Tsutsumi K, Saavedra J M
Section on Pharmacology, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892.
Am J Physiol. 1991 Sep;261(3 Pt 2):H667-70. doi: 10.1152/ajpheart.1991.261.3.H667.
Quantitative autoradiography using the agonist 125I-Sar1-angiotensin II was used to localize and characterize angiotensin II (AT) receptors in the anterior cerebral artery of the male rat. This artery showed a moderately high number of AT receptors, localized throughout the arterial wall. The number of receptors was higher (125 +/- 7 fmol/mg protein) in arteries from young 2-wk-old rats compared with those in adult 8-wk-old rats (43 +/- 2 fmol/mg protein). In the anterior cerebral artery, AT binding was insensitive to displacement with the selective AT1 antagonist DuP 753 but was readily displaced by the selective AT2 antagonist CGP-42112 A (concentration eliciting 50% of maximum inhibition: 6 +/- 1 x 10(-10) M). This indicated that the AT receptors in the cerebral artery were of the AT2 subtype. Our observations suggest that AT may exert its effects on cerebral circulation by stimulation of AT2 receptors and that these receptors may play a role during cerebrovascular development.
采用激动剂125I - Sar1 - 血管紧张素II进行定量放射自显影,以定位和表征雄性大鼠大脑前动脉中的血管紧张素II(AT)受体。该动脉显示出中等数量的AT受体,遍布整个动脉壁。与8周龄成年大鼠的动脉(43±2 fmol/mg蛋白质)相比,2周龄幼鼠动脉中的受体数量更高(125±7 fmol/mg蛋白质)。在大脑前动脉中,AT结合对选择性AT1拮抗剂DuP 753的置换不敏感,但很容易被选择性AT2拮抗剂CGP - 42112 A置换(引起最大抑制50%的浓度:6±1×10⁻¹⁰ M)。这表明大脑动脉中的AT受体是AT2亚型。我们的观察结果表明,AT可能通过刺激AT2受体对脑循环发挥作用,并且这些受体可能在脑血管发育过程中起作用。