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Bioorg Med Chem Lett. 2001 Feb 12;11(3):327-9.

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

Author information

1
Tohoku Pharmaceutical University, Sendai, Japan. ysasaki@tohoku-pharm.ac.jp

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.

PMID:
11212102
DOI:
10.1016/s0960-894x(00)00665-x
[Indexed for MEDLINE]

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