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首页> 外文期刊>Journal of cellular and molecular medicine. >Hiding in Plain Sight: Nebivolol Exhibits Compelling Tocolytic Properties
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Hiding in Plain Sight: Nebivolol Exhibits Compelling Tocolytic Properties

机译：躲藏在纯净的视线中：奈必洛尔展现出令人信服的溶卵特性

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Preterm birth before 37 weeks of completed gestation results in numerous health consequences for the foetus. Preterm labour leads to preterm birth in over 50% of cases, and no FDA‐approved treatment can prevent labour or help a foetus remain in the womb until term. Examination of nitric oxide mediated relaxation signaling in the uterine smooth muscle reveals a role for protein S‐nitrosation. The recent discovery of upregulated S‐nitrosoglutathione reductase (GSNOR) in spontaneously preterm labouring women has emphasized the need to explore the function of S‐nitrosation regulation in the maintenance of uterine quiescence. Here we have examined the ability of nebivolol to relax uterine smooth muscle and tested recent claims that nebivolol is a GSNOR inhibitor. In uterine smooth muscle strips from both mouse and human, nebivolol relaxes oxytocin‐induced contractions in a dose dependent manner. Our data indicates that nebivolol has no effect on GSNOR activity, nor does nebivolol inhibit thioredoxin reductase, two of the major protein denitrosylases. The ability of nebivolol to relax uterine smooth muscle is likely the combined effects of increased nitric oxide synthase activity and β3‐adregnegic stimulation.
机译：完全妊娠37周之前的早产会对胎儿造成许多健康后果。早产导致超过50％的病例早产，并且没有FDA批准的治疗方法可以防止分娩或帮助胎儿在分娩前留在子宫内。子宫平滑肌中一氧化氮介导的松弛信号的检查揭示了蛋白质S亚硝化的作用。最近在自发早产妇女中发现S-亚硝基谷胱甘肽还原酶（GSNOR）上调的新发现，强调需要探索S-亚硝化调节在维持子宫静止中的功能。在这里，我们检查了奈必洛尔松弛子宫平滑肌的能力，并测试了最近的说法奈必洛尔是GSNOR抑制剂。在小鼠和人的子宫平滑肌条中，奈必洛尔以剂量依赖性方式放松催产素诱导的收缩。我们的数据表明奈必洛尔对GSNOR活性没有影响，奈必洛尔也不能抑制硫氧还蛋白还原酶，这是两种主要的蛋白质脱氮酶。 nebivolol放松子宫平滑肌的能力可能是一氧化氮合酶活性增加和β3肾上腺素能刺激的综合作用。

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