Topochemical analysis of morphiceptin and dermorphin bioactivities.

  title={Topochemical analysis of morphiceptin and dermorphin bioactivities.},
  author={Takeshi Yamazaki and Seonggu Ro and Murray J Goodman},
  journal={Biochemical and biophysical research communications},
  volume={181 2},
To elucidate the topochemical requirements for bioactivities of morphiceptin (Tyr-Pro-Phe-Pro-NH2) and dermorphin (Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2), we have designed and synthesized two diastereomers Tyr-(L and D)-(NMe)Ala-Phe-D-Pro-NH2. Both the analogs display high activities in the guinea pig ileum assay. The only difference in the composition of these two diastereomers arises from the chirality at residue 2. The high mu-receptor activities are attributed to structures where the Tyr1-L… CONTINUE READING

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