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

Authors
Sasaki, Y Hirabuki, M Ambo, A Ouchi, H Yamamoto, Y
Citation
Y. Sasaki et al., Enkephalin analogues with 2 ',6 '-dimethylphenylalanine replacing phenylalanine in position 4, BIOORG MED, 11(3), 2001, pp. 327-329
Citations number
26
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
3
Year of publication
2001
Pages
327 - 329
Database
ISI
SICI code
0960-894X(20010212)11:3<327:EAW2''>2.0.ZU;2-G
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'-dimethvltyrosi ne(1), D-Dmp(4)]Enk was found to be an antagonist toward mu and delta opioi d receptors with pA(2) values of 6.90 and 5.57, respectively. (C) 2001 Else vier Science Ltd. All rights reserved.