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Structure-activity relationships of the dimeric analogues of endomorphin-2 with different lengths of spacers
Yan-Feng Gao1, Ming-Xia Zhai, Wei-Xia Liu
1Department of Bioengineering, Zhengzhou University, Zhengzhou 450001, China.
Abstract:
In the present study, seven novel dimeric analogues of endomorphin-2 with longer spacers were designed and synthesized. Through dimerization, their affinity for delta-opioid receptor was mostly increased, especially the delta-opioid receptor preferred dimeric analogue, DEM(12). The results were confirmed by the in vitro bioassay. The structure-activity relationships were also discussed.
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