Arey Rachel, McClung Colleen A
Department of Psychiatry, University of Texas Southwestern Medical Center, Dallas, USA.
Behav Pharmacol. 2012 Aug;23(4):392-6. doi: 10.1097/FBP.0b013e32835651fd.
Bipolar disorder is a terrible and debilitating disease with limited treatment options. Circadian rhythm disruptions are prominent in bipolar subjects, and studies have shown that rhythm stabilization through psychosocial interventions can improve their symptoms. Furthermore, mice with a mutation in one of the central circadian proteins, CLOCK, have severely disrupted rhythms along with a behavioral profile that closely resembles human mania. A compound has been developed (CK01, similar to PF-670462) that inhibits the activity of casein kinase 1 (CK1), a critical protein involved in the timing of the molecular clock. Previous studies have shown that PF-670462 and other similar compounds are capable of entraining and stabilizing rhythms in arrhythmic animals. Here we show that chronic administration of CK01 leads to a reversal of the anxiety-related behavior, and partial reversal of the depression-related phenotypes of the Clock mutant mouse. This drug had no significant effects on the behavior of wild-type mice at the doses tested. These results suggest that CK1ε/δ inhibitors could be viable drugs for the treatment of bipolar disorder.
双相情感障碍是一种严重且使人衰弱的疾病,治疗选择有限。昼夜节律紊乱在双相情感障碍患者中很突出,研究表明通过心理社会干预稳定节律可以改善他们的症状。此外,一种核心昼夜节律蛋白CLOCK发生突变的小鼠,其节律严重紊乱,行为特征与人类躁狂症极为相似。已经开发出一种化合物(CK01,类似于PF - 670462),它能抑制酪蛋白激酶1(CK1)的活性,CK1是参与分子时钟计时的关键蛋白。先前的研究表明,PF - 670462和其他类似化合物能够使心律失常动物的节律恢复正常并使其稳定。在此我们表明,长期给予CK01可导致Clock突变小鼠焦虑相关行为的逆转以及抑郁相关表型的部分逆转。在所测试的剂量下,这种药物对野生型小鼠的行为没有显著影响。这些结果表明,CK1ε/δ抑制剂可能是治疗双相情感障碍的可行药物。