Akil H, Hewlett W A, Barchas J D, Li C H
Eur J Pharmacol. 1980 May 30;64(1):1-8. doi: 10.1016/0014-2999(80)90363-5.
The binding of tritiated beta-endorphin (3H-beta-EP) to brain homogenates is described. This has been difficult to achieve due to the lack of availability of 3H-beta-EP and to technical difficulties associated with high non-specific binding of beta-EP. We now report that 3H-beta-EP binding is saturable, stereospecific, has high affinity and is inhibited by sodium. Its dissociation rate is ten-fold longer than that of naloxone. Its regional distribution exhibits interesting differences from naloxone and enkephalin binding. ACTH1-24 appears to displace it more effectively than it displaces 3H-naloxone. The results are discussed in terms of multiple transmitter systems and the multiple opiate receptor hypothesis.
本文描述了氚标记的β-内啡肽（3H-β-EP）与脑匀浆的结合情况。由于缺乏3H-β-EP以及与β-EP高非特异性结合相关的技术难题，此前一直难以实现这一研究。我们现在报告，3H-β-EP结合具有饱和性、立体特异性、高亲和力且受钠抑制。其解离速率比纳洛酮长十倍。其区域分布与纳洛酮和脑啡肽结合呈现出有趣的差异。促肾上腺皮质激素1-24似乎比其取代3H-纳洛酮更有效地取代它。本文从多种递质系统和多重阿片受体假说的角度对结果进行了讨论。
