Analytical characterization and comparison of the blood–brain barrier permeability of eight opioid peptides

Quantitative analysis of the opioid peptide DAMGO in rat plasma and microdialysis samples using liquid chromatography–tandem mass spectrometry

“…Worked-up samples could be stored during at least 24 h at 4 • C without degradation (data not shown). The metabolic stability of DAMGO in mouse plasma has previously been evaluated by Van Dorpe et al, resulting in a half-life of more than 2 h [7].…”

“…Quantification of DAMGO in biological matrixes has so far usually been carried out by radioactivity labeling the peptide [6,7]. Radioimmunoassay (RIA) is another common method for analysis of peptides.…”

Brainpeps: the blood–brain barrier peptide database

“…The apparent permeability is calculated as described with Eq. 10 (Gaillard et al 2001;Van Dorpe et al 2010).…”

“…These physiologically active molecules exert a variety of direct or indirect CNS effects, often showing hormesis, so that peptide drug development is a promising, but extraordinarily difficult challenge. Earlier, it was believed that peptides were not able to penetrate the BBB, but several studies disproved this criticism (Banks and Kastin 1996;Van Dorpe et al 2010, 2011. Although the sequence and other structural and genomic information can be retrieved from general protein/peptide databases like Swiss-Prot, experimental data on the BBB transport characteristics of peptides are, however, very scattered in the literature and hence, a need for a more formal approach was felt.…”

Structural modification and biological evaluation of Dmt1-DALDA analogues

“…[1] Structural modifications of the peptide have been performed in order to determine the role of the side chain charges, N-methylation of the Phe 3 -Lys 4 amide bond, and the influence of a benzazepine conformational constraint [2] at the level of Phe 3 .…”