|Title||Chiral Effect of a Phe Residue in Position 3 of the Dmt(1)-L(or D)-Tic(2) Analogues on Opioid Functional Activities.|
|Publication Type||Journal Article|
|Year of Publication||2013|
|Authors||Lee YSun, Qu HChang, Davis P, Ma S-W, Vardanyan R, Lai J, Porreca F, Hruby VJ|
|Journal||ACS Med Chem Lett|
|Date Published||2013 Jul 11|
In this letter, we describe a structure-activity relationships study, specifically related to the chirality of third amino acid residue in our H-Dmt-L(or D)-Tic analogues, of which C-terminus is attached to a piperidinyl moiety. Observed selectivities and functional activities of these analogues demonstrated that the chiralities of the second and third position residues are crucial for determining whether these ligands act as antagonists or agonists at the δ opioid receptor, but not at the μ opioid receptor.
|Alternate Journal||ACS Med Chem Lett|
|PubMed Central ID||PMC3956057|
|Grant List||R01 DA013449 / DA / NIDA NIH HHS / United States|
Chiral Effect of a Phe Residue in Position 3 of the Dmt(1)-L(or D)-Tic(2) Analogues on Opioid Functional Activities.
Faculty Member Reference:
Yeon Sun Lee
Frank Porreca, PhD