Effect of chronic treatment of ohmefentanyl stereoisomers on cyclic AMP formation in Sf9 insect cells expressing human μ-opioid receptors

Z, Liu; He, Yu; Jin, Wen-Qiao; Chen, Xinjian; Shen, Qing; Chi, Zhi-Qiang

doi:10.1016/j.lfs.2003.10.027

Cited by 7 publications

(3 citation statements)

References 22 publications

(30 reference statements)

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“…Data mentioned above showed that F9202, F9204, DHE, and morphine exhibited different abilities to stimulate the binding of [ 35 S]GTPγS to receptors, suppress adenylyl cyclase activity and induce MORs internalization. Additionally, there is also evidence showing that these compounds display great differences in their roles in developing physical and psychological dependence [28][29][30][31][32][33] and in producing cAMP overshoot [34] . To further test the relation- (one-way ANOVA, Tukey post tests).…”

Section: Methodsmentioning

confidence: 99%

Paradoxical relationship between RAVE (relative activity versus endocytosis) values of several opioid receptor agonists and their liability to cause dependence

et al. 2010

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Aim: To examine the relationship between the RAVE (relative activity versus endocytosis) values of opiate agonists and their dependence liability by studying several potent analgesics with special profiles in the development of physical and psychological dependence. Methods: The effects of (-)-cis-(3R,4S,2′R) ohmefentanyl (F9202), (+)-cis-(3R,4S,2′S) ohmefentanyl (F9204), dihydroetorphine (DHE) and morphine on [35 S]GTPγS binding, forskolin-stimulated cAMP accumulation, and receptor internalization were studied in CHO cells stably expressing HA-tagged μ-opioid receptors (CHO-HA-MOR). cAMP overshoot in response to the withdrawal of these compound treatments was also tested. Results: All four agonists exhibited the same rank order of activity in stimulation of [35 S]GTPγS binding, inhibition of adenylyl cyclase (AC) and induction of receptor internalization: DHE>F9204>F9202>morphine. Based on these findings and the previous in vivo analgesic data obtained from our and other laboratories, the RAVE values of the four agonists were calculated. The rank order of RAVE values was morphine>F9202>F9204>DHE. For the induction of cAMP overshoot, the rank order was F9202≥morphine>F9204≥DHE. Conclusion: Taken in combination with previous findings of these compounds' liability to develop dependence, the present study suggests that the agonist with the highest RAVE value seems to have a relatively greater liability to develop psychological dependence relative to the agonist with the lowest RAVE value. However, the RAVE values of these agonists are not correlated with their probability of developing physical dependence or inducing cAMP overshoot, a cellular hallmark of dependence.

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Section: Methodsmentioning

confidence: 99%

Paradoxical relationship between RAVE (relative activity versus endocytosis) values of several opioid receptor agonists and their liability to cause dependence

et al. 2010

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“…To determine the number of adverse event reports for each opioid, we extracted the report counts from the reaction table (see Table 1). To selectively extract opioids, we examined target drugs based on their µ-opioid receptor affinity, as reported in previous studies [42,[52][53][54][55][56][57][58][59]. We selected 11 opioids, which are µ-opioid receptor agonists used in Japan, including morphine, fentanyl, oxycodone, codeine, dihydrocodeine, hydromorphone, methadone, tapentadol, pethidine, loperamide, and remifentanil.…”

Section: Data Table Creationmentioning

confidence: 99%

Analysis of Opioid-Related Adverse Events in Japan Using FAERS Database

Hirai,

Uesawa

2023

Pharmaceuticals

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Adverse events associated with opioid use in palliative care have been extensively studied. However, predicting the occurrence of adverse events based on the specific opioid used remains difficult. This study aimed to comprehensively analyze the adverse events related to µ-opioid receptor stimulation of opioids approved in Japan and investigate the tendencies of adverse event occurrence among different opioids. We utilized the FDA Adverse Event Reporting System database to extract reported adverse events for opioids approved in Japan. Cluster analysis was performed on reporting odds ratios (RORs) of adverse event names among opioids to visualize relationships between opioids and adverse events, facilitating a comparative study of their classifications. We calculated the RORs of adverse events for the target opioids. Cluster analysis based on these RORs resulted in five broad clusters based on the reported adverse events: i.e., strong opioids, weak opioids, loperamide, tapentadol, and remifentanil. This study provides a comprehensive classification of the association between μ-opioid-receptor-stimulating opioids and adverse events.

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“…To selectively extract opioids, we examined target drugs based on their µ receptor affinity, as reported in previous studies [43,[52][53][54][55][56][57][58][59]. We selected 11 opioids, which are µ receptor agonists used in Japan, including morphine, fentanyl, oxycodone, codeine, dihydrocodeine, hydromorphone, methadone, tapentadol, pethidine, loperamide, and remifentanil.…”

Section: Data Table Creationmentioning

confidence: 99%

Analysis of Opioid-Related Adverse Events in Japan

Hirai,

Uesawa

2023

Preprint

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Adverse events associated with opioid use in palliative care have been extensively studied. However, predicting the occurrence of adverse events based on the specific opioid used remains unclear. This study aimed to comprehensively analyze the adverse events caused by µ receptor stimulation of opioids approved in Japan and investigate the tendencies of adverse event occur-rence among different opioids.We utilized the FDA Adverse Event Reporting System (FAERS) database to extract reported adverse events of opioids approved in Japan. Cluster analysis was performed on reporting odds ratios (RORs) of adverse event names among opioids to visualize relationships between opioids and adverse events, facilitating a comparative study of their clas-sifications.We calculated the RORs of adverse events for the target opioids. Based on these RORs, we performed a cluster analysis, which resulted in the classification of 11 target opioids into five distinct groups. we were able to comprehensively compare and examine the relationships between opioids and adverse events. This analysis helps in understanding and managing the risks and benefits of each drug in palliative care settings. By analyzing relationships between opioids and adverse events, clinicians can make informed decisions about opioid selection, dosage, and monitoring to maximize patient safety and comfort.

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Effect of chronic treatment of ohmefentanyl stereoisomers on cyclic AMP formation in Sf9 insect cells expressing human μ-opioid receptors

Cited by 7 publications

References 22 publications

Paradoxical relationship between RAVE (relative activity versus endocytosis) values of several opioid receptor agonists and their liability to cause dependence

Paradoxical relationship between RAVE (relative activity versus endocytosis) values of several opioid receptor agonists and their liability to cause dependence

Analysis of Opioid-Related Adverse Events in Japan Using FAERS Database

Analysis of Opioid-Related Adverse Events in Japan

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