TOPOGRAPHIC MODEL OF DELTA-OPIOID SELECTIVE LIGANDS - DPLPE-DELTORPHIN HYBRID ANALOGS

There are attempts to correlate the topography of the bioactive struct ures of DPDPE and deltorphins, two delta active peptide families. One of the methods utilized by us is the hybridization of necessary elemen ts for bioactivity of these opioid peptide groups. We have found that a major point determining high activity of hybrid analogues is also th e chirality of the amino acid residue in position 5. Replacing D-Pen(S ) with L-Pen(S) resulted in dramatic increases in affinity for opioid delta receptors.