Design and Synthesis of Highly Specific and Selective Enkephalin Analog Containing S-Npys-Cysteine for δ Opioid Receptors
Design and Synthesis of Highly Specific and Selective Enkephalin Analog Containing S-Npys-Cysteine for δ Opioid Receptors
复制标题
用于δ阿片受体的高度特异性和选择性的含有S-Npys-半胱氨酸的脑啡肽类似物的设计和合成
DOI：
10.1246/cl.1992.1259
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发表时间：
1992
影响因子：
1.6
通讯作者：
Y. Shimohigashi
中科院分区：
文献类型：
--
作者：
R. Matsueda;T. Yasunaga;H. Kodama;M. Kondo;T. Costa;Y. Shimohigashi
为了寻找阿片受体中可能的硫醇基团，合成了1、5或6位含有S-(3-硝基-2-吡啶磺基)半胱氨酸的脑啡肽类似物。在放射配基受体分析和生物测定中，[D-丙氨酸，亮氨酸]脑啡酰-半胱氨酸对δ的亲和力和选择性高于μ受体，并证明其通过二硫键与δ受体发生共价结合。
Enkephalin analogs containing S-(3-nitro-2-pyridinesulfenyl)cysteine at positions of 1,5, or 6 were synthesized for searching possible thiol groups in the opioid receptors. In the radio-ligand receptor assay and biological assays, [D-Ala2, Leu5]enkephalyl-Cys(Npys)6 exhibited a very high affinity and selectivity for δ over μ receptors, and its covalent attachment to δ receptors through the disulfide bonding was evidenced.