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Rational design and synthesis of ligands that act with high affinity at both mu- & delta-opioid receptors

Friday, September 18, 2015 — Poster Session V

2:00 p.m. – 3:30 p.m.
FAES Terrace
NIDA
PHARM-4

Authors

  • PW DeMatteo
  • YS Lee
  • AR Jacobson
  • KC Rice

Abstract

Two compounds with nanomolar activity for mu- and elta-opioid receptors have been synthesized. The twelve-compound library from which they were discovered demonstrates structure-activity trends, which can be further applied in the rational design of other mu-delta opioid-targeting compounds. Many of the other compounds in the library have high affinity at the mu- and a few at the mu-, delta-, and kappa-opioid receptors. DFT calculations implicate a novel interaction with a residue within the opioid binding pocket that could be targeted in the design of high affinity and selective mu-delta ligands. Such compounds have been noted to have fewer side-effects than the morphine-like mu selective ligands.

Category: Molecular Pharmacology