Agonist Activity of the delta-antagonists TIPP and TIPP-psi in cellular models expressing endogenous or transfected delta-opioid receptors.

@article{Martin2001AgonistAO,
  title={Agonist Activity of the delta-antagonists TIPP and TIPP-psi in cellular models expressing endogenous or transfected delta-opioid receptors.},
  author={Nancy A Martin and M T Terruso and Paul L. Prather},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2001},
  volume={298 1},
  pages={240-8}
}
A new class of highly selective delta-opioid receptor antagonists has been recently developed, termed the TIP(P) peptides. Two prototypical compounds in this class are TIPP (H-Tyr-Tic-Phe-Phe-OH) and a derivative, TIPP-psi (H-Tyr-Tic[CH2NH]-Phe-Phe-OH). Surprisingly, both TIPP and TIPP-psi demonstrated inhibition of adenylyl cyclase activity in GH3 cells transfected with delta-opioid receptors (GH3DORT), an effect normally observed by agonists. The agonist activity was delta-selective, because… CONTINUE READING

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