beta-casomorphins: Substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity

Authors
Longobardo, L Melck, D Siciliano, R Santini, A Di Marzo, V Cammarota, G
Citation
L. Longobardo et al., beta-casomorphins: Substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity, BIOORG MED, 10(11), 2000, pp. 1185-1188
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
11
Year of publication
2000
Pages
1185 - 1188
Database
ISI
SICI code
0960-894X(20000605)10:11<1185:BSOPWB>2.0.ZU;2-P
Abstract
Two analogues of bovine beta-casomorphin-7 and beta-casomorphin-5 containin g a beta-homo phenylalanine in substitution of the phenylalanine in positio n 3 were synthesised and tested for their mu-opioid receptor affinity. The modification enhanced the mu receptor affinity 5-fold in the case of modifi ed beta-CM-7 and 2-fold for modified beta-CM-5 when compared to the natural peptides. (C) 2000 Elsevier Science Ltd. All rights reserved.