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Potent Biphalin Analogs with µ/δ Mixed Opioid Activity: In Vivo and In Vitro Biological Evaluation
Author(s) -
Costante Roberto,
Pinnen Francesco,
Stefanucci Azzurra,
Mollica Adriano
Publication year - 2014
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201300380
Subject(s) - chemistry , in vivo , in vitro , enkephalin , moiety , stereochemistry , opioid , hydrazine (antidepressant) , biological activity , opioid peptide , pharmacology , structure–activity relationship , chemical synthesis , biochemistry , receptor , biology , microbiology and biotechnology
Biphalin [(Tyr‐ D ‐Ala‐Gly‐Phe‐NH‐) 2 ] is an octapeptide with mixed μ/δ opioid activity. Its structure is based on two identical enkephalin‐like portions linked “tail‐to‐tail” by a hydrazine bridge. This study presents the synthesis and in vitro and in vivo bioassays of two biphalin analogs that do not present the toxicity connected with the presence of the hydrazine moiety and are able to elicit a higher antinociceptive effect than biphalin.