Studies on peptides. XCIV. Synthesis and activity of kyotorphin and its analogs.

Abstract
A dipeptide named kyotorphin, H-Tyr-Arg-OH, and its retro isomer were synthesized using NG-mesitylene-2-sulfonylarginine. Two corresponding stereoisomers containing D-Arg were synthesized. H-Tyr-D-Arg-OH had an analgesic effect 6 times higher than that of the corresponding L-isomer in mice.