Structure-activity relationships of the dimeric analogues of endomorphin-2 with different lengths of spacers.
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.
Gao
Yan-Feng
YF
Department of Bioengineering, Zhengzhou University, Zhengzhou 450001, China.
Zhai
Ming-Xia
MX
Liu
Wei-Xia
WX
Liu
Xin
X
Yuan
Ye
Y
Qi
Yuan-Ming
YM
Wang
Rui
R
D000701:Analgesics, Opioid / Q000737:chemistry* / Q000378:metabolism*; D000818:Animals; D001665:Binding Sites; D006168:Guinea Pigs; D008297:Male; D051379:Mice; D009842:Oligopeptides / Q000737:chemistry* / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D017465:Receptors, Opioid, delta / Q000378:metabolism; D013329:Structure-Activity Relationship
D000701:Analgesics, Opioid; D009842:Oligopeptides; D017465:Receptors, Opioid, delta; C105294:endomorphin 2