Biological properties of Phe(o)-opioid peptide analogues.
Biological properties of new analogues, which represent Phe(o)-propeptides of a variety of opioid peptides, are described. All Phe(o)-opioid analogues expressed both receptor binding affinities and in vitro biological activities at least at the level of the primary opioid peptides. Surprisingly, some of the propeptides expressed slightly higher activity than the primary opioid peptides. Nevertheless, no significant shift in receptor selectivity was observed, which indicate that these Phe(o)-analogues undoubtedly are propeptides. The possible role of membrane proteolytic enzymes associated with opioid receptors in transformation of propeptides is discussed.
Lipkowski
A W
AW
Department of Chemistry, University of Arizona, Tucson 85721, USA.
Misicka
A
A
Hosohata
K
K
Davis
P
P
Yamamura
H I
HI
Porreca
F
F
Hruby
V J
VJ
D000595:Amino Acid Sequence; D000701:Analgesics, Opioid / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001681:Biological Assay; D004795:Enzyme Stability; D020128:Inhibitory Concentration 50; D018847:Opioid Peptides / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D011355:Prodrugs / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D017465:Receptors, Opioid, delta / Q000378:metabolism; D017450:Receptors, Opioid, mu / Q000378:metabolism
D000701:Analgesics, Opioid; D018847:Opioid Peptides; D011355:Prodrugs; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D010649:Phenylalanine