Pert A, Simantov R, Snyder S H
Brain Res. 1977 Nov 18;136(3):523-33. doi: 10.1016/0006-8993(77)90076-2.
A partially purified morphine-like peptide 'enkephalin' (PPE) extract from bovine brain elicited pronounced apparent analgesia after injection into the periaqueductal gray matter of rat brain. This analgesia was reversed by the opiate antagonist naloxone in a dose-dependent fashion. Analgesia was more rapid in onset and much shorter in duration after PPE than after morphine administration. Analgesia was elicited only by those ion exchange column fractions of PPE that competed potently for opiate receptor binding. No analgesia could be detected when PPE or morphine injections were administered at a site 2 mm lateral to the periaqueductal gray matter. The potencies of synthetic methionine- and leucine-enkephalin in eliciting analgesia were less than 1% of those of partially purified enkephalin extracts when doses of equivalent ability to compete for opiate receptor binding were compared.
从牛脑提取的部分纯化的类吗啡肽“脑啡肽”(PPE)注入大鼠脑导水管周围灰质后,引发明显的表观镇痛作用。这种镇痛作用可被阿片拮抗剂纳洛酮以剂量依赖的方式逆转。与注射吗啡后相比,PPE注射后镇痛起效更快,持续时间更短。只有那些能有效竞争阿片受体结合的PPE离子交换柱级分才能引发镇痛作用。当在导水管周围灰质外侧2毫米处注射PPE或吗啡时,未检测到镇痛作用。当比较具有同等竞争阿片受体结合能力的剂量时,合成的甲硫氨酸脑啡肽和亮氨酸脑啡肽引发镇痛作用的效力不到部分纯化脑啡肽提取物的1%。