[Dmt¹, d-1-Nal³]morphiceptin, a novel opioid peptide analog with high analgesic activity

详细信息	查看全文 | 推荐本文 |

• 作者：Jakub Fichna ; Jean-Claude do-Rego ; Nga N. Chung ; Jean Costentin ; Peter W. Schiller ; Anna Janecka
• 关键词：Biofortification ; Consumer acceptance ; Micronutrient malnutrition ; Mozambique
• 刊名：Peptides
• 出版年：2008
• 期刊代码：59_01969781
• 类别：neu
• 出版时间：April 2008
• 卷：29
• 期：4
• 页码：633-638
• 文件大小：502 K

摘要

The morphiceptin-derived peptide [Dmt¹, d-1-Nal³]morphiceptin, labeled μ-opioid receptor (MOP) with very high affinity and selectivity in the receptor binding assays. In the mouse hot plate test, [Dmt¹, d-1-Nal³]morphiceptin given intracerebroventricularly (i.c.v.) produced profound supraspinal analgesia, being approximately 100-fold more potent than the endogenous MOP receptor ligand, endomorphin-2. The antinociceptive effect of this new analog lasted up to 120 min. Thus, [Dmt¹, d-1-Nal³]morphiceptin is an interesting and extraordinarily potent analgesic, raising the possibility of novel approaches in the design of clinically useful drugs for pain treatment.