Effect ofN-Alkyl andN-Alkenyl Substituents in Noroxymorphindole, 17-Substituted-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7:2‘,3‘-indolomorphinans, on Opioid Receptor Affinity, Selectivity, and Efficacy

2001 ◽  
Vol 44 (9) ◽  
pp. 1471-1474 ◽  
Author(s):  
Sherita McLamore ◽  
Thomas Ullrich ◽  
Richard B. Rothman ◽  
Heng Xu ◽  
Christina Dersch ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Affinity

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
Keyword(s):  
Opioid Receptor ◽  
Receptor Affinity ◽  
Ligand System

scholarly journals O6C-20-nor-SalA is a stable and potent KOR agonist

2017 ◽  
Author(s):  
Ryan Shenvi ◽  
Shun Hirasawa ◽  
Min Cho ◽  
Tarsis F. Brust ◽  
Jeremy J. Roach ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Medicinal Chemistry ◽  
Kappa Opioid Receptor ◽  
Salvinorin A ◽  
High Potency ◽  
Kappa Opioid ◽  
Receptor Affinity ◽  
Weak Bases ◽  
Selective Agonist

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>

Cyclic deltorphin analogues with high δ opioid receptor affinity and selectivity

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

scholarly journals Characterization of opioid receptor in cerebral ischemia (|): The variations of the receptor affinity and density

1988 ◽  
Vol 46 ◽  
pp. 50
Author(s):  
Tomohiko Iwai ◽  
Shuichiro Ohta ◽  
Masakatsu Nozaki ◽  
Kaito Tsurumi ◽  
Hiromu Yamada ◽  
...  
Keyword(s):  
Cerebral Ischemia ◽  
Opioid Receptor ◽  
Receptor Affinity

The Pharmacology of Opioids (DRAFT)

2018 ◽  
Author(s):  
Christopher Cavacuiti
Keyword(s):  
Adverse Effects ◽  
Opioid Receptor ◽  
Extended Release ◽  
Receptor Subtypes ◽  
Synthetic Method ◽  
Physiological Effects ◽  
Opioid Use ◽  
Receptor Affinity ◽  
Opioid Receptor Subtypes ◽  
Long Acting

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.

Synthesis and Opioid Receptor Affinity of a Series of 2,4-Diaryl-Substituted 3,7-Diazabicylononanones

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

ChemInform Abstract: Stereochemistry and Opioid Receptor Affinity of 2,4-Dipyridine-3,7-diazabicyclo[3.3.1]nonanones - Influence of the Substituent in Position N7.

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

Synthesis and Biological Evaluation of 14-Alkoxymorphinans. Part 19. Effect of 14-O-Benzylation on the Opioid Receptor Affinity and Antagonist Potency of Naltrexone.

ChemInform ◽  
2003 ◽  
Vol 34 (41) ◽  
Author(s):  
Falko Schuellner ◽  
Ruth Meditz ◽  
Roland Krassing ◽  
Guenther Morandell ◽  
Valery N. Kalinin ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Biological Evaluation ◽  
Receptor Affinity ◽  
Synthesis And Biological Evaluation
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