| Literature DB >> 27028206 |
Oliwia Frączak1, Anika Lasota1, Dagmara Tymecka2, Piotr Kosson3, Adriana Muchowska3, Aleksandra Misicka2,3, Aleksandra Olma1.
Abstract
In this study, proteinogenic amino acids residues of dimeric dermorphin pentapeptides were replaced by the corresponding β(3)-homo-amino acids. The potency and selectivity of hybrid α/β dimeric dermorphin pentapeptides were evaluated by competetive receptor binding assay in the rat brain using [3H]DAMGO (a μ ligand) and [3H]DELT (a δ ligand). Tha analog containing β(3)-homo-Tyr in place of Tyr (Tyr-D-Ala-Phe-Gly-β(3)-homo-Tyr-NH-)2 showed good μ receptor affinity and selectivity (IC50 = 0.302, IC50 ratio μ/δ = 68) and enzymatic stability in human plasma.Entities:
Keywords: enzymatic stability in human plasma; hybrid α/β dimeric dermorphin pentapeptides; opioid receptors binding affinity; β3-homo-amino acids
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Year: 2016 PMID： 27028206 DOI： 10.1002/psc.2869
Source DB: PubMed Journal: J Pept Sci ISSN： 1075-2617 Impact factor: 1.905