scholarly journals Nalfurafine is a G-protein biased agonist having significantly greater bias at the human than rodent form of the kappa opioid receptor

2017 ◽  
Vol 32 ◽  
pp. 59-65 ◽  
Author(s):  
Selena S. Schattauer ◽  
Jamie R. Kuhar ◽  
Allisa Song ◽  
Charles Chavkin
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Biased Agonist

scholarly journals Asymmetric syntheses of (+)- and (–)-collybolide enable reevaluation of kappa-opioid receptor agonism

2022 ◽  
Author(s):  
Sophia Shevick ◽  
Stephan Freeman ◽  
Guanghu Tong ◽  
Robin Russo ◽  
Laura Bohn ◽  
...  
Keyword(s):  
Asymmetric Synthesis ◽  
Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Dense Core ◽  
Fungal Metabolite ◽  
Asymmetric Syntheses ◽  
Kappa Opioid ◽  
Biased Agonist

The fungal metabolite collybolide attracted attention as a non-nitrogenous, potent and biased agonist of the kappa-opioid receptor (KOR). Here we report a 10-step asymmetric synthesis of this complex sesquiterpene that enables facile access to either enantiomer. The synthesis relies on a diastereoselective α-benzoyloxylation to install the buried C6 benzoate and avoid irreversible translactonization of the congested, functionally dense core. Neither enantiomer, however, exhibited KOR agonism, indicating that collybolide has been mischaracterized as a KOR agonist and leaving open the basis for antipruritic effects in mice.

scholarly journals Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor

2017 ◽  
Vol 60 (7) ◽  
pp. 3070-3081 ◽  
Author(s):  
Zhong Zheng ◽  
Xi-Ping Huang ◽  
Thomas J. Mangano ◽  
Rodger Zou ◽  
Xin Chen ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Biased Agonist

scholarly journals Prolonged Kappa Opioid Receptor Phosphorylation Mediated by G-protein Receptor Kinase Underlies Sustained Analgesic Tolerance

2003 ◽  
Vol 279 (3) ◽  
pp. 1810-1818 ◽  
Author(s):  
Jay P. McLaughlin ◽  
Lisa C. Myers ◽  
Paul E. Zarek ◽  
Marc G. Caron ◽  
Robert J. Lefkowitz ◽  
...  
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Receptor Kinase ◽  
Kappa Opioid ◽  
Receptor Phosphorylation ◽  
Analgesic Tolerance ◽  
Protein Receptor
Sign in / Sign up

Export Citation Format

Share Document