title: Structure-activity relationships of the dimeric analogues of endomorphin-2 with different lengths of spacers.
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.
authors.affiliation: Department of Bioengineering, Zhengzhou University, Zhengzhou 450001, China.
authors.forename: Yan-Feng
authors.initials: YF
authors.lastname: Gao
authors.forename: Ming-Xia
authors.initials: MX
authors.lastname: Zhai
authors.forename: Wei-Xia
authors.initials: WX
authors.lastname: Liu
authors.forename: Xin
authors.initials: X
authors.lastname: Liu
authors.forename: Ye
authors.initials: Y
authors.lastname: Yuan
authors.forename: Yuan-Ming
authors.initials: YM
authors.lastname: Qi
authors.forename: Rui
authors.initials: R
authors.lastname: Wang
mesh_terms: 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
chemical_list: D000701:Analgesics, Opioid; D009842:Oligopeptides; D017465:Receptors, Opioid, delta; C105294:endomorphin 2