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

…, M Hirabuki, A Ambo, H Ouchi, Y Yamamoto

Index: Sasaki, Yusuke; Hirabuki, Mariko; Ambo, Akihiro; Ouchi, Hidekazu; Yamamoto, Yutaka Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 3 p. 327 - 329

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Citation Number: 15

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′-dimethyltyrosine1, d-Dmp4] Enk was found to be an antagonist toward μ and δ opioid receptors with pA2 values of 6.90 and 5.57, respectively.