Chichenkov O N, Sumbatian N V, Riabtseva O N, Korshunova G A, Shorr V A
Farmakol Toksikol. 1988 Sep-Oct;51(5):17-20.
In search of selective ligands of opioid receptors there was synthetized a number of shortened dermorphin analogues containing nucleic amino acid substituents in positions 4 and 5 and also nucleic amino acid analogues of enkephalins. All synthetized analogues of enkephalins and dermorphin possess opioid activity revealed on preparations of the guinea pig ileum and the mouse vas deferens. Among the obtained analogues there were detected analogues exhibiting a high delta-agonistic (Tyr-D-Ala-Phe-Gly-DL-Tal-OH) or mu-agonistic (Tyr-D-Phe-Gly-Tal-Leu-OH) activity comparable with that for standard preparations DADLE and DAGO.
为了寻找阿片受体的选择性配体,合成了许多在4位和5位含有核酸氨基酸取代基的缩短型德莫啡类似物以及脑啡肽的核酸氨基酸类似物。所有合成的脑啡肽和德莫啡类似物在豚鼠回肠和小鼠输精管制剂上均表现出阿片活性。在所获得的类似物中,检测到了具有高δ激动活性(酪氨酸-D-丙氨酸-苯丙氨酸-甘氨酸-DL-塔罗氨酸-OH)或μ激动活性(酪氨酸-D-苯丙氨酸-甘氨酸-塔罗氨酸-亮氨酸-OH)的类似物,其活性与标准制剂DADLE和DAGO相当。