Opioid receptor affinity of multivalent ligand system consisting of polymerized liposome

2009 ◽  
Vol 48 (1) ◽  
pp. 95-101 ◽  
Author(s):  
SHOKO TETSUI ◽  
JINBAO ZHAO ◽  
SHUNSAKU KIMURA ◽  
YUKIO IMANISHI
2001 ◽  
Vol 44 (9) ◽  
pp. 1471-1474 ◽  
Author(s):  
Sherita McLamore ◽  
Thomas Ullrich ◽  
Richard B. Rothman ◽  
Heng Xu ◽  
Christina Dersch ◽  
...  

2017 ◽  
Author(s):  
Ryan Shenvi ◽  
Shun Hirasawa ◽  
Min Cho ◽  
Tarsis F. Brust ◽  
Jeremy J. Roach ◽  
...  

Salvinorin A (SalA) is a potent and selective agonist of the kappa-opioid receptor (KOR), but its instability has frustrated medicinal chemistry efforts. Treatment of SalA with weak bases like DBU leads to C8 epimerization with loss of receptor affinity and signaling potency. Here we show that replacement of C20 with H and replacement of O6 with CH2 stabilizes the SalA scaffold relative to its C8 epimer, so much so that epimerization is completely suppressed. This new compound, O6C-20-nor-SalA, retains high potency for agonism of KOR. <br>


Peptides ◽  
1994 ◽  
pp. 514-516 ◽  
Author(s):  
H. I. Mosberg ◽  
H. B. Kroona ◽  
J. R. Omnaas ◽  
K. Sobczyk-Kojiro ◽  
P. Bush ◽  
...  

1988 ◽  
Vol 46 ◽  
pp. 50
Author(s):  
Tomohiko Iwai ◽  
Shuichiro Ohta ◽  
Masakatsu Nozaki ◽  
Kaito Tsurumi ◽  
Hiromu Yamada ◽  
...  

Author(s):  
Christopher Cavacuiti

This chapter focuses on the attributes of and component medications within the class of opioids, emphasizing kinetics, dynamics, and therapeutic and adverse effects. To help patients make informed decisions about opioid use, the clinicians prescribing these medications must be able to explain when opioids are likely to help and when they are likely to do harm. Subclasses of opioids include phenanthrenes, benzomorphans, phenylpiperidines, and diphenylheptanes; examples are given of each, with respective utilities and limitations. A discussion then follows of pharmacodynamics, pharmacokinetics, opioid receptor affinity, metabolism, and drug interactions. Tables and figures amplifying the text include: opioid class by synthetic method (Table 8.1); common physiological effects by opioid receptor subtypes (Table 8.2); opioid activity (Table 8.3); and a listing of figures and tables located in Appendix B (opioid receptor affinity, respiratory depression with opioids, adverse effects, metabolism, pharmacogenetics, extended release/long-acting opioids, abuse deterrent formulations). A text box provides supplemental resources.


2000 ◽  
Vol 43 (20) ◽  
pp. 3746-3751 ◽  
Author(s):  
Tom Siener ◽  
Antonella Cambareri ◽  
Ulrich Kuhl ◽  
Werner Englberger ◽  
Michael Haurand ◽  
...  

ChemInform ◽  
2010 ◽  
Vol 33 (52) ◽  
pp. no-no
Author(s):  
A. Cambareri ◽  
D. P. Zlotos ◽  
U. Holzgrabe ◽  
W. Englberger ◽  
M. Haurand

ChemInform ◽  
2003 ◽  
Vol 34 (41) ◽  
Author(s):  
Falko Schuellner ◽  
Ruth Meditz ◽  
Roland Krassing ◽  
Guenther Morandell ◽  
Valery N. Kalinin ◽  
...  

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