Zadina J E, Kastin A J, Hackler L, Chang S L
VA Medical Center, New Orleans, LA.
Peptides. 1994;15(8):1567-9. doi: 10.1016/0196-9781(94)90135-x.
Two cyclic analogues of the brain peptide Tyr-W-MIF-1 (Tyr-Pro-Trp-Gly-NH2) were synthesized and tested for analgesic activity in the rat tail flick test after intracerebroventricular (ICV) injection. The analogues were about 200-fold more potent than the parent peptide. Analgesia was dose dependent, and at 1 microgram the two analogues, the mu-selective enkephalin analogue DAMGO (Tyr-D-Ala-Gly-N-Me-Phe-Gly-ol), and morphine, all produced analgesia lasting between 40 and 60 min. Analgesia of longer duration was evident at higher doses of the analogues and lasted more than 6 h after 100 micrograms, the highest dose tested. The results show that peptide analogues based on the structure of the endogenously occurring Tyr-W-MIF-1 can produce potent and long-lasting effects on nociception.
合成了脑肽Tyr-W-MIF-1（Tyr-Pro-Trp-Gly-NH2）的两种环状类似物，并在脑室内（ICV）注射后通过大鼠甩尾试验测试其镇痛活性。这些类似物的效力比母体肽强约200倍。镇痛呈剂量依赖性，在1微克时，这两种类似物、μ-选择性脑啡肽类似物DAMGO（Tyr-D-Ala-Gly-N-Me-Phe-Gly-ol）和吗啡均产生持续40至60分钟的镇痛作用。在较高剂量的类似物下，镇痛持续时间更长，在测试的最高剂量100微克后持续超过6小时。结果表明，基于内源性Tyr-W-MIF-1结构的肽类似物可对伤害感受产生强效且持久的作用。
