6′-Guanidinonaltrindole (6′-GNTI) Is a G Protein-biased κ-Opioid Receptor Agonist That Inhibits Arrestin Recruitment
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منابع مشابه
Noribogaine is a G-protein biased κ-opioid receptor agonist
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A high-throughput screening campaign was conducted to interrogate a 380,000+ small-molecule library for novel D2 dopamine receptor modulators using a calcium mobilization assay. Active agonist compounds from the primary screen were examined for orthogonal D2 dopamine receptor signaling activities including cAMP modulation and β-arrestin recruitment. Although the majority of the subsequently con...
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S Discovery and Characterization of a G Protein–Biased Agonist That Inhibits b-Arrestin Recruitment to the D2 Dopamine Receptor R. Benjamin Free, Lani S. Chun, Amy E. Moritz, Brittney N. Miller, Trevor B. Doyle, Jennie L. Conroy, Adrian Padron, Julie A. Meade, Jingbo Xiao, Xin Hu, Andrés E. Dulcey, Yang Han, Lihua Duan, Steve Titus, Melanie Bryant-Genevier, Elena Barnaeva, Marc Ferrer, Jonathan...
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The κ opioid receptor (κOR) is a member of G-protein-coupled receptors, and is considered as a promising drug target for treating neurological diseases. κOR selective 6'-GNTI was proved to be a G-protein biased agonist, whereas 5'-GNTI acts as an antagonist. To investigate the molecular mechanism of how these two ligands induce different behaviors of the receptor, we built two systems containin...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 2012
ISSN: 0021-9258
DOI: 10.1074/jbc.c112.387332