Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity.

作者: Erin W Tuplin , Matthew R Holahan

DOI: 10.2174/1570159X15666170413115754

关键词:

摘要: Background The treatment of schizophrenia is challenging due to the wide range symptoms (positive, negative, cognitive) associated with disease. Typical antipsychotics that antagonize D2 receptors are effective in treating positive symptoms, but extrapyramidal side-effects (EPS) a common occurrence. Atypical targeting 5-HT2A and more at cognitive negative compared typical antipsychotics, these drugs also result such as metabolic syndromes. Objective To identify evidence literature elucidates pharmacological profile aripiprazole.s. Methods We searched PubMed for peer reviewed articles on aripiprazole its clinical efficacy, side-effects, pharmacology, effects animal models symptoms. Results Aripiprazole newer atypical antipsychotic displays unique profile, including partial agonism functionally selective properties. has potential treat least well other antipsychotics. drug favorable side-effect low propensity EPS or Animal have been used determine efficacy symptom management. In instances, resulted reversal deficits extinction, pre-pulse inhibition, social withdrawal. Because requires greater than 90% occupancy rate be clinically active does not produce EPS, this suggests effect intracellular signaling pathways. Conclusion A combination factors dopamine system stabilization via agonism, functional selectivity receptors, serotonin-dopamine interaction may contribute ability successfully manage This review examines mechanisms action further clarify actions aripiprazole.

参考文章(167)
Tomáš Urbánek, Michal Hrdlička, Ivana Dudová, Iveta Zedková, Onset of action of atypical and typical antipsychotics in the treatment of adolescent schizophrenic psychoses. Neuro endocrinology letters. ,vol. 32, pp. 667- 670 ,(2011)
CA Jones, DJG Watson, KCF Fone, Animal models of schizophrenia British Journal of Pharmacology. ,vol. 164, pp. 1162- 1194 ,(2011) , 10.1111/J.1476-5381.2011.01386.X
Alessandro Usiello, Ja-Hyun Baik, Françoise Rougé-Pont, Roberto Picetti, Andrée Dierich, Marianne LeMeur, Pier Vincenzo Piazza, Emiliana Borrelli, Distinct functions of the two isoforms of dopamine D2 receptors Nature. ,vol. 408, pp. 199- 203 ,(2000) , 10.1038/35041572
The assessment of neuropsychological functioning in schizophrenia Dialogues in clinical neuroscience. ,vol. 12, pp. 383- 392 ,(2010) , 10.31887/DCNS.2010.12.3/AREICHENBERG
E Meller, M Goldstein, Y Namba, K Bohmaker, A J Friedhoff, Relationship between receptor occupancy and response at striatal dopamine autoreceptors. Molecular Pharmacology. ,vol. 31, pp. 592- 598 ,(1987)
David Mamo, Ariel Graff, Romina Mizrahi, C. M. Shammi, Françoise Romeyer, Shitij Kapur, Differential effects of aripiprazole on D(2), 5-HT(2), and 5-HT(1A) receptor occupancy in patients with schizophrenia: a triple tracer PET study. American Journal of Psychiatry. ,vol. 164, pp. 1411- 1417 ,(2007) , 10.1176/APPI.AJP.2007.06091479
G. di Chiara, A. Imperato, Dopamine Release and Metabolism in Awake Rats after Systemic Neuroleptics as Studied by Brain Dialysis Dopaminergic Systems and their Regulation. ,vol. 5, pp. 19- 34 ,(1986) , 10.1007/978-1-349-07431-0_2