Synthesis of stereoisomeric analogues of endomorphin-2, H-Tyr-Pro-Phe-Phe-NH(2), and examination of their opioid receptor binding activities and solution conformation.

@article{Okada2000SynthesisOS,
  title={Synthesis of stereoisomeric analogues of endomorphin-2, H-Tyr-Pro-Phe-Phe-NH(2), and examination of their opioid receptor binding activities and solution conformation.},
  author={Y. Okada and A. Fukumizu and M. Takahashi and Y. Shimizu and Y. Tsuda and T. Yokoi and S. Bryant and L. Lazarus},
  journal={Biochemical and biophysical research communications},
  year={2000},
  volume={276 1},
  pages={
          7-11
        }
}
All sixteen stereoisomeric analogues of endomorphin-2 (H-Tyr-Pro-Phe-Phe-NH(2)) were synthesized by Fmoc-strategy using solid phase methods. Although synthetic endomorphin-2 exhibited similar mu- and delta-opioid receptor-binding activity to the natural compound, endomorphin-2 analogues containing d-amino acid isomers exhibited lower interaction with mu-receptors depending on the particular combination. The data clearly indicated that the three dimensional structure of endomorphin-2 with the… Expand
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