Maille Nicole, Gokina Natalia, Mandalà Maurizio, Colton Ilsley, Osol George
Department of Obstetrics and Gynecology and Reproductive Sciences, University of Vermont College of Medicine, USA.
Department of Obstetrics and Gynecology and Reproductive Sciences, University of Vermont College of Medicine, USA; Department of Biology, Ecology and Earth Science, University of Calabria, Italy.
Vascul Pharmacol. 2016 Mar;78:36-42. doi: 10.1016/j.vph.2015.07.009. Epub 2015 Jul 18.
The cellular mechanisms of hydralazine-induced relaxation were investigated in isolated mesenteric resistance arteries from pregnant rats. Administration of hydralazine relaxed phenylephrine-constricted mesenteric arteries with an EC50 of 3.6 ± 0.3 μM and an efficacy of 75 ± 6.2%. These vasodilatory effects were abolished by: (1) preconstriction with a potassium depolarizing solution, (2) endothelial denudation (for concentrations of hydralazine<10 μM), (3) addition of non-selective cyclooxygenase-1 and cyclooxygenase-2 inhibitors, and (4) pretreatment with a prostacyclin receptor antagonist (R01138452). Nitric oxide synthase (NOS) inhibition did not significantly alter the sensitivity or magnitude of the vasodilatory response; surprisingly, exposure to hydralazine also did not elevate endothelial cell Ca(2+), suggesting a novel mechanism of activation. In summary, hydralazine is a potent resistance artery vasodilator that affects both endothelial and vascular smooth muscle (VSM) cells in a concentration-dependent manner. At clinically relevant concentrations (<10 μM), its effects in the splanchnic resistance vasculature are: (1) primarily endothelial in origin, require (2) hyperpolarization and (3) activation of COX, and (4) are mediated by the PGI2 (IP) receptor.
在妊娠大鼠的离体肠系膜阻力动脉中研究了肼屈嗪诱导舒张的细胞机制。给予肼屈嗪可使去氧肾上腺素收缩的肠系膜动脉舒张,其半数有效浓度(EC50)为3.6±0.3μM,效能为75±6.2%。这些血管舒张作用被以下因素消除:(1)用钾去极化溶液预收缩;(2)内皮剥脱(对于肼屈嗪浓度<10μM);(3)添加非选择性环氧化酶-1和环氧化酶-2抑制剂;(4)用前列环素受体拮抗剂(R01138452)预处理。一氧化氮合酶(NOS)抑制并未显著改变血管舒张反应的敏感性或幅度;令人惊讶的是,暴露于肼屈嗪也未升高内皮细胞Ca(2+),提示存在一种新的激活机制。总之,肼屈嗪是一种强效的阻力动脉血管舒张剂,以浓度依赖方式影响内皮细胞和血管平滑肌(VSM)细胞。在临床相关浓度(<10μM)下,其在内脏阻力血管系统中的作用为:(1)主要起源于内皮,需要(2)超极化和(3)COX激活,且(4)由前列环素(IP)受体介导。