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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Analgesics, Opioid / chemistry*
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Analgesics, Opioid / metabolism*
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Animals
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Binding Sites
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Guinea Pigs
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Male
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Mice
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Oligopeptides / chemistry*
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Oligopeptides / metabolism*
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Rats
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Rats, Wistar
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Receptors, Opioid, delta / metabolism
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Structure-Activity Relationship
Substances
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Analgesics, Opioid
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Oligopeptides
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Receptors, Opioid, delta
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endomorphin 2