Long-term effects of neonatal handling on mu-opioid receptor levels in the brain of the offspring

2009 ◽  
Vol 51 (5) ◽  
pp. 439-449 ◽  
Author(s):  
Georgios Kiosterakis ◽  
Antonios Stamatakis ◽  
Anastasia Diamantopoulou ◽  
Maria Fameli ◽  
Fotini Stylianopoulou
2020 ◽  
pp. JN-RM-2380-20
Author(s):  
Lihua Sun ◽  
Jing Tang ◽  
Heidi Liljenbäck ◽  
Aake Honkaniemi ◽  
Jenni Virta ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5677
Author(s):  
Mariana Spetea ◽  
Helmut Schmidhammer

Adequate pain management, particularly chronic pain, remains a major challenge associated with modern-day medicine. Current pharmacotherapy offers unsatisfactory long-term solutions due to serious side effects related to the chronic administration of analgesic drugs. Morphine and structurally related derivatives (e.g., oxycodone, oxymorphone, buprenorphine) are highly effective opioid analgesics, mediating their effects via the activation of opioid receptors, with the mu-opioid receptor subtype as the primary molecular target. However, they also cause addiction and overdose deaths, which has led to a global opioid crisis in the last decades. Therefore, research efforts are needed to overcome the limitations of present pain therapies with the aim to improve treatment efficacy and to reduce complications. This review presents recent chemical and pharmacological advances on 14-oxygenated-N-methylmorphinan-6-ones, in the search of safer pain therapeutics. We focus on drug design strategies and structure–activity relationships on specific modifications in positions 5, 6, 14 and 17 on the morphinan skeleton, with the goal of aiding the discovery of opioid analgesics with more favorable pharmacological properties, potent analgesia and fewer undesirable effects. Targeted molecular modifications on the morphinan scaffold can afford novel opioids as bi- or multifunctional ligands targeting multiple opioid receptors, as attractive alternatives to mu-opioid receptor selective analgesics.


Cancers ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 134 ◽  
Author(s):  
Oscar Díaz-Cambronero ◽  
Guido Mazzinari ◽  
Francisco Giner ◽  
Amparo Belltall ◽  
Lola Ruiz-Boluda ◽  
...  

Preclinical evidence has shown increased expression of mu opioid receptor 1 (MOR-1) in colorectal cancer although its association with disease-free and overall survival (DFS and OS) has not been investigated. We hypothesized that MOR-1 was overexpressed in tumor samples compared to normal tissue and this was associated with decreased DFS and OS. We carried out a retrospective study assessing the association of MOR-1 tumor expression with long-term outcomes by immunohistochemistry in normal and tumor samples from 174 colorectal cancer patients. The primary endpoint was five years of DFS. Secondary endpoints were five years of OS, the difference in MOR-1 expression between normal and tumor tissue and the occurrence of postoperative complications. Multivariable Cox regression showed no significant association between MOR-1 expression and DFS (HR 0.791, 95% CI 0.603–1.039, p = 0.092). MOR-1 expression was higher in tumor tissue compared to non-tumor tissue. No associations were found between MOR-1 expression and OS or postoperative complications. These findings suggest that although MOR-1 is over-expressed in colorectal cancer samples there is no association to increased risk of recurrence or mortality. Future studies are warranted to elucidate the role of cancer stage, genetic polymorphism, and quantitative assessment of MOR-1 over-expression on long-term outcomes in colorectal cancer.


2018 ◽  
Vol 276 ◽  
pp. 41-45 ◽  
Author(s):  
Juho Joutsa ◽  
Henry K. Karlsson ◽  
Joonas Majuri ◽  
Pirjo Nuutila ◽  
Semi Helin ◽  
...  

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