J Recept Signal Transduct Res. 1999 Jan-Jul;19(1-4):573-88.

Subtleties of structure-agonist versus antagonist relationships of opioid peptides and peptidomimetics.

Schiller PW, Weltrowska G, Schmidt R, Berezowska I, Nguyen TM, Lemieux C, Chung NN, Carpenter KA, Wilkes BC.

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Laboratory of Chemical Biology and Peptide Research, Clinical Research Institute of Montreal, Que., Canada.

Abstract

The development of novel delta opioid antagonists and delta opioid agonists structurally derived from the prototype delta antagonist TIPP (H-Tyr-Tic-Phe-Phe-OH), is reviewed. Both delta antagonists and delta agonists with extraordinary potency and unprecedented delta receptor selectivity were discovered. Some of them are already widely used as pharmacological tools and are also of interest as potential therapeutic agents for use in analgesia. The results of the performed structure-activity studies revealed that the delta antagonist versus delta agonist behavior of this class of compounds depended on very subtle structural differences in diverse locations of the molecule. These observations can be best explained with a receptor model involving a number of different inactive and active receptor conformations.

PMID:: 10071786; [PubMed - indexed for MEDLINE]

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