Nishimura K, Ueki M, Kaneto H, Hazato T
Department of Anesthesiology, Juntendo University, School of Medicine, Tokyo.
Masui. 1993 Nov;42(11):1663-70.
Spinorphin, a potent inhibitor of enkephalin degrading enzyme isolated from the bovine spinal cord, produces a dose-related inhibition of electrically evoked contractions of both MVD (mouse vas deferens) and GPI (guinea-pig ileum). Analgesic activity of Spinorphin was evaluated by the tail pinch method. The intraventricularly injected Spinorphin produced antinociceptive effect in a dose-dependent manner, in dose of 50-200 micrograms.mouse-1. Most Spinorphin was degraded when incubated in the spinal cord for 24 hs. However, approximately 86% of the Spinorphin was intact on HPLC when incubated with probestin, which is an inhibitor of aminopeptidase-M. Spinorphin has a high inhibitory activity against enkephalin degrading enzymes when compared to the various hydrolysis products. In conclusion, the most important structure for enkephalin inhibitory activity in Spinorphin. It is suggested that Spinorphin acts as a neuromodulator of enkephalin metabolism in the spinal cord.
斯皮诺啡是一种从牛脊髓中分离出的强啡肽降解酶抑制剂，对小鼠输精管（MVD）和豚鼠回肠（GPI）的电诱发收缩产生剂量相关的抑制作用。通过夹尾法评估斯皮诺啡的镇痛活性。脑室内注射斯皮诺啡以剂量依赖方式产生抗伤害感受作用，剂量为50 - 200微克·小鼠⁻¹。当在脊髓中孵育24小时时，大多数斯皮诺啡会降解。然而，当与氨肽酶-M抑制剂普罗贝斯汀一起孵育时，约86%的斯皮诺啡在高效液相色谱上保持完整。与各种水解产物相比，斯皮诺啡对强啡肽降解酶具有高抑制活性。总之，斯皮诺啡中强啡肽抑制活性的最重要结构。提示斯皮诺啡作为脊髓中强啡肽代谢的神经调节剂发挥作用。
