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Chemical Compound Review

SerLect     1-[2-[4-[5-chloro-1-(4- fluorophenyl)indol...

Synonyms: Serdolect, Sertindol, SERTINDOLE, Sertindolum, SerLect (TN), ...
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Disease relevance of SerLect


Psychiatry related information on SerLect


High impact information on SerLect


Chemical compound and disease context of SerLect

  • With the introduction of risperidone and the imminent prospect of other atypical antipsychotic drugs (olanzapine, sertindole, quetiapine, ziprasidone), clinicians may be able to improve dramatically the methods and manner in which they treat schizophrenia and related psychotic disorders [14].
  • METHOD: Data were analyzed to determine differences in weight gain during treatment among patients receiving 5 different drug treatments (clozapine [N = 20], olanzapine [N = 13], risperidone [N = 38], haloperidol [N = 43], and sertindole [N = 8]) [11].
  • Ketanserin (0.75 and 1.5 mg/kg) dose-dependently reversed olanzapine (30 mg/kg) and sertindole (45 mg/kg)-induced catalepsy without any effect on clozapine (75 mg/kg)-induced catalepsy [15].

Biological context of SerLect


Anatomical context of SerLect

  • In canine ventricular myocytes, the IC50 value for IKr inhibition by sertindole was 107 +/- 21 nM [3].
  • OBJECTIVE: To characterise the interaction of sertindole with the 5-HT2C receptor using rat choroid plexus as a physiological receptor source [17].
  • We therefore examined the effects of sertindole on two cloned human cardiac potassium channels, the human ether-a-go-go-related gene (HERG) and Kv1.5, stably transfected into mammalian cell lines [16].
  • We have investigated the adrenergic antagonist effect of the antipsychotic sertindole in rat resistance vessels and in membranes of HEK293 cells transfected with alpha1-adrenoceptors [19].
  • Electrophysiological profile of the new atypical neuroleptic, sertindole, on midbrain dopamine neurones in rats: acute and repeated treatment [20].

Associations of SerLect with other chemical compounds


Gene context of SerLect


Analytical, diagnostic and therapeutic context of SerLect

  • Two rapid-dose titrations of sertindole in patients with schizophrenia [29].
  • Sertindole (1-[2-[4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]-1-piperidinyl]ethyl]-2-imidazolidinone), an atypical antipsychotic drug, was separated by capillary electrophoresis from its two main metabolites norsertindole and dehydrosertindole [30].
  • Clinical trials have shown antipsychotic efficacy and very few extrapyramidal symptoms (EPS) with sertindole at 20 mg/day [31].
  • This patient had averaged 2.5 inpatient admissions per year for the 8 years preceding initiation of sertindole therapy, but has had no hospitalizations or psychosis in the 3.5 years since [32].
  • This 40-day randomized, placebo-controlled, dose-ranging multicenter study was designed to assess the effect of sertindole on previously neuroleptic-responsive, hospitalized schizophrenic patients (n = 205) [33].


  1. Antipsychotic drugs: prolonged QTc interval, torsade de pointes, and sudden death. Glassman, A.H., Bigger, J.T. The American journal of psychiatry. (2001) [Pubmed]
  2. The atypical antipsychotic sertindole: a case series. Lee, A.M., Knoll, J.L., Suppes, T. The Journal of clinical psychiatry. (1997) [Pubmed]
  3. Electrophysiological safety of sertindole in dogs with normal and remodeled hearts. Thomsen, M.B., Volders, P.G., Stengl, M., Spätjens, R.L., Beekman, J.D., Bischoff, U., Kall, M.A., Frederiksen, K., Matz, J., Vos, M.A. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  4. Treatment with the new antipsychotic sertindole for late-occurring undesirable movement effects. Perquin, L.N. International clinical psychopharmacology. (2005) [Pubmed]
  5. Traditional and new antipsychotic drugs differentially alter neurotransmission markers in basal ganglia-thalamocortical neural pathways. Sakai, K., Gao, X.M., Hashimoto, T., Tamminga, C.A. Synapse (2001) [Pubmed]
  6. Behavioral effects of sertindole, risperidone, clozapine and haloperidol in Cebus monkeys. Casey, D.E. Psychopharmacology (Berl.) (1996) [Pubmed]
  7. Classical as well as novel antipsychotic drugs increase self-stimulation threshold in the rat--similar mechanism of action? Flagstad, P., Arnt, J., Olsen, C.K. Eur. J. Pharmacol. (2006) [Pubmed]
  8. Clozapine withdrawal symptoms after change to sertindole in a schizophrenic patient. Berecz, R., Glaub, T., Kellermann, M., de la Rubia, A., Llerena, A., Degrell, I. Pharmacopsychiatry (2000) [Pubmed]
  9. Effects of sertindole on sleep-wake states, electroencephalogram, behavioral patterns, and epileptic activity of rats. Coenen, A.M., Ates, N., Skarsfeldt, T., van Luijtelaar, E.L. Pharmacol. Biochem. Behav. (1995) [Pubmed]
  10. Pharmacokinetics of sertindole in healthy young and elderly male and female subjects. Wong, S.L., Cao, G., Mack, R.J., Granneman, G.R. Clin. Pharmacol. Ther. (1997) [Pubmed]
  11. Novel antipsychotics: comparison of weight gain liabilities. Wirshing, D.A., Wirshing, W.C., Kysar, L., Berisford, M.A., Goldstein, D., Pashdag, J., Mintz, J., Marder, S.R. The Journal of clinical psychiatry. (1999) [Pubmed]
  12. The relationship of pharmacology to side effects. Casey, D.E. The Journal of clinical psychiatry. (1997) [Pubmed]
  13. Serotonin: 5-HT2A receptor occupancy in vivo and response to the new antipsychotics olanzapine and sertindole. Travis, M.J., Busatto, G.F., Pilowsky, L.S., Kerwin, R.W., Mulligan, R., Gacinovic, S., Costa, D.C., Ell, P.J., Mertens, J., Terriere, D. The British journal of psychiatry : the journal of mental science. (1997) [Pubmed]
  14. Atypical antipsychotic drugs as a first-line treatment of schizophrenia: a rationale and hypothesis. Lieberman, J.A. The Journal of clinical psychiatry. (1996) [Pubmed]
  15. Quinpirole, 8-OH-DPAT and ketanserin modulate catalepsy induced by high doses of atypical antipsychotics. Ninan, I., Kulkarni, S.K. Methods and findings in experimental and clinical pharmacology. (1999) [Pubmed]
  16. The antipsychotic agent sertindole is a high affinity antagonist of the human cardiac potassium channel HERG. Rampe, D., Murawsky, M.K., Grau, J., Lewis, E.W. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  17. Sertindole is a serotonin 5-HT2c inverse agonist and decreases agonist but not antagonist binding to 5-HT2c receptors after chronic treatment. Hietala, J., Kuonnamäki, M., Pälvimäki, E.P., Laakso, A., Majasuo, H., Syvälahti, E. Psychopharmacology (Berl.) (2001) [Pubmed]
  18. In vivo occupation of dopamine D1, D2 and serotonin (5-HT)2A receptors by sertindole in the rat brain. Takahashi, Y., Kusumi, I., Ishikane, T., Matsubara, S., Koyama, T. Journal of psychiatry & neuroscience : JPN. (1998) [Pubmed]
  19. The antipsychotic drug sertindole is a specific inhibitor of alpha1A-adrenoceptors in rat mesenteric small arteries. Ipsen, M., Zhang, Y., Dragsted, N., Han, C., Mulvany, M.J. Eur. J. Pharmacol. (1997) [Pubmed]
  20. Electrophysiological profile of the new atypical neuroleptic, sertindole, on midbrain dopamine neurones in rats: acute and repeated treatment. Skarsfeldt, T. Synapse (1992) [Pubmed]
  21. Clinical efficacy of serotonin-dopamine antagonists relative to classic neuroleptics. Borison, R.L. Journal of clinical psychopharmacology. (1995) [Pubmed]
  22. Comparison of short-term administration of sertindole, clozapine and haloperidol on the inactivation of midbrain dopamine neurons in the rat. Skarsfeldt, T. Eur. J. Pharmacol. (1994) [Pubmed]
  23. The antipsychotic drugs sertindole and pimozide block erg3, a human brain K(+) channel. Kang, J., Chen, X.L., Rampe, D. Biochem. Biophys. Res. Commun. (2001) [Pubmed]
  24. The effect of erythromycin on the CYP3A component of sertindole clearance in healthy volunteers. Wong, S.L., Cao, G., Mack, R.J., Granneman, G.R. Journal of clinical pharmacology. (1997) [Pubmed]
  25. Effects of typical and atypical neuroleptics on Fos protein expression in the rat forebrain. Fink-Jensen, A., Kristensen, P. Neurosci. Lett. (1994) [Pubmed]
  26. Drug metabolism and atypical antipsychotics. Prior, T.I., Chue, P.S., Tibbo, P., Baker, G.B. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. (1999) [Pubmed]
  27. Lack of CYP3A inhibition effects of sertindole on terfenadine in healthy volunteers. Wong, S.L., Cao, G., Mack, R., Granneman, G.R. International journal of clinical pharmacology and therapeutics. (1998) [Pubmed]
  28. Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Schotte, A., Janssen, P.F., Gommeren, W., Luyten, W.H., Van Gompel, P., Lesage, A.S., De Loore, K., Leysen, J.E. Psychopharmacology (Berl.) (1996) [Pubmed]
  29. Two rapid-dose titrations of sertindole in patients with schizophrenia. Sramek, J.J., Mack, R.J., Awni, W., Hourani, J., Jhee, S.S., Barto, S., Cutler, N.R. Journal of clinical psychopharmacology. (1997) [Pubmed]
  30. Comparison of methanol and acetonitrile as solvents for the separation of sertindole and its major metabolites by capillary zone electrophoresis. Subirats, X., Reinstadler, S., Porras, S.P., Raggi, M.A., Kenndler, E. Electrophoresis (2005) [Pubmed]
  31. Low striatal and extra-striatal D2 receptor occupancy during treatment with the atypical antipsychotic sertindole. Nyberg, S., Olsson, H., Nilsson, U., Maehlum, E., Halldin, C., Farde, L. Psychopharmacology (Berl.) (2002) [Pubmed]
  32. A case of treatment-refractory psychosis responsive to sertindole. Geracioti, T.D., Parker, S., Lowther, N.B., Wortman, M., Richtand, N.M. Schizophr. Res. (1998) [Pubmed]
  33. A randomized, controlled, dose-ranging trial of sertindole in patients with schizophrenia. van Kammen, D.P., McEvoy, J.P., Targum, S.D., Kardatzke, D., Sebree, T.B. Psychopharmacology (Berl.) (1996) [Pubmed]
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