Zwart A S, Davis E A, Widdop R E
Department of Pharmacology, Monash University, Clayton, Victoria, Australia.
Br J Pharmacol. 1998 Dec;125(7):1429-36. doi: 10.1038/sj.bjp.0702210.
The aim of this study was to characterize the angiotensin II receptors in isolated uterine arteries from non pregnant and pregnant rats, since it has been reported from binding studies that ovine uterine arteries contain AT2 receptors. Uterine arterial segments were obtained from virgin, non-pregnant and late pregnant (18-21 days) Sprague-Dawley rats and mounted in small vessel myographs. Concentration-response curves were constructed to angiotensin II (1 nM-10 microM) in the absence and presence of various angiotensin II receptor subtype selective compounds. These included losartan (AT1 antagonist; 1, 10 and 100 nM), PD 123319 (AT2 antagonist; 1 microM) and CGP 42112 (AT2 agonist; 1 microM). Responses to angiotensin II were measured as increases in force (mN) and expressed as a per cent of the response to a K+ depolarizing solution. Losartan (1, 10 and 100 nM) caused significant concentration-dependent rightward shifts of the angiotensin II concentration-response curve in uterine arteries from non-pregnant and pregnant rats. The pA2 values calculated from these data were 9.8 and 9.2, respectively, although the slope of the Schild plot in the non-pregnant group was less than unity. PD 123319 (1 microM) caused significant 6- and 3 fold leftward shifts of the angiotensin II concentration-response curve in uterine arteries from non-pregnant and pregnant rats, respectively. In vessels from pregnant rats, PD 123319 also significantly increased the maximum response to angiotensin II. CGP 42112 (1 microM) attenuated the response to angiotensin II of uterine arteries from non-pregnant rats. This was reflected by a 14 fold rightward shift of the angiotensin II concentration-response curve and a decrease in the maximum response. In uterine arteries from pregnant rats, CGP 42112 (1 microM) caused a 3 fold rightward shift of the angiotensin II concentration-response curve, but had no effect on the maximum response. PD 123319 (1 microM) and CGP 42112 (1 microM) had no effect on the concentration-response curves to phenylephrine (PE) of uterine arteries from non-pregnant or pregnant rats. In addition, CGP 42112 (1 nM-1 mM) had no vasodilator effect on tissues precontracted with phenylephrine. These results suggest that the contractile responses of the rat uterine artery are mediated by the AT1 receptor. Furthermore, in this vascular preparation, the AT2 receptor appears to inhibit the response mediated by the AT1 receptor, although, this is not uniform between the non-pregnant and pregnant states.
本研究的目的是对未孕和孕鼠离体子宫动脉中的血管紧张素II受体进行表征,因为结合研究报告称绵羊子宫动脉含有AT2受体。从处女、未孕和妊娠晚期(18 - 21天)的Sprague-Dawley大鼠获取子宫动脉段,并安装在小血管肌动描记器中。在不存在和存在各种血管紧张素II受体亚型选择性化合物的情况下,构建血管紧张素II(1 nM - 10 microM)的浓度 - 反应曲线。这些化合物包括氯沙坦(AT1拮抗剂;1、10和100 nM)、PD 123319(AT2拮抗剂;1 microM)和CGP 42112(AT2激动剂;1 microM)。以力的增加(mN)来测量对血管紧张素II的反应,并表示为对K + 去极化溶液反应的百分比。氯沙坦(1、10和100 nM)使未孕和孕鼠子宫动脉中血管紧张素II浓度 - 反应曲线出现显著的浓度依赖性右移。根据这些数据计算出的pA2值分别为9.8和9.2,尽管未孕组Schild图的斜率小于1。PD 123319(1 microM)使未孕和孕鼠子宫动脉中血管紧张素II浓度 - 反应曲线分别显著左移6倍和3倍。在孕鼠的血管中,PD 123319还显著增加了对血管紧张素II的最大反应。CGP 42112(1 microM)减弱了未孕鼠子宫动脉对血管紧张素II的反应。这表现为血管紧张素II浓度 - 反应曲线右移14倍以及最大反应降低。在孕鼠子宫动脉中,CGP 42112(1 microM)使血管紧张素II浓度 - 反应曲线右移3倍,但对最大反应无影响。PD 123319(1 microM)和CGP 42112(1 microM)对未孕或孕鼠子宫动脉对去氧肾上腺素(PE)的浓度 - 反应曲线无影响。此外,CGP 42112(1 nM - 1 mM)对用去氧肾上腺素预收缩的组织无舒张血管作用。这些结果表明,大鼠子宫动脉的收缩反应由AT1受体介导。此外,在这种血管制剂中,AT2受体似乎抑制由AT1受体介导的反应,尽管在未孕和孕态之间情况并不一致。