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

Bart De Spiegeleer UGent, Sofie Stalmans UGent, Evelien Wynendaele UGent, Nathalie Bracke UGent, Mathieu Verbeken UGent, Kathelijne Peremans UGent, Ingeborgh Polis UGent and Christian Burvenich UGent (2012) JOURNAL OF PEPTIDE SCIENCE. 18(suppl. 1). p.S49-S49
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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author
organization
alternative title
Receptor and blood-brain barrier characterisation of opioid peptides in drug research & early development
year
type
conference
publication status
published
subject
in
JOURNAL OF PEPTIDE SCIENCE
J. Pept. Sci.
volume
18
issue
suppl. 1
pages
S49 - S49
conference name
32nd European Peptide Symposium
conference location
Athens, Greece
conference start
2012-09-02
conference end
2012-09-07
Web of Science type
Meeting Abstract
Web of Science id
000308091500085
JCR category
CHEMISTRY, ANALYTICAL
JCR impact factor
2.071 (2012)
JCR rank
35/74 (2012)
JCR quartile
2 (2012)
ISSN
1075-2617
language
English
UGent publication?
yes
classification
C3
additional info
uploaded document is presentation version
copyright statement
I have retained and own the full copyright for this publication
id
2998895
handle
http://hdl.handle.net/1854/LU-2998895
date created
2012-09-25 11:33:45
date last changed
2012-12-10 13:20:57
@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},
}

Chicago
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.
APA
De Spiegeleer, B., Stalmans, S., Wynendaele, E., Bracke, N., Verbeken, M., Peremans, K., Polis, I., et al. (2012). Receptor and blood-brain barrier characterisation of opioid peptides in drug research and early development. JOURNAL OF PEPTIDE SCIENCE (Vol. 18, pp. S49–S49). Presented at the 32nd European Peptide Symposium.
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. JOURNAL OF PEPTIDE SCIENCE. 2012. p. S49–S49.
MLA
De Spiegeleer, Bart, Sofie Stalmans, Evelien Wynendaele, et al. “Receptor and Blood-brain Barrier Characterisation of Opioid Peptides in Drug Research and Early Development.” Journal of Peptide Science. Vol. 18. 2012. S49–S49. Print.