From the potent and selective μ opioid receptor agonist H-Dmt-D-Arg-Phe-Lys-NH2 to the potent δ antagonist H-Dmt-Tic-Phe-Lys(Z)-OH

被引：5

作者：

Balboni, G ^{[1
]}

Cocco, MT

Salvadori, S

Romagnoli, R

Sasaki, Y

Okada, Y

Bryant, SD

Jinsmaa, Y

Lazarus, LH

机构：

[1] Univ Cagliari, Dept Toxicol, I-09124 Cagliari, Italy

[2] Univ Ferrara, Dept Pharmaceut Sci, I-44100 Ferrara, Italy

[3] Univ Ferrara, Ctr Biotechnol, I-44100 Ferrara, Italy

[4] Tohoku Pharmaceut Univ, Aoba Ku, Sendai, Miyagi 9818558, Japan

[5] Kobe Gakuin Univ, Fac Pharmaceut Sci, Dept Med Chem, Kobe, Hyogo 6512180, Japan

[6] Kobe Gakuin Univ, High Technol Res Ctr, Kobe, Hyogo 6512180, Japan

[7] NIEHS, Lab Pharmacol & Chem, Med Chem Grp, Res Triangle Pk, NC 27709 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 17期

关键词：

D O I：

10.1021/jm0504959

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

H-Dmt-D-Arg-Phe-Lys-NH2 ([Dmt(1)]DALDA) binds with high affinity and selectivity to the mu opioid receptor and is a potent and long-acting analgesic. Substitution of D-Arg in position 2 with Tic and masking of the lysine amine side chain by Z protection and of the C-terminal carboxylic function instead of the amide function transform a potent and selective mu agonist into a potent and selective delta antagonist H-Dmt-Tic-Phe-Lys(Z)-OH. Such a delta antagonist could be used as a pharmacological tool.

引用

页码：5608 / 5611

页数：4

共 23 条

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