Laboratoire Venins et Molécules Thérapeutiques, Institut Pasteur de Tunis, Tunis El Manar University, 13 Place Pasteur BP74, 1002 Tunis, Tunisia.
Faculty of Sciences of Bizerte, Carthage University, 7021 Bizerte, Tunisia.
Int J Mol Sci. 2020 Sep 29;21(19):7175. doi: 10.3390/ijms21197175.
Kv3.1 channel is abundantly expressed in neurons and its dysfunction causes sleep loss, neurodegenerative diseases and depression. Fluoxetine, a serotonin selective reuptake inhibitor commonly used to treat depression, acts also on Kv3.1. To define the relationship between Kv3.1 and serotonin receptors (SR) pharmacological modulation, we showed that 1C11, a serotonergic cell line, expresses different voltage gated potassium (VGK) channels subtypes in the presence (differentiated cells (1C11D)) or absence (not differentiated cells (1C11ND)) of induction. Only Kv1.2 and Kv3.1 transcripts increase even if the level of Kv3.1b transcripts is highest in 1C11D and, after fluoxetine, in 1C11ND but decreases in 1C11D. The Kv3.1 channel protein is expressed in 1C11ND and 1C11D but is enhanced by fluoxetine only in 1C11D. Whole cell measurements confirm that 1C11 cells express (VGK) currents, increasing sequentially as a function of cell development. Moreover, SR 5HT1b is highly expressed in 1C11D but fluoxetine increases the level of transcript in 1C11ND and significantly decreases it in 1C11D. Serotonin dosage shows that fluoxetine at 10 nM blocks serotonin reuptake in 1C11ND but slows down its release when cells are differentiated through a decrease of 5HT1b receptors density. We provide the first experimental evidence that 1C11 expresses Kv3.1b, which confirms its major role during differentiation. Cells respond to the fluoxetine effect by upregulating Kv3.1b expression. On the other hand, the possible relationship between the fluoxetine effect on the kinetics of 5HT1b differentiation and Kv3.1bexpression, would suggest the Kv3.1b channel as a target of an antidepressant drug as well as it was suggested for 5HT1b.
Kv3.1 通道在神经元中大量表达,其功能障碍导致睡眠不足、神经退行性疾病和抑郁症。氟西汀是一种常用于治疗抑郁症的选择性 5-羟色胺再摄取抑制剂,也作用于 Kv3.1。为了定义 Kv3.1 与 5-羟色胺受体 (SR) 药理学调节之间的关系,我们表明,1C11,一种血清素能细胞系,在诱导存在(分化细胞 (1C11D)) 或不存在(未分化细胞 (1C11ND)) 的情况下表达不同的电压门控钾 (VGK) 通道亚型。只有 Kv1.2 和 Kv3.1 转录本增加,即使 Kv3.1b 转录本的水平在 1C11D 中最高,并且在氟西汀后在 1C11ND 中降低,但在 1C11D 中降低。Kv3.1 通道蛋白在 1C11ND 和 1C11D 中表达,但仅在 1C11D 中被氟西汀增强。全细胞测量证实,1C11 细胞表达 (VGK) 电流,随着细胞发育的进行而依次增加。此外,SR 5HT1b 在 1C11D 中高度表达,但氟西汀增加 1C11ND 中转录本的水平,并显著降低 1C11D 中转录本的水平。血清素剂量表明,氟西汀在 10 nM 时阻断 1C11ND 中的血清素再摄取,但通过降低 5HT1b 受体密度来减缓其释放。我们提供了第一个实验证据,证明 1C11 表达 Kv3.1b,这证实了它在分化过程中的主要作用。细胞通过上调 Kv3.1b 表达来响应氟西汀的作用。另一方面,氟西汀对 5HT1b 分化和 Kv3.1b 表达动力学的影响之间的可能关系表明,Kv3.1b 通道不仅是抗抑郁药物的靶点,也可能是 5HT1b 的靶点。