兔肠系膜动脉中两种亚型的P2嘌呤受体：活性蓝2选择性抑制通过P2Y嘌呤受体而非P2X嘌呤受体介导的反应。
P2-purinoceptors of two subtypes in the rabbit mesenteric artery: reactive blue 2 selectively inhibits responses mediated via the P2y-but not the P2x-purinoceptor.
作者信息
Burnstock G, Warland J J
出版信息
Br J Pharmacol. 1987 Feb;90(2):383-91. doi: 10.1111/j.1476-5381.1987.tb08968.x.
Abstract
alpha,beta-Methylene ATP and ATP both produced concentration-dependent contractions of the isolated mesenteric artery of the rabbit that were not inhibited by reactive blue 2. In preparations where the tone had been raised with noradrenaline, ATP and 2-methylthio ATP, but not alpha,beta-methylene ATP, produced relaxations of the vessel. These relaxations were inhibited in the presence of reactive blue 2. Reactive blue 2 did not inhibit the contractions to noradrenaline, and only slightly inhibited relaxations to adenosine and acetylcholine. The rank order of potency of purine nucleotide analogues in contracting the vessel was: alpha,beta-methylene ATP greater than beta,gamma-methylene ATP = 2-methylthio ATP greater than ATP, and in relaxing the vessel at raised tone was: 2-methylthio ATP greater than ATP greater than beta,gamma-methylene ATP greater than alpha,beta-methylene ATP. It is concluded from this study that in the isolated mesenteric artery of the rabbit, purine nucleotides act via P2y-purinoceptors to cause the muscle to relax and via P2x-purinoceptors to cause the muscle to contract. The results also suggest that reactive blue 2 selectively inhibits responses mediated via the P2y-purinoceptor, at least within a limited concentration range.
摘要
α,β-亚甲基ATP和ATP均可使家兔离体肠系膜动脉产生浓度依赖性收缩，且不受活性蓝2的抑制。在已用去甲肾上腺素提高张力的标本中，ATP和2-甲硫基ATP可使血管舒张，但α,β-亚甲基ATP不能。这些舒张作用在活性蓝2存在时受到抑制。活性蓝2不抑制对去甲肾上腺素的收缩反应，仅轻微抑制对腺苷和乙酰胆碱的舒张反应。嘌呤核苷酸类似物使血管收缩的效力顺序为：α,β-亚甲基ATP＞β,γ-亚甲基ATP = 2-甲硫基ATP＞ATP，在提高张力时使血管舒张的效力顺序为：2-甲硫基ATP＞ATP＞β,γ-亚甲基ATP＞α,β-亚甲基ATP。本研究得出结论，在家兔离体肠系膜动脉中，嘌呤核苷酸通过P2y嘌呤受体使肌肉舒张，通过P2x嘌呤受体使肌肉收缩。结果还表明，活性蓝2至少在有限浓度范围内选择性抑制通过P2y嘌呤受体介导的反应。
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