Developmental Potential for Endomorphin Opioidmimetic Drugs
المؤلفون المشاركون
Tsuda, Yuko
Salvadori, Severo
Lazarus, Lawrence H.
Okada, Yoshio
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
2012-06-15
دولة النشر
مصر
عدد الصفحات
10
التخصصات الرئيسية
الملخص EN
Morphine, which is agonist for μ-opioid receptors, has been used as an anti-pain drug for millennia.
The opiate antagonists, naloxone and naltrexone, derived from morphine, were employed for drug addiction and alcohol abuse.
However, these exogenous agonists and antagonists exhibit numerous and unacceptable side effects.
Of the endogenous opioid peptides, endomorphin(EM)-1 and endomorphin(EM)-2 with their high μ-receptor affinity and exceptionally high selectivity relative to δ- and κ-receptors in vitro and in vivo provided a sufficiently sequence-flexible entity in order to prepare opioid-based drugs.
We took advantage of this unique feature of the endomorphins by exchanging the N-terminal residue Tyr1 with 2′,6′-dimethyl-L-tyrosine (Dmt) to increase their stability and the spectrum of bioactivity.
We systematically altered specific residues of [Dmt1]EM-1 and [Dmt1]EM-2 to produce various analogues.
Of these analogues, [N-allyl-Dmt1]EM-1 (47) and [N-allyl-Dmt1]EM-2 (48) exhibited potent and selective antagonism to μ-receptors: they completely inhibited naloxone- and naltrexone-induced withdrawal from following acute morphine dependency in mice and reversed the alcohol-induced changes observed in sIPSC in hippocampal slices.
Overall, we developed novel and efficacious opioid drugs without deleterious side effects that were able to resist enzymatic degradation and were readily transported intact through epithelial membranes in the gastrointestinal tract and the blood-brain-barrier.
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Okada, Yoshio& Tsuda, Yuko& Salvadori, Severo& Lazarus, Lawrence H.. 2012. Developmental Potential for Endomorphin Opioidmimetic Drugs. International Journal of Medicinal Chemistry،Vol. 2012, no. 2012, pp.1-10.
https://search.emarefa.net/detail/BIM-492770
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Okada, Yoshio…[et al.]. Developmental Potential for Endomorphin Opioidmimetic Drugs. International Journal of Medicinal Chemistry No. 2012 (2012), pp.1-10.
https://search.emarefa.net/detail/BIM-492770
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Okada, Yoshio& Tsuda, Yuko& Salvadori, Severo& Lazarus, Lawrence H.. Developmental Potential for Endomorphin Opioidmimetic Drugs. International Journal of Medicinal Chemistry. 2012. Vol. 2012, no. 2012, pp.1-10.
https://search.emarefa.net/detail/BIM-492770
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-492770
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