人类小肺动脉中两种P2嘌呤受体亚型的证据。

Evidence for two P2-purinoceptor subtypes in human small pulmonary arteries.

Liu S F, McCormack D G, Evans T W, Barnes P J

Department of Thoracic Medicine, National Heart and Lung Institute, London.

Br J Pharmacol. 1989 Nov;98(3):1014-20. doi: 10.1111/j.1476-5381.1989.tb14633.x.

Abstract

P2-purinoceptors have not been characterized in human pulmonary vessels and we therefore examined the effects of adenosine 5'-triphosphate (ATP) and its analogues on human isolated small pulmonary arteries (SPA) in vitro. 2. Contractile responses were induced by all of the analogues, with the rank order of potency alpha,beta-methylene-ATP (alpha,beta-meATP) = beta,gamma-methylene-ATP (beta,gamma-meATP) greater than ATP greater than 2-methylthio-ATP, indicating the presence of vasoconstrictor P2x receptors. 3. In precontracted SPA, vasodilator responses were produced by all of the analogues. The rank order of potency for the analogues causing vasodilator responses was: 2-methylthio-ATP much greater than ATP much greater than beta,gamma-meATP = alpha,beta-meATP, indicating a vasodilator P2y receptor. 4. Removal of endothelial cells had no significant effect on either the contractile or relaxant responses to any of the analogues. 5. After pretreatment of the endothelium-denuded vessels with alpha,beta-meATP (to desensitize P2x receptors), the contractile response to beta,gamma-meATP (a potent P2x receptor agonist) was abolished. 6. We conclude that both P2x- and P2y-purinoceptors are present in human SPA and that both receptors reside on the vascular smooth muscle.

摘要

P2嘌呤受体尚未在人肺血管中得到鉴定，因此我们在体外研究了5'-三磷酸腺苷（ATP）及其类似物对人离体小肺动脉（SPA）的作用。2. 所有类似物均诱导出收缩反应，其效力顺序为α,β-亚甲基ATP（α,β-meATP）=β,γ-亚甲基ATP（β,γ-meATP）＞ATP＞2-甲硫基ATP，表明存在血管收缩性P2x受体。3. 在预收缩的SPA中，所有类似物均产生血管舒张反应。引起血管舒张反应的类似物的效力顺序为：2-甲硫基ATP＞＞ATP＞＞β,γ-meATP =α,β-meATP，表明存在血管舒张性P2y受体。4. 去除内皮细胞对任何类似物的收缩或舒张反应均无显著影响。5. 用α,β-meATP预处理去内皮血管（以使P2x受体脱敏）后，对β,γ-meATP（一种有效的P2x受体激动剂）的收缩反应被消除。6. 我们得出结论，P2x和P2y嘌呤受体均存在于人SPA中，且两种受体均位于血管平滑肌上。