213688-73-4Relevant academic research and scientific papers
Syntheses of potent LEU-enkephalin analogs possessing β-hydroxy-α,α- disubstituted-α-amino acid and their characterization to opioid receptors
Horikawa, Manabu,Shigeri, Yasushi,Yumoto, Noboru,Yoshikawa, Susumu,Nakajima, Terumi,Ohfune, Yasufumi
, p. 2027 - 2032 (1998)
Novel Leu-enkephalin (Leu-Enk) (1) analogs possessing various types of α-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 μ-, δ-, and κ-receptors revealed that [(1R,2S)- Ahh2]Enk (7) was the most potent agonist of δ-opioid receptors among all the synthetic analogs tested, and was 10 times more potent than the native Leu-Enk.
