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Receptor and blood-brain barrier characterisation of opioid peptides in drug research and early development

(2012) JOURNAL OF PEPTIDE SCIENCE. 18(suppl. 1). p.S49-S49
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Abstract
The penetration of the blood–brain barrier (BBB) combined with the receptor-subtype selectivity determines the medical activity of opioid peptides within the central nervous system (CNS). The opioid receptor-subtype selectivity can be assessed not only by the classic radio-ligand binding methods, but also by novel techniques such as SAW (surface acoustic wave) measuring binding kinetics. Pharmacokinetics include metabolic stability, brain influx and efflux characteristics, as well as brain capillary retention. Metabolic stability is evaluated by in vitro kinetic studies using different target tissues. When applying the in vivo mouse model, the influx transfer constant from serum into mouse brain is determined by multiple time regression, while the efflux kinetics are investigated with the intra-cerebroventricular injection technique. Furthermore, brain parenchyma-capillary cell distribution is evaluated by capillary depletion. Finally, the in vivo antinociceptive activity can be quantified in a mouse model. Since the evaluation of opioid peptides as potential therapeutic or diagnostic CNS agents requires the consideration of these opposing criteria, the CNS-functional drugability of opioid peptides is evaluated using a desirability criterion combining these different requirements. Information about the BBB behaviour of peptides, including the opioid peptides, are found in the database Brainpeps, which can also be used for QSPR.

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MLA
De Spiegeleer, Bart, et al. “Receptor and Blood-Brain Barrier Characterisation of Opioid Peptides in Drug Research and Early Development.” JOURNAL OF PEPTIDE SCIENCE, vol. 18, no. suppl. 1, 2012, pp. S49–S49.
APA
De Spiegeleer, B., Stalmans, S., Wynendaele, E., Bracke, N., Verbeken, M., Peremans, K., … Burvenich, C. (2012). Receptor and blood-brain barrier characterisation of opioid peptides in drug research and early development. JOURNAL OF PEPTIDE SCIENCE, 18(suppl. 1), S49–S49.
Chicago author-date
De Spiegeleer, Bart, Sofie Stalmans, Evelien Wynendaele, Nathalie Bracke, Mathieu Verbeken, Kathelijne Peremans, Ingeborgh Polis, and Christian Burvenich. 2012. “Receptor and Blood-Brain Barrier Characterisation of Opioid Peptides in Drug Research and Early Development.” In JOURNAL OF PEPTIDE SCIENCE, 18:S49–S49.
Chicago author-date (all authors)
De Spiegeleer, Bart, Sofie Stalmans, Evelien Wynendaele, Nathalie Bracke, Mathieu Verbeken, Kathelijne Peremans, Ingeborgh Polis, and Christian Burvenich. 2012. “Receptor and Blood-Brain Barrier Characterisation of Opioid Peptides in Drug Research and Early Development.” In JOURNAL OF PEPTIDE SCIENCE, 18:S49–S49.
Vancouver
1.
De Spiegeleer B, Stalmans S, Wynendaele E, Bracke N, Verbeken M, Peremans K, et al. Receptor and blood-brain barrier characterisation of opioid peptides in drug research and early development. In: JOURNAL OF PEPTIDE SCIENCE. 2012. p. S49–S49.
IEEE
[1]
B. De Spiegeleer et al., “Receptor and blood-brain barrier characterisation of opioid peptides in drug research and early development,” in JOURNAL OF PEPTIDE SCIENCE, Athens, Greece, 2012, vol. 18, no. suppl. 1, pp. S49–S49.
@inproceedings{2998895,
  abstract     = {{The penetration of the blood–brain barrier (BBB) combined with the receptor-subtype selectivity determines the medical activity of opioid peptides within the central nervous system (CNS). The opioid receptor-subtype selectivity can be assessed not only by the classic radio-ligand binding methods, but also by novel techniques such as SAW (surface acoustic wave) measuring binding kinetics. Pharmacokinetics include metabolic stability, brain influx and efflux characteristics, as well as brain capillary retention. Metabolic stability is evaluated by in vitro kinetic studies using different target tissues. When applying the in vivo mouse model, the influx transfer constant from serum into mouse brain is determined by multiple time regression, while the efflux kinetics are investigated with the intra-cerebroventricular injection technique. Furthermore, brain parenchyma-capillary cell distribution is evaluated by capillary depletion. Finally, the in vivo antinociceptive activity can be quantified in a mouse model.
Since the evaluation of opioid peptides as potential therapeutic or diagnostic CNS agents requires the consideration of these opposing criteria, the CNS-functional drugability of opioid peptides is evaluated using a desirability criterion combining these different requirements. Information about the BBB behaviour of peptides, including the opioid peptides, are found in the database Brainpeps, which can also be used for QSPR.}},
  author       = {{De Spiegeleer, Bart and Stalmans, Sofie and Wynendaele, Evelien and Bracke, Nathalie and Verbeken, Mathieu and Peremans, Kathelijne and Polis, Ingeborgh and Burvenich, Christian}},
  booktitle    = {{JOURNAL OF PEPTIDE SCIENCE}},
  issn         = {{1075-2617}},
  language     = {{eng}},
  location     = {{Athens, Greece}},
  number       = {{suppl. 1}},
  pages        = {{S49--S49}},
  title        = {{Receptor and blood-brain barrier characterisation of opioid peptides in drug research and early development}},
  volume       = {{18}},
  year         = {{2012}},
}

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