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Design, Synthesis, and Evaluation of Opioid Analogues with Non-Peptidic β-Turn Scaffold:  Enkephalin and Endomorphin Mimetics

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posted on 2002-03-03, 00:00 authored by Masakatsu Eguchi, Richard Y. W. Shen, J. Paul Shea, Min S. Lee, Michael Kahn
We have identified a μ-selective opioid receptor agonist without a cationic amino group in the molecule from libraries of bicyclic β-turn peptidomimetics. The biologically active conformation of the lead is proposed to mimic an endomorphin type III 4 → 1 β-turn conformation.

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