Sesti Casilde, Koyama Motohiro, Broekman M Johan, Marcus Aaron J, Levi Roberto
Department of Pharmacology, Room LC419, 1300 York Ave., Weill Medical College of Cornell University, New York, NY 10021, USA.
J Pharmacol Exp Ther. 2003 Jul;306(1):238-44. doi: 10.1124/jpet.103.049874. Epub 2003 Apr 3.
We recently reported that ATP, coreleased with norepinephrine (NE) from cardiac sympathetic nerves, increases NE exocytosis via a positive feedback mechanism. A neuronal ectonucleotidase (E-NTPDase) metabolizes the released ATP, decreasing NE exocytosis. Excessive NE release in myocardial ischemia exacerbates cardiac dysfunction. Thus, we studied whether the ATP-mediated autocrine amplification of NE release is operative in ischemia and, if so, whether it can be modulated by E-NTPDase and its recombinant equivalent, solCD39. Isolated, guinea pig hearts underwent 10- or 20-min ischemic episodes, wherein NE was released by exocytosis and reversal of the NE transporter, respectively. Furthermore, to restrict the role of E-NTPDase to transmitter ATP, sympathetic nerve endings were isolated (cardiac synaptosomes) and subjected to increasing periods of ischemia. Availability of released ATP at the nerve terminals was either increased via E-NTPDase inhibition or diminished by enhancing ATP hydrolysis with solCD39. P2X receptor blockade with PPADS was used to attenuate the effects of released ATP. We found that, in short-term ischemia (but, as anticipated, not in protracted ischemia, where NE release is carrier-mediated), ATP exocytosis was linearly correlated with that of NE. This indicates that by limiting the availability of ATP at sympathetic terminals, E-NTPDase effectively attenuates NE exocytosis in myocardial ischemia. Our findings suggest a key role for neuronal E-NTPDase in the control of adrenergic function in the ischemic heart. Because excessive NE release is an established cause of dysfunction in ischemic heart disease, solCD39 may offer a novel therapeutic approach to myocardial ischemia and its consequences.
我们最近报道,三磷酸腺苷(ATP)与去甲肾上腺素(NE)从心脏交感神经共同释放,通过正反馈机制增加NE的胞吐作用。一种神经元外切核苷酸酶(E-NTPDase)可代谢释放的ATP,减少NE的胞吐作用。心肌缺血时NE的过度释放会加剧心脏功能障碍。因此,我们研究了ATP介导的NE释放自分泌放大在缺血时是否起作用,如果是,它是否可被E-NTPDase及其重组等效物可溶性CD39调节。分离的豚鼠心脏经历10或20分钟的缺血发作,其中NE分别通过胞吐作用和NE转运体的逆转而释放。此外,为了将E-NTPDase的作用限制于递质ATP,分离了交感神经末梢(心脏突触体)并使其经历不同时长的缺血。通过抑制E-NTPDase增加神经末梢释放的ATP的可利用性,或通过用可溶性CD39增强ATP水解来减少其可利用性。用吡哆醛-6-偶氮-2′,4′-二磺酸(PPADS)阻断P2X受体以减弱释放的ATP的作用。我们发现,在短期缺血时(但正如预期的,在长期缺血时并非如此,长期缺血时NE的释放是由载体介导的),ATP的胞吐作用与NE的胞吐作用呈线性相关。这表明通过限制交感神经末梢处ATP的可利用性,E-NTPDase可有效减弱心肌缺血时NE的胞吐作用。我们的研究结果表明神经元E-NTPDase在缺血心脏肾上腺素能功能的控制中起关键作用。由于NE的过度释放是缺血性心脏病功能障碍的既定原因,可溶性CD39可能为心肌缺血及其后果提供一种新的治疗方法。