Basic Information
ID: ALA1130911
Journal: Bioorg Med Chem Lett
Title: Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.
Authors: Horikawa M, Shigeri Y, Yumoto N, Yoshikawa S, Nakajima T, Ohfune Y.
Abstract: Novel Leu-enkephalin (Leu-Enk) (1) analogs possessing various types of alpha-substituted serine instead of its glycine residue in the position 2 were synthesized via an efficient O,N-migration method. The binding characteristics of the synthetic analogs using Chinese hamster ovary (CHO) cells expressed cloned rat mu-, delta-, and kappa-receptors revealed that [(1R,2S)-Ahh2]Enk (7) was the most potent agonist of delta-opioid receptors among all the synthetic analogs tested, and was 10 times more potent than the native Leu-Enk.
CiteXplore: 9873480
DOI: 10.1016/s0960-894x(98)00349-7
Patent ID: ┄
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