Functional selectivity of 6′-guanidinonaltrindole (6′-GNTI) at κ-opioid receptors in striatal neurons

Cullen L. Schmid, John M. Streicher, Chad E. Groer, Thomas A. Munro, Lei Zhou, Laura M. Bohn

Research output: Contribution to journalArticlepeer-review

73 Scopus citations

Abstract

Background: 6′-Guanidinonaltrindole (6′-GNTI) activates G protein coupling to κ-opioid receptors (KOR) without β-arrestin2 recruitment in transfected cells. Results: In striatal neurons, 6′-GNTI activates Akt but not ERK1/2; U69,593 activates both kinases. Conclusion: In neurons, U69,593-induced activation of ERK1/2 is β-arrestin2-dependent, whereas activation of Akt is G protein-mediated. Significance: Identification of KOR signaling pathways in endogenous systems will inform the development of KOR-directed medications.

Original languageEnglish (US)
Pages (from-to)22387-22398
Number of pages12
JournalJournal of Biological Chemistry
Volume288
Issue number31
DOIs
StatePublished - Aug 2 2013
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology

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