(+)-and (−)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/σ1 antagonist properties and antinociceptive effects
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- 关键词：Sigma-1 receptor ; (+)-Phenazocine ; (&minus ; )-Phenazocine ; Mechanical antinociception ; Bifunctional ligand ; Opioid
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2017
- 出版时间：5 January 2017
- 年：2017
- 卷：125
- 期：Complete
- 页码：603-610
- 全文大小：1245 K
- 卷排序：125
文摘
We investigated the σ1 pharmacological profile of Phenazocine enantiomers. We improved the plethora of information about the analgesic activity of Phenazocine. We employed phenytoin as σ1 receptor positive allosteric modulator. PRE-084 unmasked σ1 antagonistic component of (+)- and (−)- phenazocine. (+) and (−)-Phenazocine display σ1 antagonist activity and opioid analgesia.