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Being a disabling symptom of many medical conditions, effective pain control is one of the most important therapeutic priorities. Morphine and other opioid drugs produce analgesia primarily through μ opioid (MOP) receptors, which mediate beneficial but also the non-beneficial actions. Appropriate identification of novel opioid analgesics may reduce complications and improve patient compliance. It was reported that hydrazones, oximes, carbazones and semicarbazone derivatives of morphinan-6-ones, e.g. dihydromorphinone or oxymorphone, exhibit high affinity at the MOP receptor . Since most of these structures show high antinociceptive potency while having less pronounced side effects, it remains a promising task to convert the carbonyl group of morphinan-6-ones into various functionalities. In this study, we aimed to investigate the effect of the replacement of the 6-keto function with a 6-cyano group on in vitro and in vivo pharmacological profiles.
© 2011 Follia et al; licensee BioMed Central Ltd. This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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VCU Pharmacology and Toxicology Publications