N., McGrath, J., Lambert, T., Catts, S., Vaddadi, K., Burrows, G., Varghese, F., George, T., Hustig, H., Burnett, P. Acta psychiatrica Scandinavica. (1994) [Pubmed]
  8. Development of behavioral sensitization to the cocaine-like fungicide triadimefon is prevented by AMPA, NMDa, DA D1 but not DA D2 receptor antagonists. Reeves, R., Thiruchelvam, M., Cory-Slechta, D.A. Toxicol. Sci. (2004) [Pubmed]
  9. Antipsychotic effect of remoxipride, a new substituted benzamide with selective antidopaminergic activity. Lund Laursen, A., Gerlach, J. Acta psychiatrica Scandinavica. (1986) [Pubmed]
  10. A common action of clozapine, haloperidol, and remoxipride on D1- and D2-dopaminergic receptors in the primate cerebral cortex. Lidow, M.S., Goldman-Rakic, P.S. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  11. Regulation of depotentiation and long-term potentiation in the dentate gyrus of freely moving rats by dopamine D2-like receptors. Manahan-Vaughan, D., Kulla, A. Cereb. Cortex (2003) [Pubmed]
  12. Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors. Seeman, P., Corbett, R., Van Tol, H.H. Neuropsychopharmacology (1997) [Pubmed]
  13. Remoxipride. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in schizophrenia. Wadworth, A.N., Heel, R.C. Drugs (1990) [Pubmed]
  14. Remoxipride versus haloperidol in healthy volunteers: psychometric performance and subjective tolerance profiles. Rammsayer, T., Gallhofer, B. International clinical psychopharmacology. (1995) [Pubmed]
  15. Hypotensive and bradycardic effects elicited by spinal dopamine receptor stimulation: effects of D1 and D2 receptor agonists and antagonists. Pellissier, G., Demenge, P. J. Cardiovasc. Pharmacol. (1991) [Pubmed]
  16. Remoxipride in Parkinson's disease: differential response in patients with dyskinesias fluctuations versus psychosis. Lang, A.E., Sandor, P., Duff, J. Clinical neuropharmacology. (1995) [Pubmed]
  17. Effects of remoxipride's metabolites on dopamine D2 receptors and receptor functions in the rat. Ogren, S.O., Hall, H., Widman, M., Angeby-Möller, K. Pharmacol. Toxicol. (1993) [Pubmed]
  18. Functional changes implicating dopaminergic systems following perinatal treatments. Archer, T., Fredriksson, A. Developmental pharmacology and therapeutics. (1992) [Pubmed]
  19. Pharmacokinetics and effects on prolactin of remoxipride in patients with tardive dyskinesia. Widerlöv, E., Andersson, U., von Bahr, C., Nilsson, M.I. Psychopharmacology (Berl.) (1991) [Pubmed]
  20. Steady-state pharmacokinetics of controlled release and immediate release formulations of remoxipride in patients with chronic schizophrenia. Tench, D., Soni, S.D., Ashwood, T., Movin, G. Psychopharmacology (Berl.) (1990) [Pubmed]
  21. Effects of remoxipride, a dopamine D-2 antagonist antipsychotic, on sleep-waking patterns and EEG activity in rats and rabbits. Ongini, E., Bo, P., Dionisotti, S., Trampus, M., Savoldi, F. Psychopharmacology (Berl.) (1992) [Pubmed]
  22. Investigation into the antinociceptive potential of remoxipride administered intrathecally in sheep. Main, D.C., Waterman, A.E., Kilpatrick, I.C. Naunyn Schmiedebergs Arch. Pharmacol. (1997) [Pubmed]
  23. Remoxipride: pharmacokinetics and effect on plasma prolactin. Movin-Osswald, G., Hammarlund-Udenaes, M. British journal of clinical pharmacology. (1991) [Pubmed]
  24. High concentrations of the neuroleptic remoxipride block voltage-activated Na+ channels in central and peripheral nerve membranes. Westlind-Danielsson, A., Ericsson, G., Sandell, L., Elinder, F., Arhem, P. Eur. J. Pharmacol. (1992) [Pubmed]
  25. Comparison of the effect of substituted benzamides on midbrain dopamine neurones after treatment of rats for 21 days. Skarsfeldt, T. Eur. J. Pharmacol. (1993) [Pubmed]
  26. A placebo controlled trial of remoxipride in the prevention of relapse in chronic schizophrenia. King, D.J., Blomqvist, M., Cooper, S.J., Doherty, M.M., Mitchell, M.J., Montgomery, R.C. Psychopharmacology (Berl.) (1992) [Pubmed]
  27. Dopamine D2 receptor blockade in vivo with the novel antipsychotics risperidone and remoxipride--an 123I-IBZM single photon emission tomography (SPET) study. Busatto, G.F., Pilowsky, L.S., Costa, D.C., Ell, P.J., Verhoeff, N.P., Kerwin, R.W. Psychopharmacology (Berl.) (1995) [Pubmed]
  28. Drug discrimination in methamphetamine-trained monkeys: agonist and antagonist effects of dopaminergic drugs. Tidey, J.W., Bergman, J. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  29. Dopamine D-1/D-5 receptor activation is required for long-term potentiation in the rat neostriatum in vitro. Kerr, J.N., Wickens, J.R. J. Neurophysiol. (2001) [Pubmed]
  30. Neuroendocrinological and neurochemical effects of sigma ligands. Gudelsky, G.A., Nash, J.F. Neuropharmacology (1992) [Pubmed]
  31. Atypical antipsychotics: mechanism of action. Seeman, P. Canadian journal of psychiatry. Revue canadienne de psychiatrie. (2002) [Pubmed]
  32. Influence of the dosing interval on prolactin release after remoxipride. Movin-Osswald, G., Hammarlund-Udenaes, M., Von Bahr, C., Eneroth, P., Walton-Bowen, K. British journal of clinical pharmacology. (1995) [Pubmed]
  33. Effects of remoxipride and raclopride on prolactin release from clonal pituitary tumour cells. Nilsson, C.L., Eriksson, E. Pharmacol. Toxicol. (1995) [Pubmed]
  34. Studies on the effect of MDMA ('ecstasy') on the body temperature of rats housed at different ambient room temperatures. Green, A.R., O'Shea, E., Saadat, K.S., Elliott, J.M., Colado, M.I. Br. J. Pharmacol. (2005) [Pubmed]
  35. Remoxipride--a new potential antipsychotic compound. Tolerability and pharmacokinetics after single oral and intravenous administration in healthy male volunteers. Grind, M., Nilsson, M.I., Nilsson, L., Oxenstierna, G., Sedvall, G., Wahlén, A. Psychopharmacology (Berl.) (1989) [Pubmed]
  36. Double blind comparative study of remoxipride and haloperidol in acute schizophrenic patients. Den Boer, J.A., Ravelli, D.P., Huisman, J., Ohrvik, J., Verhoeven, W.M., Westenberg, H.G. Psychopharmacology (Berl.) (1990) [Pubmed]
  37. Tolerability of remoxipride in the long term treatment of schizophrenia. An overview. Holm, A.C., Edsman, I., Lundberg, T., Odlind, B. Drug safety : an international journal of medical toxicology and drug experience. (1993) [Pubmed]
  38. Determination of remoxipride in plasma and urine by reversed-phase column liquid chromatography. Nilsson, L.B. J. Chromatogr. (1990) [Pubmed]
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