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  • Title: Interaction of p-nitrophenylalanine enkephalins with mu-, delta- and kappa-subtypes of the opiate receptor.
    Author: Fauchère JL, Do KQ, Schwyzer R, Robson LE, Gillan MG, Paterson SJ, Kosterlitz HW.
    Journal: Eur J Pharmacol; 1982 Feb 05; 77(4):339-42. PubMed ID: 6277677.
    Abstract:
    Substitution of L-p-nitrophenylalanine for phenylalanine in position 4 of [D-Ala2, KLeu-NH2(5)]enkephalin analogues increased their affinity for mu-, delta- and kappa-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 of activity.
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