Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.

@article{Li2007TransformationOM,
  title={Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.},
  author={Tingyou Li and Y. Jinsmaa and M. Nedachi and A. Miyazaki and Y. Tsuda and A. Ambo and Y. Sasaki and S. Bryant and E. Marczak and Q. Li and H. Swartzwelder and L. Lazarus and Y. Okada},
  journal={Bioorganic \& medicinal chemistry},
  year={2007},
  volume={15 3},
  pages={
          1237-51
        }
}
N-Allylation (-CH(2)-CHCH(2)) of [Dmt(1)]endomorphins yielded the following: (i) [N-allyl-Dmt(1)]endomorphin-2 (Dmt=2',6'-dimethyl-l-tyrosine) (12) and [N-allyl-Dmt(1)]endomorphin-1 (15) (K(i)mu=0.45 and 0.26nM, respectively) became mu-antagonists (pA(2)=8.59 and 8.18, respectively) with weak delta-antagonism (pA(2)=6.32 and 7.32, respectively); (ii) intracerebroventricularly administered 12 inhibited morphine-induced CNS-mediated antinociception in mice [AD(50) (0.148ng/mouse) was 16-fold more… Expand
Novel highly potent mu-opioid receptor antagonist based on endomorphin-2 structure.
[N-Allyl-Dmt1]-Endomorphins Are μ-Opioid Receptor Antagonists Lacking Inverse Agonist Properties
Developmental Potential for Endomorphin Opioidmimetic Drugs
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