Putative Kappa Opioid Heteromers As Targets for Developing Analgesics Free of Adverse Effects

@inproceedings{Naour2014PutativeKO,
  title={Putative Kappa Opioid Heteromers
As Targets for Developing Analgesics Free of Adverse Effects},
  author={Morgan Le Naour and Mary M. Lunzer and Michael D. Powers and Alexander E. Kalyuzhny and Michael A. Benneyworth and Mark J Thomas and Philip S. Portoghese},
  booktitle={Journal of medicinal chemistry},
  year={2014}
}
It is now generally recognized that upon activation by an agonist, β-arrestin associates with G protein-coupled receptors and acts as a scaffold in creating a diverse signaling network that could lead to adverse effects. As an approach to reducing side effects associated with κ opioid agonists, a series of β-naltrexamides 3-10 was synthesized in an effort to selectively target putative κ opioid heteromers without recruiting β-arrestin upon activation. The most potent derivative 3 (INTA… CONTINUE READING

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