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Chemical Compound Review

Abilitat     7-[4-[4-(2,3- dichlorophenyl)piperazin-1...

Synonyms: Discmelt, Abilify, Arpizol, Aripirazole, aripiprazol, ...
 
 
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Disease relevance of Aripiprazole

 

Psychiatry related information on Aripiprazole

 

High impact information on Aripiprazole

  • Hyperglycemia in a 7-year-old child treated with aripiprazole [11].
  • Hypertension and aripiprazole [12].
  • METHOD: This 3-week, multicenter, double-blind study randomly assigned 262 bipolar disorder patients in an acute manic or mixed episode to aripiprazole, 30 mg/day (reduced to 15 mg/day if needed for tolerability), or placebo [3].
  • Like methylspiperone, aripiprazole, and OPC4392, the two D4-selective 1,4-DAPs that are insensitive to the D4-F2.61V mutation are sensitive to aromatics at position 2.60 (D4-L2.60W, 7-20-fold increase), and they all have longer spacer arms that permit their tethered aromatics to adopt alternative orientations in the binding-site crevice [13].
  • 0. Whereas aripiprazole partially activated both the MAPK and AA pathways, its potency vs MAPK phosphorylation was much lower relative to potencies in assays either of AA release or inhibition of cyclic adenosine 3',5'-cyclic monophosphate accumulation [14].
 

Chemical compound and disease context of Aripiprazole

 

Biological context of Aripiprazole

 

Anatomical context of Aripiprazole

 

Associations of Aripiprazole with other chemical compounds

 

Gene context of Aripiprazole

  • In Chinese hamster ovary (CHO) cells stably expressing 5-HT2 receptors, aripiprazole displayed a dual agonist/antagonist profile for 5-HT2C receptor (VNI isoform) mediated calcium signaling (EC50 1070 nM, IC50 281 nM) [30].
  • The influence of CYP3A4 inhibition on the pharmacokinetics of ARIPIPRAZOLE was not considered to be clinically significant [31].
  • The modest 5-HT2A antagonism and 5-HT2C partial agonism, along with reported D2 and 5-HT1A partial agonism, may allow aripiprazole to stabilize the disturbed dopamine-serotonin interplay in schizophrenia with a moderate yet adequate pharmacological intervention [30].
  • In human embryonic kidney (HEK) cells transiently expressing 5-HT2C receptor isoforms, aripiprazole exhibited full agonism at the unedited INI, but partial agonism at the partially edited VNI and fully edited VSV isoforms (EC50s of 571, 1086 and 2099 nM, respectively) [30].
  • Aripiprazole potently (ED50 0.66 mg/kg p.o.) but partially (32 ng/ml) induced prolactin release [32].
 

Analytical, diagnostic and therapeutic context of Aripiprazole

References

  1. Possible neuroleptic malignant syndrome with aripiprazole and fluoxetine. Duggal, H.S., Kithas, J. The American journal of psychiatry. (2005) [Pubmed]
  2. Reversal of symptomatic hyperprolactinemia by aripiprazole. Wahl, R., Ostroff, R. The American journal of psychiatry. (2005) [Pubmed]
  3. A placebo-controlled, double-blind study of the efficacy and safety of aripiprazole in patients with acute bipolar mania. Keck, P.E., Marcus, R., Tourkodimitris, S., Ali, M., Liebeskind, A., Saha, A., Ingenito, G. The American journal of psychiatry. (2003) [Pubmed]
  4. Aripiprazole and Parkinson's disease psychosis. Schönfeldt-Lecuona, C., Connemann, B.J. The American journal of psychiatry. (2004) [Pubmed]
  5. Aripiprazole-induced movement disorder. Zacher, J.L., Hatchett, A.D. The American journal of psychiatry. (2006) [Pubmed]
  6. A case series: evaluation of the metabolic safety of aripiprazole. De Hert, M., Hanssens, L., van Winkel, R., Wampers, M., Van Eyck, D., Scheen, A., Peuskens, J. Schizophr. Bull (2007) [Pubmed]
  7. Aripiprazole, an antipsychotic with a novel mechanism of action, and risperidone vs placebo in patients with schizophrenia and schizoaffective disorder. Potkin, S.G., Saha, A.R., Kujawa, M.J., Carson, W.H., Ali, M., Stock, E., Stringfellow, J., Ingenito, G., Marder, S.R. Arch. Gen. Psychiatry (2003) [Pubmed]
  8. Aripiprazole in the treatment of patients with borderline personality disorder: a double-blind, placebo-controlled study. Nickel, M.K., Muehlbacher, M., Nickel, C., Kettler, C., Gil, F.P., Bachler, E., Buschmann, W., Rother, N., Fartacek, R., Egger, C., Anvar, J., Rother, W.K., Loew, T.H., Kaplan, P. The American journal of psychiatry. (2006) [Pubmed]
  9. A comparison of aripiprazole, methylphenidate, and placebo for amphetamine dependence. Tiihonen, J., Kuoppasalmi, K., F??hr, J., Tuomola, P., Kuikanm??ki, O., Vorma, H., Sokero, P., Haukka, J., Meririnne, E. The American journal of psychiatry (2007) [Pubmed]
  10. Treatment of tics in tourette syndrome with aripiprazole. Kastrup, A., Schlotter, W., Plewnia, C., Bartels, M. Journal of clinical psychopharmacology. (2005) [Pubmed]
  11. Hyperglycemia in a 7-year-old child treated with aripiprazole. Logue, D.D., Gonzalez, N., Heligman, S.D., McLaughlin, J.V., Belcher, H.M. The American journal of psychiatry (2007) [Pubmed]
  12. Hypertension and aripiprazole. Borras, L., Constant, E.L., Eytan, A., Huguelet, P. The American journal of psychiatry. (2005) [Pubmed]
  13. Certain 1,4-disubstituted aromatic piperidines and piperazines with extreme selectivity for the dopamine D4 receptor interact with a common receptor microdomain. Kortagere, S., Gmeiner, P., Weinstein, H., Schetz, J.A. Mol. Pharmacol. (2004) [Pubmed]
  14. Aripiprazole has Functionally Selective Actions at Dopamine D(2) Receptor-Mediated Signaling Pathways. Urban, J.D., Vargas, G.A., von Zastrow, M., Mailman, R.B. Neuropsychopharmacology (2007) [Pubmed]
  15. Use of atypical antipsychotics in refractory depression and anxiety. Nemeroff, C.B. The Journal of clinical psychiatry. (2005) [Pubmed]
  16. Efficacy of aripiprazole against hostility in schizophrenia and schizoaffective disorder: data from 5 double-blind studies. Volavka, J., Czobor, P., Citrome, L., McQuade, R.D., Carson, W.H., Kostic, D., Hardy, S., Marcus, R. The Journal of clinical psychiatry. (2005) [Pubmed]
  17. Neuroleptic malignant syndrome with aripiprazole and lithium: a case report. Ali, S., Pearlman, R.L., Upadhyay, A., Patel, P. Journal of clinical psychopharmacology. (2006) [Pubmed]
  18. Antipsychotic-like vs cataleptogenic actions in mice of novel antipsychotics having D2 antagonist and 5-HT1A agonist properties. Bardin, L., Kleven, M.S., Barret-Grévoz, C., Depoortère, R., Newman-Tancredi, A. Neuropsychopharmacology (2006) [Pubmed]
  19. Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Swainston Harrison, T., Perry, C.M. Drugs (2004) [Pubmed]
  20. Interaction of the novel antipsychotic aripiprazole with 5-HT(1A) and 5-HT (2A) receptors: functional receptor-binding and in vivo electrophysiological studies. Stark, A.D., Jordan, S., Allers, K.A., Bertekap, R.L., Chen, R., Mistry Kannan, T., Molski, T.F., Yocca, F.D., Sharp, T., Kikuchi, T., Burris, K.D. Psychopharmacology (Berl.) (2007) [Pubmed]
  21. Effects of novel antipsychotics, amisulpiride and aripiprazole, on maternal behavior in rats. Li, M., Budin, R., Fleming, A.S., Kapur, S. Psychopharmacology (Berl.) (2005) [Pubmed]
  22. Does antipsychotic polypharmacy increase the risk for metabolic syndrome? Correll, C.U., Frederickson, A.M., Kane, J.M., Manu, P. Schizophr. Res. (2007) [Pubmed]
  23. Dissociation between in vivo occupancy and functional antagonism of dopamine D2 receptors: comparing aripiprazole to other antipsychotics in animal models. Natesan, S., Reckless, G.E., Nobrega, J.N., Fletcher, P.J., Kapur, S. Neuropsychopharmacology (2006) [Pubmed]
  24. Aripiprazole for the treatment of psychosis in patients with Alzheimer's disease: a randomized, placebo-controlled study. De Deyn, P., Jeste, D.V., Swanink, R., Kostic, D., Breder, C., Carson, W.H., Iwamoto, T. Journal of clinical psychopharmacology. (2005) [Pubmed]
  25. Inhibition by aripiprazole of dopaminergic inputs to striatal neurons from substantia nigra. Matsubayashi, H., Amano, T., Sasa, M. Psychopharmacology (Berl.) (1999) [Pubmed]
  26. 7-(4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2(1H)-quinolinone (OPC-14597), a new putative antipsychotic drug with both presynaptic dopamine autoreceptor agonistic activity and postsynaptic D2 receptor antagonistic activity. Kikuchi, T., Tottori, K., Uwahodo, Y., Hirose, T., Miwa, T., Oshiro, Y., Morita, S. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  27. Olanzapine: a review of its use in the management of bipolar I disorder. McCormack, P.L., Wiseman, L.R. Drugs (2004) [Pubmed]
  28. Adjunctive treatment with a dopamine partial agonist, aripiprazole, for antipsychotic-induced hyperprolactinemia: a placebo-controlled trial. Shim, J.C., Shin, J.G., Kelly, D.L., Jung, D.U., Seo, Y.S., Liu, K.H., Shon, J.H., Conley, R.R. Am. J. Psychiatry (2007) [Pubmed]
  29. Aripiprazole blocks reinstatement of cocaine seeking in an animal model of relapse. Feltenstein, M.W., Altar, C.A., See, R.E. Biol. Psychiatry (2007) [Pubmed]
  30. Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoforms. Zhang, J.Y., Kowal, D.M., Nawoschik, S.P., Lou, Z., Dunlop, J. Biochem. Pharmacol. (2006) [Pubmed]
  31. Influence of itraconazole co-administration and CYP2D6 genotype on the pharmacokinetics of the new antipsychotic ARIPIPRAZOLE. Kubo, M., Koue, T., Inaba, A., Takeda, H., Maune, H., Fukuda, T., Azuma, J. Drug Metab. Pharmacokinet. (2005) [Pubmed]
  32. Partial agonist properties of the antipsychotics SSR181507, aripiprazole and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release. Cosi, C., Carilla-Durand, E., Assié, M.B., Ormiere, A.M., Maraval, M., Leduc, N., Newman-Tancredi, A. Eur. J. Pharmacol. (2006) [Pubmed]
  33. The use of aripiprazole in obsessive-compulsive disorder: preliminary observations in 8 patients. Connor, K.M., Payne, V.M., Gadde, K.M., Zhang, W., Davidson, J.R. The Journal of clinical psychiatry. (2005) [Pubmed]
  34. Therapeutic monitoring of aripiprazole by HPLC with column-switching and spectrophotometric detection. Kirschbaum, K.M., Müller, M.J., Zernig, G., Saria, A., Mobascher, A., Malevani, J., Hiemke, C. Clin. Chem. (2005) [Pubmed]
 
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