dermorphin and 2-amino-4-phenylbutyric-acid

dermorphin has been researched along with 2-amino-4-phenylbutyric-acid* in 1 studies

Other Studies

1 other study(ies) available for dermorphin and 2-amino-4-phenylbutyric-acid

Article	Year
Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified with β3-homo-amino acids. Journal of peptide science : an official publication of the European Peptide Society, 2016, Volume: 22, Issue:4 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. Topics: Aminobutyrates; Animals; Binding, Competitive; Drug Stability; Humans; Inhibitory Concentration 50; Male; Opioid Peptides; Protein Binding; Rats; Rats, Wistar; Receptors, Opioid; Tyrosine	2016

Article

Year

Synthesis, binding affinities and metabolic stability of dimeric dermorphin analogs modified with β3-homo-amino acids.

Journal of peptide science : an official publication of the European Peptide Society, 2016, Volume: 22, Issue:4

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.

Topics: Aminobutyrates; Animals; Binding, Competitive; Drug Stability; Humans; Inhibitory Concentration 50; Male; Opioid Peptides; Protein Binding; Rats; Rats, Wistar; Receptors, Opioid; Tyrosine

2016