Immunohistochemical localization of the carboxy terminus of the novel mu opioid receptor splice variant MOR-IC within the human spinal cord

Neuroreport ◽  
2000 ◽  
Vol 11 (9) ◽  
pp. 1953-1957 ◽  
Author(s):  
Catherine Abbadie ◽  
S Humayun Gultekin ◽  
Gavril W. Pasternak
2014 ◽  
Vol 232 (4) ◽  
pp. 815-824 ◽  
Author(s):  
Ahmad A. Altarifi ◽  
Yunyun Yuan ◽  
Yan Zhang ◽  
Dana E. Selley ◽  
S. Stevens Negus

2021 ◽  
Vol 35 (S1) ◽  
Author(s):  
Miriam Barnett ◽  
Brian Knapp ◽  
Jean Bidlack

2003 ◽  
Vol 341 (2) ◽  
pp. 107-110 ◽  
Author(s):  
Qing-Ping Wang ◽  
James E. Zadina ◽  
Jian-Lian Guan ◽  
Seiji Shioda

2008 ◽  
Vol 9 (4) ◽  
pp. 1 ◽  
Author(s):  
P. Gris ◽  
P. Cheng ◽  
J. Gauthier ◽  
S. Shabalina ◽  
W. Maixner ◽  
...  

2019 ◽  
Author(s):  
Ricardo Rosas, Jr. ◽  
Xi-Ping Huang ◽  
Bryan L. Roth ◽  
Chris Dockendorff

The concept recently postulated by Stein and coworkers (Science 2017, 355, 966) that mu opioid receptor (MOR) agonists possessing amines with attenuated basicity show pH-dependent activity and can selectively act at damaged, low pH tissues has been additionally supported by in vitro studies reported here. We synthesized and tested analogs of fentanyl possessing one or two fluorine atoms at the beta position of the phenethylamine side chain, with additional fluorines optionally added to the benzene ring of the side chain. These compounds were synthesized in 1 to 3 steps from commercial building blocks. The novel bis-fluorinated analog RR-49 showed superior pH sensitivity, with full efficacy relative to DAMGO, but with 19-fold higher potency (EC<sub>50</sub>) in a MOR cAMP assay at pH 6.5 versus 7.4. Such compounds hold significant promise as analgesics for inflammatory pain with reduced abuse potential.


Sign in / Sign up

Export Citation Format

Share Document