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Development of 5-Substituted N-Methylmorphinan-6-ones as Potent Opioid Analgesics with Improved Side-Effect Profile
Joint Authors
Spetea, Mariana
Schmidhammer, Helmut
Source
International Journal of Medicinal Chemistry
Issue
Vol. 2012, Issue 2012 (31 Dec. 2012), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2012-06-17
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
One of the most important functions of the opioid system is the control of pain.
Among the three main opioid receptor classes (μ, δ, κ), the μ (MOR) is the main type targeted for pharmacotherapy of pain.
Opioid analgesics such as morphine, oxycodone and fentanyl are agonists at the MOR and are the mainstay for the treatment of moderate-to-severe pain.
However, adverse effects related to opioid use are severe and often lead to early discontinuation and inadequate analgesia.
The development of more effective and safer medications for the management of pain still remains a major direction in pharmaceutical research.
Chemical approaches towards the identification of novel MOR analgesics with reduced side effects include structural modifications of 14-alkoxy-N-methylmorphinan-6-ones in key positions that are important for binding, selectivity, potency, and efficacy at opioid receptors.
This paper describes a representative strategy to improve the therapeutic usefulness of opioid analgesics from the morphinan class of drugs by targeting position 5.
The focus is on chemical and biological studies and structure-activity relationships of this series of ligands.
We report on 14-alkoxymorphinan-6-ones having a methyl and benzyl group at position 5 as strong opioid antinociceptive agents with reduced propensity to cause undesired effects compared to morphine although interacting selectively with MORs.
American Psychological Association (APA)
Schmidhammer, Helmut& Spetea, Mariana. 2012. Development of 5-Substituted N-Methylmorphinan-6-ones as Potent Opioid Analgesics with Improved Side-Effect Profile. International Journal of Medicinal Chemistry،Vol. 2012, no. 2012, pp.1-10.
https://search.emarefa.net/detail/BIM-454607
Modern Language Association (MLA)
Schmidhammer, Helmut& Spetea, Mariana. Development of 5-Substituted N-Methylmorphinan-6-ones as Potent Opioid Analgesics with Improved Side-Effect Profile. International Journal of Medicinal Chemistry No. 2012 (2012), pp.1-10.
https://search.emarefa.net/detail/BIM-454607
American Medical Association (AMA)
Schmidhammer, Helmut& Spetea, Mariana. Development of 5-Substituted N-Methylmorphinan-6-ones as Potent Opioid Analgesics with Improved Side-Effect Profile. International Journal of Medicinal Chemistry. 2012. Vol. 2012, no. 2012, pp.1-10.
https://search.emarefa.net/detail/BIM-454607
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-454607