Copeland E S, Boykin M E, Kelley J A, Kullberg M P
Biophys J. 1975 Nov;15(11):1125-39. doi: 10.1016/S0006-3495(75)85889-9.
Morphine spin labeled on the phenolic hydroxy group has been prepared using commercially available reagents and characterized by thin layer chromatography, mass spectroscopy, and electron spin resonance spectroscopy. It has been shown that morphine modified in this way retains some opiate activity, does not pass through the blood-brain barrier, and specifically binds to isolate rat brain synaptosomes. Spin labeled morphine has been shown to be an effective biophysical probe complementing radioactive tracer techniques in the study of the narcotic receptor site.
利用市售试剂制备了酚羟基自旋标记的吗啡,并通过薄层色谱、质谱和电子自旋共振光谱对其进行了表征。结果表明,以这种方式修饰的吗啡保留了一些阿片活性,不能穿过血脑屏障,且能特异性结合分离的大鼠脑突触体。自旋标记的吗啡已被证明是一种有效的生物物理探针,可在麻醉受体位点的研究中补充放射性示踪技术。