Highly selective fluorescent analogue of the potent δ-opioid receptor antagonist Dmt-Tic

被引：25

作者：

Balboni, G

Salvadori, S

Dal Piaz, A

Bortolotti, F

Argazzi, R

Negri, L

Lattanzi, R

Bryant, SD

Jinsmaa, Y

Lazarus, LH ^{[1
]}

机构：

[1] Univ Cagliari, Dept Toxicol, I-09126 Cagliari, Italy

[2] Univ Ferrara, Dept Chem, I-44100 Ferrara, Italy

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

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

[5] Univ Roma La Sapienza, Dept Human Physiol & Pharmacol Vittorio Erspamer, I-00185 Rome, Italy

[6] NIEHS, LCBRA, Med Chem Grp, Res Triangle Pk, NC 27709 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 26期

关键词：

D O I：

10.1021/jm040128h

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A fluorescent tripeptide probe derived by coupling fluorescein to H-Dmt-Tic-Glu-NH2 was developed to interact with delta-opioid receptors with high affinity (K-i = 0.035 nM) and selectivity (K-i(mu)/K-i(delta) = 4371). It acts as an irreversible delta-opioid receptor antagonist, and binding to NG108-15 cells is blocked by the standard nonpeptidic delta-opioid receptor antagonist naltrindole. This probe should prove useful in the study of the distribution of delta-opioid receptors in tissues and the internalization of opioid peptides during signal transduction.

引用

页码：6541 / 6546

页数：6

共 29 条

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