Brain Physiology and Metabolism Section, National Institute on Aging, National Institutes of Health, Bethesda, MD 20892, USA.
Mol Psychiatry. 2010 Jun;15(6):602-14. doi: 10.1038/mp.2008.117. Epub 2008 Nov 4.
Agents effective against mania in bipolar disorder are reported to decrease turnover of arachidonic acid (AA) in phospholipids and expression of calcium-dependent AA-selective cytosolic phospholipase A(2) (cPLA(2)) in rat brain. In contrast, fluoxetine, an antidepressant that is reported to switch bipolar depressed patients to mania, increases cPLA(2) expression and AA turnover in rat brain. We therefore hypothesized that antidepressants that increase switching to mania generally increase cPLA(2) and AA turnover in brain. To test this hypothesis, adult male CDF-344 rats were administered imipramine and bupropion, with reported high and low switching rates, respectively, at daily doses of 10 and 30 mg kg(-1) i.p., respectively, or i.p. saline (control) for 21 days. Frontal cortex expression of different PLA(2) enzymes and AA turnover rates in brain when the rats were unanesthetized were measured. Compared with chronic saline, chronic imipramine but not bupropion significantly increased cortex cPLA(2) mRNA activity, protein and phosphorylation, expression of the cPLA(2) transcription factor, activator protein-2alpha (AP-2alpha) and AA turnover in phospholipids. Protein levels of secretory phospholipase A(2), calcium-independent phospholipase A(2), cyclooxygenase (COX)-1 and COX-2 were unchanged, and prostaglandin E(2) was unaffected. These results, taken with prior data on chronic fluoxetine in rats, suggest that antidepressants that increase the switching tendency of bipolar depressed patients to mania do so by increasing AA recycling and metabolism in brain. Mania in bipolar disorder thus may involve upregulated brain AA metabolism.
有报道称,在双相情感障碍中治疗躁狂的药物可降低花生四烯酸(AA)在磷脂中的周转率和钙依赖性 AA 选择性胞质型 PLA2(cPLA2)在大鼠脑中的表达。相比之下,百忧解是一种抗抑郁药,有报道称它会使双相抑郁患者转为躁狂,增加大鼠脑中 cPLA2 的表达和 AA 的周转率。因此,我们假设会增加躁狂发作转换的抗抑郁药通常会增加大脑中的 cPLA2 和 AA 的周转率。为了验证这一假设,成年雄性 CDF-344 大鼠分别给予丙咪嗪和安非他酮,其报告的转换率分别为高和低,剂量分别为每天 10 和 30mg/kg 腹腔注射,或腹腔注射生理盐水(对照)21 天。当大鼠未麻醉时,测量前额皮质中不同 PLA2 酶的表达和大脑中的 AA 周转率。与慢性生理盐水相比,慢性丙咪嗪但不是安非他酮显著增加了皮质 cPLA2 mRNA 活性、蛋白和磷酸化、cPLA2 转录因子激活蛋白-2α(AP-2α)的表达和磷脂中的 AA 周转率。分泌型 PLA2、钙非依赖性 PLA2、环氧化酶(COX)-1 和 COX-2 的蛋白水平不变,前列腺素 E2 不受影响。这些结果与先前大鼠慢性氟西汀的数据相结合,表明增加双相情感障碍中躁狂发作转换倾向的抗抑郁药通过增加大脑中 AA 的再循环和代谢来实现。因此,双相情感障碍中的躁狂可能涉及大脑 AA 代谢的上调。