Jóźwiak-Bębenista Marta, Kowalczyk Edward
Department of Pharmacology and Toxicology, The Interfaculty Chair of Basic and Clinical Pharmacology and Toxicology, Medical University of Lodz, Zeligowskiego 7/9, 90-752, Lodz, Poland.
Neurochem Res. 2017 Apr;42(4):943-952. doi: 10.1007/s11064-016-2127-2. Epub 2016 Nov 30.
Several lines of evidence suggest that pituitary adenylate cyclase-activating polypeptide (PACAP) is a neuropeptide playing an important role as a neuromodulator. It has been indicated that PACAP is associated with mental diseases, and that regulation of the PACAPergic signals could be a potential target for the treatment of such psychiatric states as schizophrenia. Recent studies have suggested that action of neuroleptic drugs is mediated not only by dopaminergic and serotonergic neurotransmission, but also via neuropeptides which may act both as neurotransmitters and as neuromodulators. The present study examines whether currently-used neuroleptics influence the action of PACAP receptors, whose expression is altered in a schizophrenic patient. Real-time polymerase chain reaction (PCR) was used to examine the effects of haloperidol, olanzapine and amisulpride on the expression of genes coding PAC1/VPAC type receptors in the T98G glioblastoma cell line, as an example of an in vitro model of glial cells. PAC1 mRNA expression fell after 24-h incubation with haloperidol or olanzapine; however the effect was not maintained after 72 h, and haloperidol even up-regulated PAC1 mRNA expression in a dose-dependent manner. All the examined drugs decreased VPAC2 mRNA expression, especially after 72-h incubation. Haloperidol (typical neuroleptic) was distinctly more potent than atypical neuroleptic drugs (olanzapine and amisulpride). In addition, PACAP increased PAC1 and VPAC2 mRNA expression. In conclusion, our findings suggest PACAP receptors may be involved in the mechanism of typical and atypical neuroleptic drugs.
多条证据表明,垂体腺苷酸环化酶激活多肽(PACAP)作为一种神经调质发挥着重要作用的神经肽。已有研究表明,PACAP与精神疾病有关,并且调节PACAP能信号可能是治疗精神分裂症等精神状态的潜在靶点。最近的研究表明,抗精神病药物的作用不仅通过多巴胺能和5-羟色胺能神经传递介导,还通过可能同时作为神经递质和神经调质的神经肽介导。本研究考察了目前使用的抗精神病药物是否会影响PACAP受体的作用,该受体在精神分裂症患者中表达发生改变。以T98G胶质母细胞瘤细胞系作为胶质细胞的体外模型,采用实时聚合酶链反应(PCR)检测氟哌啶醇、奥氮平和氨磺必利对编码PAC1/VPAC型受体的基因表达的影响。与氟哌啶醇或奥氮平孵育24小时后,PAC1 mRNA表达下降;然而,72小时后这种作用未持续,氟哌啶醇甚至以剂量依赖的方式上调PAC1 mRNA表达。所有检测药物均降低VPAC2 mRNA表达,尤其是孵育72小时后。氟哌啶醇(典型抗精神病药物)比非典型抗精神病药物(奥氮平和氨磺必利)的作用明显更强。此外,PACAP增加PAC1和VPAC2 mRNA表达。总之,我们的研究结果表明,PACAP受体可能参与典型和非典型抗精神病药物的作用机制。