Kitajima S, Ozaki H, Karaki H
Department of Veterinary Pharmacology, Faculty of Agriculture, University of Tokyo, Japan.
Eur J Pharmacol. 1994 Feb 15;266(3):263-7. doi: 10.1016/0922-4106(94)90135-x.
The role of different subtypes of P2 purinoceptors on cytosolic Ca2+ level ([Ca2+]i) was examined in vascular smooth muscle of rat aorta. alpha beta-Methylene-ATP (P2X agonist), 2-methylthio-ATP (P2Y agonist), UTP and ATP gamma S (P2U agonists), and ATP (nonselective P2 agonist) induced a transient increase followed by a small sustained increase in [Ca2+]i in a concentration dependent manner. Among these agonists, alpha beta-methylene-ATP was the most potent. In the absence of extracellular Ca2+ (with 0.5 mM EGTA), ATP, UTP and ATP gamma S induced a transient increase in [Ca2+]i whereas alpha beta-methylene-ATP and 2-methylthio-ATP were ineffective. ATP gamma S showed the highest potency in Ca(2+)-free solution. After desensitization of P2X purinoceptor, ATP, UTP and ATP gamma S induced a rapid increase in [Ca2+]i followed by a sustained increase while alpha beta-methylene-ATP and 2-methylthio-ATP were ineffective. These results suggest that Ca2+ release from the intracellular Ca2+ store is mediated by P2U purinoceptor whereas Ca2+ influx is mediated by both P2X and P2U purinoceptors in the rat aortic smooth muscle.
在大鼠主动脉血管平滑肌中研究了P2嘌呤受体不同亚型对胞质Ca2+水平([Ca2+]i)的作用。αβ-亚甲基ATP(P2X激动剂)、2-甲硫基ATP(P2Y激动剂)、UTP和ATPγS(P2U激动剂)以及ATP(非选择性P2激动剂)以浓度依赖性方式诱导[Ca2+]i先短暂升高,随后小幅持续升高。在这些激动剂中,αβ-亚甲基ATP最有效。在无细胞外Ca2+(含0.5 mM EGTA)的情况下,ATP、UTP和ATPγS诱导[Ca2+]i短暂升高,而αβ-亚甲基ATP和2-甲硫基ATP无效。ATPγS在无Ca2+溶液中效力最高。P2X嘌呤受体脱敏后,ATP、UTP和ATPγS诱导[Ca2+]i迅速升高,随后持续升高,而αβ-亚甲基ATP和2-甲硫基ATP无效。这些结果表明,在大鼠主动脉平滑肌中,细胞内Ca2+储存释放Ca2+由P2U嘌呤受体介导,而Ca2+内流由P2X和P2U嘌呤受体共同介导。