Departamento de Bioquímica, E.U. Óptica, Universidad Complutense de Madrid, Madrid, Spain.
Pharmacogenet Genomics. 2011 Sep;21(9):587-9. doi: 10.1097/FPC.0b013e32834910d1.
We have demonstrated that 5-methoxycarbonylamino-N-acetyltryptamine (5-MCA-NAT), reduces intraocular pressure (IOP) in rabbits. In addition, we have reported a link between hypotensive effect of 5-MCA-NAT and sympathetic nervous system. Moreover, it is known that aqueous humour production is controlled by the activation of adrenoceptors (ADRs) present in the ocular ciliary epithelium. Thus, the aim of this study is to investigate if the hypotensive effect of 5-MCA-NAT is due to a regulation of ciliary ADR genes expression. To confirm this we followed the effect of 5-MCA-NAT on rabbit IOP for 144 consecutive hours. A sustained IOP reduction for up to 72 h (P<0.01) was seen. In addition, changes in ADRB2 and ADRA2A mRNA were measured in cultured rabbit nonpigmented ciliary epithelial cells. After 5-MCA-NAT treatment, a significant downregulation of ADRB2 and upregulation of ADRA2A was observed. These results provide the regulation of ADRs mRNA by 5-MCA-NAT.
我们已经证明 5-甲氧基羰基氨基-N-乙酰色胺（5-MCA-NAT）可降低兔眼内压（IOP）。此外，我们还报告了 5-MCA-NAT 的降压作用与交感神经系统之间的联系。此外，已知房水的产生受到眼睫状上皮中存在的肾上腺素能受体（ADRs）的激活的控制。因此，本研究的目的是研究 5-MCA-NAT 的降压作用是否归因于睫状 ADR 基因表达的调节。为了证实这一点，我们连续 144 小时跟踪 5-MCA-NAT 对兔 IOP 的影响。观察到长达 72 小时的持续 IOP 降低（P<0.01）。此外，还测量了培养的兔非色素睫状上皮细胞中 ADRB2 和 ADRA2A mRNA 的变化。5-MCA-NAT 处理后，ADRB2 的表达显著下调，ADRA2A 的表达上调。这些结果提供了 5-MCA-NAT 对 ADRs mRNA 的调节。
