Abstract
Substitution of L-p-nitrophenylalanine for phenylalanine in position 4 of [D-Ala 2, Leu-NH 2 2]enkephalin analogues increased their affinity for μ-, δ- and κ-binding sites in guinea-pig brain, increased their potency to inhibit electrically evoked contractions of the guinea-pig ileum and mouse vas deferens, and increased their analgesic potency in the mouse tail flick test. Introduction of L-adamantylalanine, but not of L-neopentylglycine, in position 5 resulted in a loss activity.
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