Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists.

@article{Claude1996MutationOA,
  title={Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists.},
  author={P A Claude and D R Wotta and Xiang H. F. Zhang and Paul L. Prather and Therese M McGinn and Lennart Erickson and Horace H. Loh and Ping-Yee Law},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={1996},
  volume={93 12},
  pages={5715-9}
}
The involvement of a conserved serine (Ser196 at the mu-, Ser177 at the delta-, and Ser187 at the kappa-opioid receptor) in receptor activation is demonstrated by site-directed mutagenesis. It was initially observed during our functional screening of a mu/delta-opioid chimeric receptor, mu delta2, that classical opioid antagonists such as naloxone, naltrexone, naltriben, and H-Tyr-Tic[psi,CH2NH]Phe-Phe-OH (TIPPpsi; Tic = 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) could inhibit forskolin… CONTINUE READING

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