Kharkevich D A, Sumbatyan N V, Topin A N, Chichenkov O N, Zaitsev S V, Korshunova G A
Department of Pharmacology, I.M. Sechenov Moscow Medical Academy, Russian Federation.
FEBS Lett. 1994 Sep 12;351(3):308-10. doi: 10.1016/0014-5793(94)00849-3.
Four new [D-MetO2]dermorphin tetrapeptides with substituted N- and C-terminal groups and a thymine-modified alanine residue at position 4 were prepared and tested for their activity. All analogues were found to be mu-opioid receptor ligands. Two of them, H-Tyr-D-MetO-Phe-TalNHR (R = H, Ad) displayed an extremely high mu-opioid receptor selectivity comparable with that of the most mu-selective agonists among opioid peptides.
制备了四种新型的[D-MetO2]皮啡肽四肽，其N端和C端基团被取代，且在第4位有一个胸腺嘧啶修饰的丙氨酸残基，并对其活性进行了测试。发现所有类似物均为μ-阿片受体配体。其中两种，即H-Tyr-D-MetO-Phe-TalNHR（R = H，Ad）表现出极高的μ-阿片受体选择性，可与阿片肽中最具μ选择性的激动剂相媲美。
