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Pathway Description
Aripiprazole lauroxil Serotonin Antagonist Action Pathway
Homo sapiens
Drug Action Pathway
Aripiprazole lauroxil is a long-acting injectable atypical antipsychotic drug used in the treatment of schizophrenia in adult patients. It is a prodrug of aripiprazole, which acts as a partial agonist at the D2 and 5-HT1A receptors, and as an antagonist at the 5-HT2A receptors. Aripiprazole, which is a major pharmacological metabolite of aripiprazole lauroxil, serves to improve the positive and negative symptoms of schizophrenia by modulating dopaminergic signalling pathways. Aripiprazole lauroxil is reported to have minimal effects on sexual function or prolactin levels. The pharmacological activity of aripiprazole lauroxil is thought to be mainly mediated by its metabolite aripiprazole, and to a lesser extent, dehydro-aripiprazole.
References
Aripiprazole lauroxil Serotonin Antagonist Pathway References
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Pubmed: 29126136
Van Oekelen D, Luyten WH, Leysen JE: 5-HT2A and 5-HT2C receptors and their atypical regulation properties. Life Sci. 2003 Apr 18;72(22):2429-49. doi: 10.1016/s0024-3205(03)00141-3.
Pubmed: 12650852
Gettu N, Saadabadi A: Aripiprazole.
Pubmed: 31613519
Simon N, Azorin JM: [Aripiprazole as dopamine partial agonist model: Basic concepts and clinical impact]. Encephale. 2018 Dec;44(6):558-564. doi: 10.1016/j.encep.2018.10.003. Epub 2018 Nov 20.
Pubmed: 30466778
Han M, Huang XF, Deng C: Aripiprazole differentially affects mesolimbic and nigrostriatal dopaminergic transmission: implications for long-term drug efficacy and low extrapyramidal side-effects. Int J Neuropsychopharmacol. 2009 Aug;12(7):941-52. doi: 10.1017/S1461145709009948. Epub 2009 Feb 10.
Pubmed: 19203411
de Bartolomeis A, Tomasetti C, Iasevoli F: Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism. CNS Drugs. 2015 Sep;29(9):773-99. doi: 10.1007/s40263-015-0278-3.
Pubmed: 26346901
Kadoguchi M, Arakawa H, Honda R, Hotta K, Shirasaka Y, Deguchi Y, Tamai I: Characterization of Aripiprazole Uptake Transporter in the Blood-Brain Barrier Model hCMEC/D3 Cells by Targeted siRNA Screening. Pharm Res. 2022 Jul;39(7):1549-1559. doi: 10.1007/s11095-022-03223-z. Epub 2022 Mar 21.
Pubmed: 35314999
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