Guimarães S, Paiva M Q, Moura D, Vaz-da-Silva M J, Albino-Teixeira A
Institute of Pharmacology and Therapeutics, Faculty of Medicine, Porto, Portugal.
Naunyn Schmiedebergs Arch Pharmacol. 1994 Dec;350(6):692-5. doi: 10.1007/BF00169376.
The present investigation was undertaken to see whether a long-term inhibition of adenosine receptors--leading to hypertension--interferes with alpha 2-adrenoceptor-mediated modulation of noradrenaline release. Rat tail arteries were removed from normal and from hypertensive animals obtained by chronic treatment with intraperitoneally infused DPSPX (1,3-dipropyl-8-sulphophenylxanthine) or orally administered L-NAME (NG-Nitro-L-arginine methyl ester). To study prejunctional effects, the influence of UK-14,304 (5-bromo-6(imidazoline-2-ylamino)-quinoxaline) and yohimbine on the overflow of tritium evoked by electrical stimulation (100 V; 1 Hz; 2 ms; 5 min) from tissues preloaded with 3H-noradrenaline was analysed. To study postjunctional effects, concentration-response curves to UK-14,304 were determined. In DPSPX-treated rats there was an enhancement of the prejunctional effects of UK-14,304: its Ec30% was reduced from 381 (250; 579) to 85 (73; 99) nmol.l-1 (n = 5; P < 0.05) and its maximal effect--expressed as percent reduction of tritium overflow-increased from 45 +/- 5% to 61 +/- 5% (n = 6; P < 0.05). In L-NAME-treated rats there was no change in either of these two parameters. At the postjunctional level, there was no change in the sensitivity to UK-14,304 in tissues from either DPSPX- or L-NAME-treated rats. Yohimbine (10-1000 nmol.l-1) caused a concentration-dependent increase of tritium overflow evoked by electrical stimulation in both control and hypertensive animals (either DPSPX- or L-NAME-treated).(ABSTRACT TRUNCATED AT 250 WORDS)
本研究旨在观察长期抑制腺苷受体(导致高血压)是否会干扰α₂肾上腺素能受体介导的去甲肾上腺素释放调节。从正常大鼠以及通过腹腔注射DPSPX(1,3 - 二丙基 - 8 - 磺苯基黄嘌呤)或口服L - 精氨酸甲酯(L - NAME)进行慢性治疗获得的高血压大鼠身上取出尾动脉。为研究接头前效应,分析了UK - 14,304(5 - 溴 - 6(咪唑啉 - 2 - 基氨基)喹喔啉)和育亨宾对预先用³H - 去甲肾上腺素加载的组织经电刺激(100 V;1 Hz;2 ms;5分钟)诱发的氚溢出的影响。为研究接头后效应,测定了对UK - 14,304的浓度 - 反应曲线。在DPSPX处理的大鼠中,UK - 14,304的接头前效应增强:其引起30%效应的浓度(Ec30%)从381(250;579)降至85(73;99)nmol·L⁻¹(n = 5;P < 0.05),其最大效应(以氚溢出减少百分比表示)从45±5%增加到61±5%(n = 6;P < 0.05)。在L - NAME处理的大鼠中,这两个参数均无变化。在接头后水平,DPSPX或L - NAME处理的大鼠组织对UK - 14,304的敏感性均无变化。育亨宾(10 - 1000 nmol·L⁻¹)在对照动物和高血压动物(DPSPX或L - NAME处理)中均引起电刺激诱发的氚溢出呈浓度依赖性增加。(摘要截短于250字)