Opioid ligands with extraordinarily high μ‐selectivity: Dermorphin tetrapeptides containing thymine‐modified alanine residues

FEBS Letters

Kharkevich, D.A.¹  Chichenkov, O.N.¹  Sumbatyan, N.V.²  Topin, A.N.²  Korshunova, G.A.²  Zaitsev, S.V.² 

[1]Department of Pharmacology, I.M. Sechenov Moscow Medical Academy, Moscow, Russian Federation

[2]A.N. Belozersky Institute of Physico-Chemical Biology and Chemistry Department, Moscow State University, Moscow, 119899, Russian Federation

关键词: Opioid;    μ-selective ligand;    Dermorphin analogue;    3-(Thyminyl-1)alanine;    Ad;    1-adamantyl;    DAGO;    H-Tyr-d-Ala-Gly-MePhe-Gly-ol;    DM/1-4/;    dermorphin tetrapeptide;    H-Tyr-d-Ala-Phe-Gly-NH2;    DSLET;    H-Tyr-d-Ser-Gly-Phe-Leu-Thr-OH;    GPI;    guinea-pig ileum;    MVD;    mouse vas deferens;    Tal;    3-(thyminyl-1)alanine;   

DOI  :  10.1016/0014-5793(94)00849-3

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 μ-opioid receptor ligands. Two of them, H-Tyr-d-MetO-Phe-TalNHR (R=H, Ad) displayed an extremely highu μ-opioid receptor selectivity comparable with that of the most μ-selective agonists among opioid peptides.

【 授权许可】

Unknown