Experimental data regarding the implications of certain minimum structure enkephalin-like peptides in nociceptive processing.

Irina M Jaba, D Vasincu, G Manolidis, I Haulică, O C Mungiu
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Abstract

The aim of this study was to investigate the importance of the amino acidic sequence at N-terminal end of certain minimum structure enkephalin-like peptides for the analgesic activity. Different groups of mice or rats were treated with 1) L-tyrosine (i.p. 200 mg/kg), 2) Tyr-Phe (i.t. 0.5 mg/rat), 3) Tyr-Pro-Phe (i.t. 0.5 mg/rat), 4) Gly-Tyr (i.t. 0.5 mg/rat), 5) Tyr-Gly-Gly (i.t. 0.5 mg/rat). Different tests were utilized to evaluate the antinociceptive effect of the substances tested: thermal nociception (hot plate test, plantar test), mechanical nociception (analgesymeter test). Tyr-Pro-Phe, Tyr-Gly-Gly, Tyr-Phe, but not Gly-Tyr, elicited analgesic activity. So, the presumption made in the case of atypical opioid peptides that opioid-like activity in case of peptides presumes a tyrosine residue at the N-terminal sequence, applies for shorter peptides. It appears also that minimal structure brain peptides with an N-terminal Tyr-Pro, rather than the Tyr-Gly-Gly-Phe sequence typical of other endogenous opioids, can provide better affinity for the opioid receptors and stronger analgesic activity. The inhibition of their analgesic effect by previous administration of naloxone proves that this effect is mediated through the endogenous opioid system.

某些最小结构脑啡肽样肽在伤害性加工中的意义的实验数据。
本研究的目的是探讨某些最小结构脑啡肽样肽n端氨基酸序列对镇痛活性的重要性。各组小鼠或大鼠分别给予1)l -酪氨酸(灌胃200 mg/kg)、2)酪氨酸-丙氨酸(灌胃0.5 mg/kg)、3)酪氨酸-脯氨酸(灌胃0.5 mg/kg)、4)甘氨酸-酪氨酸(灌胃0.5 mg/kg)、5)甘氨酸-甘氨酸-甘氨酸(灌胃0.5 mg/kg)。采用热痛觉(热板试验、足底试验)、机械痛觉(镇痛计试验)两种不同的试验来评价所测物质的抗痛觉作用。Tyr-Pro-Phe, Tyr-Gly-Gly, Tyr-Phe,但Gly-Tyr不具有镇痛活性。因此,在非典型阿片样肽的情况下,阿片样活性在肽的情况下假定在n端序列有酪氨酸残基,适用于较短的肽。与其他内源性阿片的典型的Tyr-Gly-Gly-Phe序列相比,具有n端Tyr-Pro序列的最小结构脑肽对阿片受体具有更好的亲和力和更强的镇痛活性。先前服用纳洛酮对其镇痛作用的抑制证明这种作用是通过内源性阿片系统介导的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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