The structure-activity relationship of Dmt-NH-X on opioid receptor affinity

摘要

2',6'-DimethyItyrosine(Dmt)has enhancement effects of both receptor affinity and functional bioactivity in vitro and in vivo by utilization in terms of Tyr in opioid peptide.For example,the replacement with Dmt of Tyr in H-Tyr-Pro-NH_2 increased mu-opioid receptor(MOR)affinity 630-fold,and in the case of H-Tyr-Tic-OH,delta-opioid receptor affinity(DOR)was increased 8700-fold.These results promoted us to examine the opiate activity of Dmt itself.