910132-89-7Relevant academic research and scientific papers
A novel cyclic enkephalin analogue with potent opioid antagonist activity
Weltrowska, Grazyna,Lu, Yixin,Lemieux, Carole,Chung, Nga N.,Schiller, Peter W.
, p. 4731 - 4733 (2004)
The synthesis and in vitro activity profile of a potent opioid peptide antagonist lacking an N-terminal amino group are described. 2′,6′- Dimethyl substitution of the Tyr1 residue in opioid agonist peptides and deletion of the N-terminal amino
Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists
Lu, Yixin,Lum, Tze Keong,Augustine, Yoon Wui Leow,Weltrowska, Grazyna,Nguyen, Thi M.-D.,Lemieux, Carole,Chung, Nga N.,Schiller, Peter W.
, p. 5382 - 5385 (2007/10/03)
3-(2,6-Dimethyl-4-carbamoylphenyl)propanoic acid (Dcp), a 2′,6′-dimethyltyrosine analogue containing a carbamoyl group in place of the hydroxyl function and lacking the amino group, was synthesized. The replacement of Tyr1 in an enkephalin analogue and in dynorphin A(1-11)-NH2 with Dcp resulted in the first opioid peptide-derived antagonists that do not contain a phenolic hydroxyl group at the 1-position residue. The cyclic peptide Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH 2 represents a novel, potent μ opioid antagonist.
