Abstract：
:Dermenkephalin (Tyr-D-Met-Phe-His-Leu-Met-AspNH2) is a highly potent and selective delta-opioid peptide isolated from frog skin. It was recently recognized that the C-terminus His4-Leu5-Met6-Asp7NH2 of dermenkephalin was responsible for the addressing of the peptide towards the delta-opioid receptor. In order to investigate the role played by residues 4, 5 and 6 in this 'delta address', we synthesized and evaluated 20 new analogues for their ability to displace tritiated ligands from mu- and delta-opioid sites. Results showed that position 4 of dermenkephalin contributes to delta selectivity independently of delta-opioid receptor binding by preventing a high affinity mu binding. Position 5 requires a hydrophobic side chain to enhance delta affinity. A high delta affinity was obtained with any amino acids introduced in position 6 suggesting that residue 6 serves as a neutral spacer. Thus, the main features responsible for the high delta-opioid selectivity of dermenkephalin are electrostatic repulsions with the mu-opioid receptor, additional hydrophobic interactions with the delta-opioid receptor and folding of the C-terminal domain.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Charpentier S,Sagan S,Naim M,Delfour A,Nicolas Pdoi
10.1016/0922-4106(94)90107-4subject
Has Abstractpub_date
1994-01-15 00:00:00pages
175-80issue
2eissn
0014-2999issn
1879-0712journal_volume
266pub_type
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