Synergistic combinations of the dual enkephalinase inhibitor PL265 given orally with various analgesic compounds acting on different targets, in a murine model of cancer-induced bone pain

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• 作者：Sara Gonzá ; lez-Rodrí ; guez^a ; ¹ ; Hervé ; Poras^b ; ¹ ; Luis Mené ; ndez^a ; Ana Lastra^a ; Tanja Ouimet^b ; Marie-Claude Fournié ; -Zaluski^b ; Bernard P. Roques^b ; ^c ; ^{bernard.roques@pharmaleads.com} ; Ana Baamonde^a
• 关键词：ACEA ; arachidonyl-2&prime ; -chloroethylamide ; AEA ; N-arachidonoylethanolamide ; anandamide ; APN ; aminopeptidase N ; BNI ; nor-binaltorphimine ; CCI ; chronic constrictive injury ; CYP ; cyprodime ; DENKI ; dual enkephalinase inhibitor ; DOR ; delta opioid receptor ; ENK ; enkephalin ; FAAH ; fatty acid amide hydrolase ; i.p. ; intraperitoneal ; KOR ; kappa opioid receptor ; MOR ; mu opioid receptor ; NEP ; neprilysin ; NTI ; naltrindole ; Nlx-Met ; naloxone methiodide ; UHP ; unilateral hot plate test ; p.o. ; per os ; s.c. ; su
• 刊名：Scandinavian Journal of Pain
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：14
• 期：Complete
• 页码：25-38
• 全文大小：1208 K
• 卷排序：14

文摘

Combination of DENKI with non-opioid analgesic drugs results in synergistic antihyperalgesic effects. Mechanism of action involves the direct activation of the enkephalinergic system. The multi-target based strategy allows the reduction of doses in the treatment of chronic pain.