Rubino A, Ziabary L, Burnstock G
Autonomic Neuroscience Institute, Royal Free and University College Medical School, University College London, UK.
Eur J Pharmacol. 1999 Apr 9;370(2):139-43. doi: 10.1016/s0014-2999(99)00150-8.
Vasoconstrictor and vasodilator responses of isolated rat intrapulmonary arteries to the pyrimidine nucleotides UTP and UDP were evaluated and compared with vascular responses to ATP and its analogues. UTP and UDP (1-500 microM) were equipotent in inducing concentration-dependent vasoconstriction, unaffected by the P2 receptor antagonists suramin (100 microM) and Reactive blue 2 (50 microM); ATP (10-500 microM) produced weaker vasoconstriction. UTP and UDP lacked vasodilator activity, while ATP and its analogue 2-methylthio ATP evoked endothelium-dependent vasodilatation. These results indicate that UTP and UDP evoke vasoconstriction of rat intrapulmonary arteries whereas ATP is predominantly a vasodilator at the same arteries. Furthermore, the pharmacological profile of the native UTP/UDP receptor differs from that of the known P2Y2, P2Y4 and P2Y6 recombinant receptors for pyrimidine nucleotides.
评估了离体大鼠肺内动脉对嘧啶核苷酸UTP和UDP的血管收缩和血管舒张反应,并与对ATP及其类似物的血管反应进行了比较。UTP和UDP(1-500微摩尔)在诱导浓度依赖性血管收缩方面具有同等效力,不受P2受体拮抗剂苏拉明(100微摩尔)和活性蓝2(50微摩尔)的影响;ATP(10-500微摩尔)产生较弱的血管收缩。UTP和UDP缺乏血管舒张活性,而ATP及其类似物2-甲硫基ATP可引起内皮依赖性血管舒张。这些结果表明,UTP和UDP可引起大鼠肺内动脉血管收缩,而ATP在相同动脉中主要起血管舒张作用。此外,天然UTP/UDP受体的药理学特征与已知的嘧啶核苷酸P2Y2、P2Y4和P2Y6重组受体不同。