Noribogaine is a G-protein biased κ-opioid receptor agonist
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- 作者：Emeline L. Mailleta ; emaillet@demerx.us" class="auth_mail" title="E-mail the corresponding author ; emailletlaure@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Nicolas Milona ; Mari D. Heghiniana ; James Fishbacka ; Stephan C. Schü ; rerb ; c ; Nandor Garamszegia ; Deborah C. Masha ; 1
- 关键词：Noribogaine ; Mu opioid receptor ; Kappa opioid receptor ; Biased agonist ; Functional selectivity ; Addiction ; Narcotic ; Analgesia ; G-protein pathway ; Beta-arrestin pathway ; Computational simulation ; Ibogaine ; 18-MC
- 刊名：Neuropharmacology
- 出版年：2015
- 出版时间：December 2015
- 年：2015
- 卷：99
- 期：Complete
- 页码：675-688
- 全文大小：2046 K
文摘
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The anti-addictive drug noribogaine was functionally characterized at the opioid receptors.
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Noribogaine is a G-protein biased kappa opioid agonist.
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Noribogaine is also a mu antagonist and a beta-arrestin biased kappa antagonist.
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The unique pharmacological profile of noribogaine may explain its atypical effects on the opioid system in vivo.