262616-19-3Relevant articles and documents
Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists
Page,McClory,Mischki,Schmidt,Butterworth,St-Onge,Labarre,Payza,Brown
, p. 167 - 170 (2000)
A series of Dmt-Tic analogues with substitution on the Tic aromatic ring has been synthesized and evaluated for opioid receptor affinity and activation. Incorporation of large hydrophobic groups at position 7 of Tic did not greatly alter the δ opioid receptor binding affinities of the dipeptides whereas substitution at position 6 substantially diminished their affinity. These modified Dmt-Tic peptides showed binding affinities as low as 2.5 nM with up to 500-fold selectivity for the δ versus μ opioid receptor and proved to be δ receptor antagonists.
