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Restrict the search for
morphine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
BIX-02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2. Intrathecal injection of BIX-02188, a novel specific inhibitor of mitogen-activated protein kinases kinase 5 (MEK5), produced a dose- and time-dependent inhibition of the activation of spinal ERK5, without affecting activation of other MAPKs. Moreover, selective attenuation of spinal p-ERK5 expression by BIX-02188 could significantly relieve morphine withdrawal symptom, accompanying with the decreased phosphorylation of cAMP response-element binding protein (CREB) in the spinal cord. These findings suggested that activation of the ERK5 signaling pathway might contribute to morphine physical dependence and its specific pharmacological inhibitor BIX0-2188 could be a potential therapeutic choice for alleviation of morphine withdrawal symptoms in the future.
Morphinone is an oxidation product of morphine with weak agonistic activity toward mu opioid receptor. Morphinone is the intermediate when morphine is being converted to hydromorphone. Morphinone is toxic compound, subcutaneous administration of morphinone produced a reduction of hepatic non-protein sulfhydryl concentration. Glutathione or cysteine significantly decrease Morphinone toxicity.
