scholarly journals Chronic Ethanol Consumption in Rats Produces Opioid Antinociceptive Tolerance through Inhibition of Mu Opioid Receptor Endocytosis

PLoS ONE ◽  
2011 ◽  
Vol 6 (5) ◽  
pp. e19372 ◽  
Author(s):  
Li He ◽  
Jennifer L. Whistler
Keyword(s):  
Opioid Receptor ◽  
Ethanol Consumption ◽  
Mu Opioid Receptor ◽  
Chronic Ethanol ◽  
Mu Opioid ◽  
Receptor Endocytosis ◽  
Chronic Ethanol Consumption ◽  
Antinociceptive Tolerance

scholarly journals Convallatoxin enhance the ligand-induced mu-opioid receptor endocytosis and attenuate morphine antinociceptive tolerance in mice

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Po-Kuan Chao ◽  
Hsiao-Fu Chang ◽  
Li-Chin Ou ◽  
Jian-Ying Chuang ◽  
Pin-Tse Lee ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Mu Opioid Receptor ◽  
Mu Opioid ◽  
Receptor Endocytosis ◽  
Antinociceptive Tolerance

scholarly journals Role of mu opioid receptor endocytosis in the beneficial and side‐effects of prolonged opioid use

2012 ◽  
Vol 26 (S1) ◽  
Author(s):  
Jennifer Lynne Whistler ◽  
Amy Chang Berger ◽  
Anuradha Madhavan ◽  
Johan Enquist ◽  
Li He ◽  
...  
Keyword(s):  
Side Effects ◽  
Opioid Receptor ◽  
Mu Opioid Receptor ◽  
Opioid Use ◽  
Mu Opioid ◽  
Receptor Endocytosis

scholarly journals Drug discovery to counteract antinociceptive tolerance with mu-opioid receptor endocytosis

2017 ◽  
Author(s):  
Po-Kuan Chao ◽  
Yi-Yu Ke ◽  
Hsiao-Fu Chang ◽  
Yi-Han Huang ◽  
Li-Chin Ou ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
High Throughput Screening ◽  
Adaptor Protein ◽  
Morphine Tolerance ◽  
Mu Opioid Receptor ◽  
Chronic Morphine ◽  
Mu Opioid ◽  
Thermal Pain ◽  
Antinociceptive Tolerance ◽  
Highly Correlated

AbstractMorphine antinociceptive tolerance is highly correlated with its poor ability to promote mu-opioid– receptor (MOR) endocytosis. Our objective was to discover a novel positive allosteric modulator of MOR to enhance morphine-induced MOR endocytosis. We used high-throughput screening to identify several cardiotonic steroids as positive allosteric modulators of morphine-induced MOR endocytosis having high potency and efficacy, independently of Na+/K+-ATPase inhibition. Convallatoxin was found to enhance morphine-induced MOR endocytosis through an adaptor protein 2/clathrin-dependent mechanism without regulating G protein- or β-arrestin-mediated pathways. Both F243 and I292 residues of MOR were essential to the effect of convallatoxin on MOR endocytosis. Co-treatment with chronic morphine and convallatoxin reduced morphine tolerance in animal models of acute thermal pain and chronic inflammatory pain. Acute convallatoxin administration reversed morphine tolerance in morphine-tolerant mice. These findings suggest that cardiotonic steroids are potentially therapeutic for morphine side effects and open a new avenue for the study of MOR trafficking.

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