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用纳洛肼(NZI,1×10~(-5)M)或14-羟基双氢吗啡肼(HZI,1×10~(-6))与大鼠脑匀浆P_2膜制备保温后,以Tris缓冲液反复洗涤,阿片受点可完全恢复与[~3H]双氢吗啡([~3H]DHM)的结合能力。在离体豚鼠回肠纵肌(GPI)试验中,HZI对电刺激收缩的抑制及NZI对吗啡(Mor)抑制作用的对抗亦皆可被洗掉,此外HZI对收缩的抑制还可被纳洛酮(Nal)所逆转,说明它们与阿片受点的结合都是可逆的。HZI镇痛作用ED_(50)为1.3 mg/kg(小鼠热板法SC),略强于Mor(3 mg/kg),持续时间与Mor相似。NZI对Mor镇痛的对抗可持续十余小时。
After incubation with naloxone (NZI, 1 × 10 -5 M) or 14-hydroxyhydromorphine hydrazine (HZI, 1 × 10 -6) and rat brain homogenate P 2 membrane, Repeated washing with Tris buffer and opiate receiving point completely restored the binding ability to [~ 3H] dihydromorphine ([~ 3H] DHM). In isolated guinea pig ileum longitudinal muscle (GPI) test, HZI inhibition of electrical stimulation contraction and NZI antagonism of morphine (Mor) inhibition can also be washed off, in addition HZI inhibition of contraction can also be naloxone (Nal), indicating that their binding to opiate receptors is reversible. HZI analgesia ED_ (50) 1.3 mg / kg (mouse hot plate method SC), slightly stronger than Mor (3 mg / kg), duration and Mor similar. The antagonism of NZI to Mor Analgesia lasts more than ten hours.