Abstract
Morphiceptin (Tyr-Pro-Phe-Pro-NH 2 ) and the potent analog PLO17 (Tyr-Pro-MePhe-D-Pro-NH 2 ) belong both to the family of μ-selective opioid compounds. Our previous work done on the synthesis and biological activity of glycosylated morphiceptins showed that the introduction of sugar moieties into such β-casomorphin substructure lead to less active or quite inactive analogs. As an extension of this investigation, we have further studied the ability of [Hyp 4 ] morphiceptin, and its galactosyl and glucosyl conjugates, to displace [ 3 H][D-Ala 2 , MePhe 4 , Gly-ol 5 ] enkephalin from its binding sites in homogenates of guinea pig brain. Results showed that the glucosyl derivative was able to displace with moderate affinity only a fraction of the binding defined by [ 3 H]DAMGO
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