Abstract The synthesis and biological testing of analogues of Met-enkephalin, a recently discovered opioid peptide from mammalian brain, are described. Testing involved determination of affinity constants for an opiate receptor site and of analgesic potency in the tail-flick test in mouse. The effects on opioid activity of modifying various parts of the enkephalin molecule are discussed. Tyr-D-Ala-Gly-MePheMet (O)-ol 1 (FK 33-824), which ...
[Schneider, Paulo H.; Schrekker, Henri S.; Silveira, Claudio C.; Wessjohann, Ludger A.; Braga, Antonio L. European Journal of Organic Chemistry, 2004 , # 12 p. 2715 - 2722]