Structure–Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain

2013 ◽  
Vol 56 (20) ◽  
pp. 8019-8031 ◽  
Author(s):  
Xiao-Tao Chen ◽  
Philip Pitis ◽  
Guodong Liu ◽  
Catherine Yuan ◽  
Dimitar Gotchev ◽  
...  
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Severe Pain ◽  
Receptor Ligand ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Μ Opioid Receptor ◽  
Ethyl Amine

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Francesca Rosato ◽  
Monika Wozniak ◽  
Jeremy Blavier ◽  
Maëlle Charles ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptor ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
G Protein Coupled

A First‐in‐Human Clinical Study With TRV734, an Orally Bioavailable G‐Protein–Biased Ligand at the μ‐Opioid Receptor

2019 ◽  
Vol 9 (2) ◽  
pp. 256-266 ◽  
Author(s):  
Ian E. James ◽  
Franck Skobieranda ◽  
David G. Soergel ◽  
Kimberly A. Ramos ◽  
Dennis Ruff ◽  
...  
Keyword(s):  
Clinical Study ◽  
G Protein ◽  
Opioid Receptor ◽  
Μ Opioid Receptor ◽  
Orally Bioavailable ◽  
Human Clinical Study

scholarly journals A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal

2019 ◽  
Vol 45 (2) ◽  
pp. 416-425 ◽  
Author(s):  
Travis W. Grim ◽  
Cullen L. Schmid ◽  
Edward L. Stahl ◽  
Fani Pantouli ◽  
Jo-Hao Ho ◽  
...  
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Morphine Tolerance ◽  
Morphine Withdrawal ◽  
G Protein Signaling ◽  
Protein Signaling ◽  
Μ Opioid Receptor ◽  
Biased Agonist

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2020 ◽  
Vol 41 (12) ◽  
pp. 947-959 ◽  
Author(s):  
Alexander Gillis ◽  
Andrea Kliewer ◽  
Eamonn Kelly ◽  
Graeme Henderson ◽  
Macdonald J. Christie ◽  
...  
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Critical Assessment ◽  
Biased Agonism ◽  
Μ Opioid Receptor
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