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Chemical Compound Review

pimozide     3-[1-[4,4-bis(4- fluorophenyl)butyl]-4...

Synonyms: pimozida, Antalon, Orap, Orap forte, R-6238, ...
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Disease relevance of pimozide


Psychiatry related information on pimozide


High impact information on pimozide


Chemical compound and disease context of pimozide


Biological context of pimozide


Anatomical context of pimozide

  • Reward-blocking doses of the neuroleptic pimozide activated the caudate and the lateral habenula but did not alter any of the unilateral effects of stimulation [19].
  • Forebrain origins and terminations of the medial forebrain bundle metabolically activated by rewarding stimulation or by reward-blocking doses of pimozide [19].
  • Pimozide inhibited LMC by 50% at 15 microM but caused a substantial decrease in lymphocyte ATP content and viability at this concentration [20].
  • In whole-cell patch-clamp experiments, pimozide blocked Ca2+ current through L type channels of rat ventricular myocytes, in a voltage-dependent manner [21].
  • Endocrine effects of pimozide, a specific dopaminergic blocker [22].

Associations of pimozide with other chemical compounds


Gene context of pimozide

  • Our results suggest that pimozide metabolism is catalyzed mainly by CYP3A, but CYP1A2 also contributes [28].
  • Pimozide itself was a potent inhibitor of CYP2D6 in HLMs when preincubated for 15 min (Ki = 0.75 +/- 0.98 microM) and a moderate inhibitor of CYP3A (Ki = 76.7 +/- 34.5 microM), with no significant effect on other isoforms tested [28].
  • Clarithromycin inhibited CYP3A-mediated pimozide metabolism and the resulting elevation in plasma concentrations may increase the risk of pimozide cardiotoxicity [15].
  • Pimozide was without effect on SRIF release and did not alter the stimulatory effect of hGRF-40 [29].
  • Tail-pinch- or CRF-induced food intake was blocked by naloxone, pimozide, and spiperone [30].

Analytical, diagnostic and therapeutic context of pimozide


  1. Treatment of metastatic malignant melanoma with pimozide. Taub, R.N., Baker, M.A. Lancet (1979) [Pubmed]
  2. Functional ion channels in pulmonary alveolar type I cells support a role for type I cells in lung ion transport. Johnson, M.D., Bao, H.F., Helms, M.N., Chen, X.J., Tigue, Z., Jain, L., Dobbs, L.G., Eaton, D.C. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  3. Inhibition of human breast cancer cell proliferation in tissue culture by the neuroleptic agents pimozide and thioridazine. Strobl, J.S., Kirkwood, K.L., Lantz, T.K., Lewine, M.A., Peterson, V.A., Worley, J.F. Cancer Res. (1990) [Pubmed]
  4. Increased lethality of calmodulin antagonists and bleomycin to human bone marrow and bleomycin-resistant malignant cells. Lazo, J.S., Chen, D.L., Gallicchio, V.S., Hait, W.N. Cancer Res. (1986) [Pubmed]
  5. Pimozide in treatment of anorexia nervosa. Plantey, F. Lancet (1977) [Pubmed]
  6. Controlled study of haloperidol, pimozide and placebo for the treatment of Gilles de la Tourette's syndrome. Shapiro, E., Shapiro, A.K., Fulop, G., Hubbard, M., Mandeli, J., Nordlie, J., Phillips, R.A. Arch. Gen. Psychiatry (1989) [Pubmed]
  7. Lack of behavioral supersensitivity to d-amphetamine after pimozide withdrawal. A trial with schizophrenic patients. van Kammen, D.P., Docherty, J.P., Marder, S.R., Schulz, S.C., Bunney, W.E. Arch. Gen. Psychiatry (1980) [Pubmed]
  8. Monoaminergic mechanisms and experimental cataplexy. Foutz, A.S., Delashaw, J.B., Guilleminault, C., Dement, W.C. Ann. Neurol. (1981) [Pubmed]
  9. Placebo-controlled study of pimozide augmentation of fluoxetine in body dysmorphic disorder. Phillips, K.A. The American journal of psychiatry. (2005) [Pubmed]
  10. Activation of mouse sperm T-type Ca2+ channels by adhesion to the egg zona pellucida. Arnoult, C., Cardullo, R.A., Lemos, J.R., Florman, H.M. Proc. Natl. Acad. Sci. U.S.A. (1996) [Pubmed]
  11. The Ca(2+) channel antagonists mibefradil and pimozide inhibit cell growth via different cytotoxic mechanisms. Bertolesi, G.E., Shi, C., Elbaum, L., Jollimore, C., Rozenberg, G., Barnes, S., Kelly, M.E. Mol. Pharmacol. (2002) [Pubmed]
  12. Neuroleptics in the short-term treatment of anorexia nervosa. A double-blind placebo-controlled study with sulpiride. Vandereycken, W. The British journal of psychiatry : the journal of mental science. (1984) [Pubmed]
  13. Studies on the mechanism of a fatal clarithromycin-pimozide interaction in a patient with Tourette syndrome. Flockhart, D.A., Drici, M.D., Kerbusch, T., Soukhova, N., Richard, E., Pearle, P.L., Mahal, S.K., Babb, V.J. Journal of clinical psychopharmacology. (2000) [Pubmed]
  14. Risperidone versus pimozide in Tourette's disorder: a comparative double-blind parallel-group study. Bruggeman, R., van der Linden, C., Buitelaar, J.K., Gericke, G.S., Hawkridge, S.M., Temlett, J.A. The Journal of clinical psychiatry. (2001) [Pubmed]
  15. Effect of clarithromycin on the pharmacokinetics and pharmacodynamics of pimozide in healthy poor and extensive metabolizers of cytochrome P450 2D6 (CYP2D6). Desta, Z., Kerbusch, T., Flockhart, D.A. Clin. Pharmacol. Ther. (1999) [Pubmed]
  16. Factors influencing the response of the cerebral circulation to phenylethylamine. McCulloch, J., Harper, A.M. Neurology (1979) [Pubmed]
  17. Neurotransmitters involved in mediating the steroid-dependent suppression of pulsatile luteinizing hormone secretion in anestrous ewes: effects of receptor antagonists. Meyer, S.L., Goodman, R.L. Endocrinology (1985) [Pubmed]
  18. Three thousand days of pregnancy. A case of monosymptomatic delusional pseudocyesis responding to pimozide. de Pauw, K.W. The British journal of psychiatry : the journal of mental science. (1990) [Pubmed]
  19. Forebrain origins and terminations of the medial forebrain bundle metabolically activated by rewarding stimulation or by reward-blocking doses of pimozide. Gallistel, C.R., Gomita, Y., Yadin, E., Campbell, K.A. J. Neurosci. (1985) [Pubmed]
  20. Effects of calmodulin antagonists on immune mouse lymphocytes. Wolberg, G., Zimmerman, T.P. Mol. Pharmacol. (1984) [Pubmed]
  21. Antipsychotic pimozide is a potent Ca2+ channel blocker in heart. Enyeart, J.J., Dirksen, R.T., Sharma, V.K., Williford, D.J., Sheu, S.S. Mol. Pharmacol. (1990) [Pubmed]
  22. Endocrine effects of pimozide, a specific dopaminergic blocker. Collu, R., Jéquier, J.C., Leboeuf, G., Letarte, J., Ducharme, J.R. J. Clin. Endocrinol. Metab. (1975) [Pubmed]
  23. Characterization of Ca2+-stimulated secretion in permeable GH3 pituitary cells. Ronning, S.A., Martin, T.F. J. Biol. Chem. (1986) [Pubmed]
  24. Status dystonicus: the syndrome and its management. Manji, H., Howard, R.S., Miller, D.H., Hirsch, N.P., Carr, L., Bhatia, K., Quinn, N., Marsden, C.D., Bahtia, K. Brain (1998) [Pubmed]
  25. A dopaminergic mechanism in mania. Gerner, R.H., Post, R.M., Bunney, W.E. The American journal of psychiatry. (1976) [Pubmed]
  26. Prolactin monitoring of haloperidol and pimozide treatment in children with Tourette's syndrome. Sallee, F.R., Dougherty, D., Sethuraman, G., Vrindavanam, N. Biol. Psychiatry (1996) [Pubmed]
  27. Effect of gamma-aminobutyric acid on growth hormone and prolactin secretion in man: influence of pimozide and domperidone. Cavagnini, F., Benetti, G., Invitti, C., Ramella, G., Pinto, M., Lazza, M., Dubini, A., Marelli, A., Müller, E.E. J. Clin. Endocrinol. Metab. (1980) [Pubmed]
  28. Identification and characterization of human cytochrome P450 isoforms interacting with pimozide. Desta, Z., Kerbusch, T., Soukhova, N., Richard, E., Ko, J.W., Flockhart, D.A. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  29. Stimulation of somatostatin release in vitro by synthetic human growth hormone-releasing factor by a nondopaminergic mechanism. Aguila, M.C., McCann, S.M. Endocrinology (1985) [Pubmed]
  30. Corticotropin-releasing factor as well as opioid and dopamine are involved in tail-pinch-induced food intake of rats. Samarghandian, S., Ohata, H., Yamauchi, N., Shibasaki, T. Neuroscience (2003) [Pubmed]
  31. Relative efficacy of haloperidol and pimozide in children and adolescents with Tourette's disorder. Sallee, F.R., Nesbitt, L., Jackson, C., Sine, L., Sethuraman, G. The American journal of psychiatry. (1997) [Pubmed]
  32. ECG changes during haloperidol and pimozide treatment of Tourette's disorder. Fulop, G., Phillips, R.A., Shapiro, A.K., Gomes, J.A., Shapiro, E., Nordlie, J.W. The American journal of psychiatry. (1987) [Pubmed]
  33. Dopaminergic receptor sites in human brain: positron emission tomography. Baron, J.C., Comar, D., Zarifian, E., Agid, Y., Crouzel, C., Loo, H., Deniker, P., Kellershohn, C. Neurology (1985) [Pubmed]
  34. Effect of the dopamine receptor blocking agent pimozide on the growth hormone response to arginine and exercise and on the spontaneous growth hormone fluctuations. Schwinn, G., Schwarck, H., McIntosh, C., Milstrey, H.R., Willms, B., Köbberling, J. J. Clin. Endocrinol. Metab. (1976) [Pubmed]
  35. Prolactin suppression by (-) delta-9-tetrahydrocannabinol (THC): involvement of serotonergic and dopaminergic pathways. Kramer, J., Ben-David, M. Endocrinology (1978) [Pubmed]
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