Pert C B, Pert A, Chang J K, Fong B T
Science. 1976 Oct 15;194(4262):330-2. doi: 10.1126/science.968485.
[D-Ala2]-Met-enkephalinamide (DALA), a synthetic enkephalin analog designed by in vitro analysis, binds to opiate receptors almost as tightly as methionine-enkephalin. Since it is not susceptible to degradation by brain enzymes, low doses (5 to 10 micrograms) cause profound, long-lasting, morphine-like analgesia when microinjected into rat brain.
[D-丙氨酸2]-甲硫氨酸脑啡肽酰胺(DALA)是一种通过体外分析设计的合成脑啡肽类似物,它与阿片受体的结合亲和力几乎与甲硫氨酸脑啡肽相同。由于它不易被脑内酶降解,当以低剂量(5至10微克)微量注射到大鼠脑内时,会产生深度、持久的吗啡样镇痛作用。