Endomorphin-1 analogs containing alpha-methyl-beta-amino acids exhibit potent analgesic activity after peripheral administration
Endomorphin-1 analogs containing alpha-methyl-beta-amino acids exhibit potent analgesic activity after peripheral administration
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含有 α-甲基-β-氨基酸的 Endomorphin-1 类似物在外周给药后表现出有效的镇痛活性
DOI：
10.1039/c7ob01115f
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发表时间：
2017
影响因子：
3.2
通讯作者：
Wang R
中科院分区：
文献类型：
--
作者：
Wang Yuan;Yang Junxian;Liu Xin;Zhao Long;Yang Dongxu;Zhou Jingjing;Wang Dan;Mou Lingyun;Wang Rui;Wang R
本研究设计并合成了含有c端芳香α-甲基-β-氨基酸和n端天然酪氨酸或2,6-二甲基酪氨酸的内啡肽-1类似物。我们表明，与母体肽相比，这些类似物在静脉给药后表现出更好的生物活性和血脑屏障穿透性，并且诱导便秘和镇静的倾向低于吗啡。
This study describes the design and synthesis of endomorphin-1 analogs containing C-terminal aromatic α-methyl-β-amino acids and an N-terminal native tyrosine or 2,6-dimethyl-tyrosine. We show that, in comparison with the parent peptide, these analogs exhibit improved bioactivity and blood–brain barrier penetration after intravenous administration, and have a lower tendency to induce constipation and sedation than morphine.