Highly selective fluorescent analogue of the potent δ-opioid receptor antagonist Dmt-Tic
Highly selective fluorescent analogue of the potent δ-opioid receptor antagonist Dmt-Tic
复制标题
DOI：
10.1021/jm040128h
复制
发表时间：
2004-12-16
影响因子：
7.3
通讯作者：
Lazarus, LH
中科院分区：
文献类型：
--
作者：
Balboni, G;Salvadori, S;Lazarus, LH
通过将荧光素偶联到H-Dmt-Tic-Glu-NH 2衍生的荧光三肽探针被开发为以高亲和力（Ki = 0.035 nM）和选择性（Ki（mu）/Ki（delta）= 4371）与δ-阿片受体相互作用。它作为一种不可逆的δ-阿片受体拮抗剂，与NG 108 -15细胞的结合被标准的非肽δ-阿片受体拮抗剂纳曲吲哚阻断。这种探针应证明是有用的δ-阿片受体在组织中的分布和信号转导过程中的阿片肽的内化的研究。
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.