Compounds > enkephalin--ala(2)-mephe(4)-gly(5)-

enkephalin--ala(2)-mephe(4)-gly(5)- and oxymorphindole

enkephalin--ala(2)-mephe(4)-gly(5)- has been researched along with oxymorphindole* in 1 studies

Other Studies

1 other study(ies) available for enkephalin--ala(2)-mephe(4)-gly(5)- and oxymorphindole

Article	Year
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles. Journal of medicinal chemistry, 2003, Apr-10, Volume: 46, Issue:8 The 14-amino analogue of oxymorphindole (OMI) was synthesized and found to possess delta-opioid binding affinity and selectivity similar to OMI. Substitution of the amino group with alkyl, arylalkyl, and acyl groups had relatively little effect on delta-affinity but delta-selectivity was reduced. In functional assays the 14-phenylacetylamino derivative 6d was a selective delta-agonist whereas the phenethylamino analogue 5d was a mu-agonist and low efficacy delta partial agonist that warrants further investigation as an analgesic with low tolerance and dependence. Topics: Analgesics, Opioid; Animals; Binding, Competitive; CHO Cells; Cricetinae; Morpholines; Radioligand Assay; Receptors, Opioid, delta; Receptors, Opioid, mu; Structure-Activity Relationship	2003

Article

Year

14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.

Journal of medicinal chemistry, 2003, Apr-10, Volume: 46, Issue:8

The 14-amino analogue of oxymorphindole (OMI) was synthesized and found to possess delta-opioid binding affinity and selectivity similar to OMI. Substitution of the amino group with alkyl, arylalkyl, and acyl groups had relatively little effect on delta-affinity but delta-selectivity was reduced. In functional assays the 14-phenylacetylamino derivative 6d was a selective delta-agonist whereas the phenethylamino analogue 5d was a mu-agonist and low efficacy delta partial agonist that warrants further investigation as an analgesic with low tolerance and dependence.

Topics: Analgesics, Opioid; Animals; Binding, Competitive; CHO Cells; Cricetinae; Morpholines; Radioligand Assay; Receptors, Opioid, delta; Receptors, Opioid, mu; Structure-Activity Relationship

2003