Development of 5-Substituted N-Methylmorphinan-6-ones as Potent Opioid Analgesics with Improved Side-Effect Profile
المؤلفون المشاركون
Spetea, Mariana
Schmidhammer, Helmut
المصدر
International Journal of Medicinal Chemistry
العدد
المجلد 2012، العدد 2012 (31 ديسمبر/كانون الأول 2012)، ص ص. 1-10، 10ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2012-06-17
دولة النشر
مصر
عدد الصفحات
10
التخصصات الرئيسية
الملخص 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.
نمط استشهاد جمعية علماء النفس الأمريكية (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
نمط استشهاد الجمعية الأمريكية للغات الحديثة (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
نمط استشهاد الجمعية الطبية الأمريكية (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
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-454607
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
تقوم هذه الخدمة بالتحقق من التشابه أو الانتحال في الأبحاث والمقالات العلمية والأطروحات الجامعية والكتب والأبحاث باللغة العربية، وتحديد درجة التشابه أو أصالة الأعمال البحثية وحماية ملكيتها الفكرية. تعرف اكثر