Quantitative comparison of ohmefentanyl isomers induced conditioning place preference in mice

Guo, Gui-Wen; Z, Liu; Jin, Wen-Qiao; Zhang, Hongping; Chen, Xinjian; Zhu, Yu; Chi, Zhi-Qiang

doi:10.1016/s0024-3205(01)01030-x

Cited by 7 publications

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“…The results of the present study demonstrated that DHE had the lowest RAVE value, while morphine had the highest RAVE value. Likewise, F9204 and F9202 had lower RAVE values relative to morphine but displayed less psychological dependence than morphine [29] . These findings are consistent with the RAVE hypothesis that agonists with lower RAVE values are less likely to induce psychological dependence.…”

Section: Discussionmentioning

confidence: 92%

“…The rank order of the RAVE values was morphine>F9202>F9204>DHE. Accordingly, morphine displayed a greater liability to induce psychological dependence relative to the other three compounds [29] . However, based on the results from the present in vitro cAMP overshoot assay and our previous in vivo physical dependence comparison [28] , F9202 displayed an extraordinarily strong ability to induce physical and cAMP overshoot.…”

Section: Wwwchinapharcom Wang Yh Et Almentioning

confidence: 91%

“…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%

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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: Discussionmentioning

confidence: 92%

Section: Wwwchinapharcom Wang Yh Et Almentioning

confidence: 91%

Section: Methodsmentioning

confidence: 99%

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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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“…Subsequently, we studied the dependence potential of ohmefentanyl stereoisomers in mice and found that there was a stereo-structural difference among these isomers. Isomer F9202 displayed stronger dependence potential than F9204 although they had similar analgesic activity and similar affinity for A-opioid receptors (Guo et al, 2000(Guo et al, , 2001. The present study was designed to further investigate the binding affinity of six active isomers for A-opioid receptors in Sf9-A cells.…”

Section: Introductionmentioning

confidence: 99%

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

Jin

et al. 2004

Life Sciences

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Opioids and addiction: Emerging pharmaceutical strategies for reducing reward and opponent processes

Bryant¹,

Zaki²,

Carroll³

et al. 2005

Clinical Neuroscience Research

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Quantitative comparison of ohmefentanyl isomers induced conditioning place preference in mice

Cited by 7 publications

References 0 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

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

Opioids and addiction: Emerging pharmaceutical strategies for reducing reward and opponent processes

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