scholarly journals Kappa opioid receptor binding in major depression: A pilot study

Synapse ◽  
2018 ◽  
Vol 72 (9) ◽  
pp. e22042 ◽  
Author(s):  
Jeffrey M. Miller ◽  
Francesca Zanderigo ◽  
Priya D. Purushothaman ◽  
Christine DeLorenzo ◽  
Harry Rubin-Falcone ◽  
...  
Keyword(s):  
Pilot Study ◽  
Major Depression ◽  
Opioid Receptor ◽  
Receptor Binding ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Opioid Receptor Binding

The mu1, mu2, delta, kappa opioid receptor binding profiles of methadone stereoisomers and morphine

Life Sciences ◽  
1994 ◽  
Vol 56 (2) ◽  
pp. 45-50 ◽  
Author(s):  
Kim Kristensen ◽  
Christian Broen Christensen ◽  
Lona L. Christrup
Keyword(s):  
Opioid Receptor ◽  
Receptor Binding ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Opioid Receptor Binding

scholarly journals A DFT and Semiempirical Model-Based Study of Opioid Receptor Affinity and Selectivity in a Group of Molecules with a Morphine Structural Core

2012 ◽  
Vol 2012 ◽  
pp. 1-16 ◽  
Author(s):  
Tamara Bruna-Larenas ◽  
Juan S. Gómez-Jeria
Keyword(s):  
Binding Affinity ◽  
Opioid Receptor ◽  
Receptor Binding ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Receptor Binding Affinity ◽  
Reactivity Indices ◽  
Model Based ◽  
Local Reactivity ◽  
Opioid Receptor Binding

We report the results of a search for model-based relationships between mu, delta, and kappa opioid receptor binding affinity and molecular structure for a group of molecules having in common a morphine structural core. The wave functions and local reactivity indices were obtained at the ZINDO/1 and B3LYP/6-31 levels of theory for comparison. New developments in the expression for the drug-receptor interaction energy expression allowed several local atomic reactivity indices to be included, such as local electronic chemical potential, local hardness, and local electrophilicity. These indices, together with a new proposal for the ordering of the independent variables, were incorporated in the statistical study. We found and discussed several statistically significant relationships for mu, delta, and kappa opioid receptor binding affinity at both levels of theory. Some of the new local reactivity indices incorporated in the theory appear in several equations for the first time in the history of model-based equations. Interaction pharmacophores were generated for mu, delta, and kappa receptors. We discuss possible differences regulating binding and selectivity in opioid receptor subtypes. This study, contrarily to the statistically backed ones, is able to provide a microscopic insight of the mechanisms involved in the binding process.

scholarly journals In Major Depression, Increased Serum Dynorphin and Kappa Opioid Receptor Levels are Positively Associated with Mu Opioid Receptor Levels and Immune Activation and Are Attenuated by Nicotine Dependence

2019 ◽  
Author(s):  
Hussein Al-Hakeim ◽  
Suhaer Al-Fadhel ◽  
Arafat Hussein Al-Dujaili ◽  
Michael Maes
Keyword(s):  
Major Depression ◽  
Nicotine Dependence ◽  
Opioid Receptor ◽  
Immune Activation ◽  
Kappa Opioid Receptor ◽  
Receiver Operating Curve ◽  
Kappa Opioid ◽  
Mu Opioid ◽  
Beta Endorphin ◽  
Opioid Systems

Background: There is now evidence that immune and opioid systems show functional reciprocal relationships and that both systems may participate in the pathophysiology of major depression (MDD). Objective: The present study was carried out to delineate differences between MDD patients and healthy controls in dynorphin and kappa opioid receptor (KORs) in association with levels of β-endorphins and mu opioid receptors (MORs), interleukin-6 (IL-6) and IL-10. Method: The present study recruited 60 drug-free male participants with MDD aged 24-70 year and 30 age-matched healthy males as control group and measured serum levels of dynorphin, KOR, β-endorphin, MOR, IL-6 and IL-10. Results: Serum dynorphin, KOR, β-endorphin and MOR are significantly increased in MDD as compared with controls. The increases in the dynorphin/KOR system and β-endorhin/MOR system are significantly intercorrelated and are both strongly associated with increased IL-6 and IL-10 levels. Dynorphin, β-endorphin, KOR and both cytokines showed a good diagnostic performance for MDD versus controls, whereby both opioid peptides and cytokines show a bootstrapped (n=2000) area under the receiver operating curve of 0.972. KOR and the dynorphin/KOR system are both significantly decreased in depressed subjects with comorbid nicotine dependence. Conclusion: Our findings suggest that in MDD, immune activation is associated with a simultaneous activation of dynorphin/KOR and β-endorhin/MOR signaling and that these opioid systems may participate in the pathophysiology of depression by a) exerting immune regulatory activities attenuating the primary immune response; and b) modulating reward responses and mood as well as emotional and behavioral responses to stress.

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