Enkephalin analogues with 2′,6′-dimethylphenylalanine replacing phenylalanine in position 4

Bioorganic & Medicinal Chemistry Letters
2001.0

Abstract

Four Leu-enkephalin (Enk) analogues containing 2',6'-dimethyphenylalanine (Dmp) in position 4 were prepared and tested for their receptor binding and biological activities. Among the analogues prepared, [2', 6'-dimethyltyrosine, D-Dmp4]Enk was found to be an antagonist toward mu and delta opioid receptors with pA2 values of 6.90 and 5.57, respectively.

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