Zakusov V V, Bulaev V M, Ostrovskaia R U
Biull Eksp Biol Med. 1982 Dec;94(12):51-3.
The effect of intracellular modulators and ions on the analgetic action of the two tetrapeptide analogs, Tyr-D-Ala-Gly-Phe-NH2 and Tyr-D-Ala-Gly-Phe (NO) NH2, was studied in rat experiments. The threshold of pain reaction to electrical stimulation of the tail, evidenced by vocalization, was measured. PGE1, PGE2, PGE2 alpha, cAMP, and dibutyryl cAMP were shown to diminish the effect of the above-mentioned enkephalin analogs. In contrast to cAMP, cGMP was not active in this respect. Among the ions under study (calcium, lithium, rubidium, and cesium), cesium was shown to be the most active. It prevented the increase of the pain reaction threshold and shortened the duration of analgesia. Lithium had no antagonistic effect as regards the enkephalin-induced analgesia. Comparison of these findings with the previously obtained data on the antagonism of the substances under consideration with morphine suggests similarities in the mechanisms of modulation of the effects of opiates and opioids. At the same time the failure of lithium to antagonize the enkephalin analogs and the presence of morphine antagonism point out that the similarities in the mechanisms of ion regulation of exogenous analgetics and enkephalins cannot be regarded as complete enough.
在大鼠实验中研究了细胞内调节剂和离子对两种四肽类似物Tyr-D-Ala-Gly-Phe-NH2和Tyr-D-Ala-Gly-Phe(NO)NH2镇痛作用的影响。通过发声来衡量对尾部电刺激的疼痛反应阈值。结果显示，PGE1、PGE2、PGE2α、cAMP和二丁酰cAMP会减弱上述脑啡肽类似物的作用。与cAMP不同，cGMP在这方面没有活性。在所研究的离子（钙、锂、铷和铯）中，铯表现出最活跃的作用。它阻止了疼痛反应阈值的升高，并缩短了镇痛持续时间。锂对脑啡肽诱导的镇痛没有拮抗作用。将这些结果与先前获得的关于所研究物质与吗啡拮抗作用的数据进行比较，表明在阿片类药物和阿片样物质作用调节机制方面存在相似性。同时，锂不能拮抗脑啡肽类似物以及存在吗啡拮抗作用这一情况表明，外源性镇痛药和脑啡肽在离子调节机制方面的相似性还不够充分。
