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Chemical Compound Review

Lullan     (3aS,7aR)-2-[4-[4-(7-thia-8...

Synonyms: Perospirone, SureCN120579, CHEMBL1472975, AC1L3H05, M813, ...
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Disease relevance of Lullan


Psychiatry related information on Lullan


High impact information on Lullan

  • The present study suggests that CYP3A4 is significantly involved in metabolism of perospirone in humans [7].
  • Perospirone is an atypical antipsychotic agent originated and clinically used in Japan. Based on an in vitro study, it is reported that perospirone is mainly metabolized to ID-15036 by cytochrome P450 (CYP) 3A4 [7].
  • Effects of itraconazole and tandospirone on the pharmacokinetics of perospirone [7].
  • Plasma concentrations of perospirone, hydroxyperospirone, and prolactin were monitored just before and up to 12 hours after the dosing [8].
  • Perospirone is a novel atypical antipsychotic with a unique combination of 5-HT1A receptor agonism as well as 5-HT2A and D2 receptor antagonism [9].

Chemical compound and disease context of Lullan

  • We report on a patient with HD, whose involuntary movements and psychiatric symptoms were clinically improved with perospirone, a second-generation antipsychotic agent with antagonistic effects on serotonin 5-HT(2A) and dopamine D(2) (D(2)) receptors, as well as a unique agonistic effect on serotonin 5-HT(1A) (5-HT(1A)) receptors [3].
  • We examined the anxiolytic potential of perospirone, a novel serotonin-2 and dopamine-2 antagonist (SDA)-type antipsychotic agent, and compared its effects with those of the standard anxiolytic diazepam and the conventional antipsychotic haloperidol by using conditioned defensive burying (CDB) and social interaction (SI) tests in rats [10].

Biological context of Lullan


Anatomical context of Lullan


Associations of Lullan with other chemical compounds


Gene context of Lullan

  • Quinidine (a specific inhibitor of CYP2D6) did not markedly affect the metabolism of perospirone, whereas quercetin (an inhibitor of CYP2C8) and ketoconazole (an inhibitor of CYP3A4) caused a decrease in the metabolism with human liver microsomes in a concentration dependent fashion [20].
  • The distinct cognitive enhancement profile of perospirone may be attributable to its partial 5-HT1A agonist action [21].
  • The change in P300 amplitude following a switch to perospirone correlated significantly with the improvement of general psychopathology symptoms, as well as with the change in scores on items of delusions, hallucinatory behavior, emotional withdrawal, depression, poor attention, and disturbance of volition [22].
  • We studied the effects of perospirone (SM-9018), a novel serotonin-2 (5-HT2) and dopamine-2 (D2) receptor antagonist (SDA), on conditioned fear stress (CFS)-induced freezing behavior in rats and compared its actions with those of other antipsychotics [23].
  • Switching to equivalent dose of perospirone from prior antipsychotic medication was associated with a significant improvement in indices of verbal memory organization of the Auditory Verbal Learning Test. Negative symptoms and extrapyramidal side effects were also ameliorated after switching to perospirone [21].

Analytical, diagnostic and therapeutic context of Lullan


  1. Neuroleptic malignant syndrome related to a switch to perospirone and anticholinergic withdrawal. Tanii, H., Fujita, K., Okazaki, Y. The American journal of psychiatry. (2006) [Pubmed]
  2. Use of perospirone for obesity and diabetes mellitus in patients with schizophrenia: three case reports. Nishida, M., Nakamura, M. International clinical psychopharmacology. (2004) [Pubmed]
  3. Perospirone in treatment of Huntington's disease: A first case report. Roppongi, T., Togo, T., Nakamura, S., Asami, T., Yoshimi, A., Shiozaki, K., Kato, D., Kawanishi, C., Hirayasu, Y. Prog. Neuropsychopharmacol. Biol. Psychiatry (2007) [Pubmed]
  4. Effective treatment of coprophagia in a patient with schizophrenia with the novel atypical antipsychotic drug perospirone. Harada, K.I., Yamamoto, K., Saito, T. Pharmacopsychiatry (2006) [Pubmed]
  5. Efficacy of perospirone in the management of aggressive behavior associated with dementia. Sato, S., Mizukami, K., Moro, K., Tanaka, Y., Asada, T. Prog. Neuropsychopharmacol. Biol. Psychiatry (2006) [Pubmed]
  6. Efficacy of carbamazepine against neuroleptic-induced akathisia in treatment with perospirone: case series. Masui, T., Kusumi, I., Takahashi, Y., Koyama, T. Prog. Neuropsychopharmacol. Biol. Psychiatry (2005) [Pubmed]
  7. Effects of itraconazole and tandospirone on the pharmacokinetics of perospirone. Masui, T., Kusumi, I., Takahashi, Y., Koyama, T. Therapeutic drug monitoring. (2006) [Pubmed]
  8. Steady-state pharmacokinetics of a new antipsychotic agent perospirone and its active metabolite, and its relationship with prolactin response. Yasui-Furukori, N., Furukori, H., Nakagami, T., Saito, M., Inoue, Y., Kaneko, S., Tateishi, T. Therapeutic drug monitoring. (2004) [Pubmed]
  9. Perospirone, a novel atypical antipsychotic drug, potentiates fluoxetine-induced increases in dopamine levels via multireceptor actions in the rat medial prefrontal cortex. Yoshino, T., Nisijima, K., Shioda, K., Yui, K., Katoh, S. Neurosci. Lett. (2004) [Pubmed]
  10. Anxiolytic-like effects of perospirone, a novel serotonin-2 and dopamine-2 antagonist (SDA)-type antipsychotic agent. Sakamoto, H., Matsumoto, K., Ohno, Y., Nakamura, M. Pharmacol. Biochem. Behav. (1998) [Pubmed]
  11. Localization and pharmacological characterization of [3H]perospirone-binding sites in rat brain. Tanaka, H., Ohno, Y., Nakamura, M. Gen. Pharmacol. (1998) [Pubmed]
  12. Perospirone, a novel antipsychotic agent, hyperpolarizes rat dorsal raphe neurons via 5-HT1A receptor. Shiwa, T., Amano, T., Matsubayashi, H., Seki, T., Sasa, M., Sakai, N. J. Pharmacol. Sci. (2003) [Pubmed]
  13. Effects of perospirone, a novel antipsychotic agent, on the dopaminergic neurons in the rat ventral tegmental area. Yu, H., Ishihara, K., Matsubayashi, H., Amano, T., Sasa, M. Jpn. J. Pharmacol. (1997) [Pubmed]
  14. Effects of perospirone, a novel 5-HT2 and D2 receptor antagonist, on Fos protein expression in the rat forebrain. Ishibashi, T., Tagashira, R., Nakamura, M., Noguchi, H., Ohno, Y. Pharmacol. Biochem. Behav. (1999) [Pubmed]
  15. In vitro drug-drug interactions with perospirone and concomitantly administered drugs in human liver microsomes. Shimakura, J., Tani, N., Mizuno, Y., Komuro, S., Kanamaru, H. European journal of drug metabolism and pharmacokinetics. (2003) [Pubmed]
  16. In vitro metabolism of perospirone in rat, monkey and human liver microsomes. Mizuno, Y., Tani, N., Komuro, S., Kanamaru, H., Nakatsuka, I. European journal of drug metabolism and pharmacokinetics. (2003) [Pubmed]
  17. Effects of perospirone (SM-9018), a potential atypical neuroleptic, on dopamine D1 receptor-mediated vacuous chewing movement in rats: a role of 5-HT2 receptor blocking activity. Ohno, Y., Ishida-Tokuda, K., Ishibashi, T., Nakamura, M. Pharmacol. Biochem. Behav. (1997) [Pubmed]
  18. Differential effects of subchronic treatments with atypical antipsychotic drugs on dopamine D2 and serotonin 5-HT2A receptors in the rat brain. Kusumi, I., Takahashi, Y., Suzuki, K., Kameda, K., Koyama, T. Journal of neural transmission (Vienna, Austria : 1996) (2000) [Pubmed]
  19. Effect of carbamazepine on the single oral dose pharmacokinetics of perospirone and its active metabolite. Masui, T., Kusumi, I., Takahashi, Y., Koyama, T. Prog. Neuropsychopharmacol. Biol. Psychiatry (2006) [Pubmed]
  20. Characterization of human cytochrome P450 enzymes involved in the in vitro metabolism of perospirone. Kitamura, A., Mizuno, Y., Natsui, K., Yabuki, M., Komuro, S., Kanamaru, H. Biopharmaceutics & drug disposition. (2005) [Pubmed]
  21. Perospirone in the treatment of schizophrenia: effect on verbal memory organization. Araki, T., Yamasue, H., Sumiyoshi, T., Kuwabara, H., Suga, M., Iwanami, A., Kato, N., Kasai, K. Prog. Neuropsychopharmacol. Biol. Psychiatry (2006) [Pubmed]
  22. The effect of perospirone on auditory P300 in schizophrenia: a preliminary study. Araki, T., Kasai, K., Rogers, M.A., Kato, N., Iwanami, A. Prog. Neuropsychopharmacol. Biol. Psychiatry (2006) [Pubmed]
  23. Evaluation of perospirone (SM-9018), a novel serotonin-2 and dopamine-2 receptor antagonist, and other antipsychotics in the conditioned fear stress-induced freezing behavior model in rats. Ishida-Tokuda, K., Ohno, Y., Sakamoto, H., Ishibashi, T., Wakabayashi, J., Tojima, R., Morita, T., Nakamura, M. Jpn. J. Pharmacol. (1996) [Pubmed]
  24. Determination of a new atypical antipsychotic agent perospirone and its metabolite in human plasma by automated column-switching high-performance liquid chromatography. Yasui-Furukori, N., Inoue, Y., Tateishi, T. J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. (2003) [Pubmed]
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