Document Detail

Permeability of the blood-brain barrier to peptides: an approach to the development of therapeutically useful analogs.
MedLine Citation:
PMID:  1494505     Owner:  NLM     Status:  MEDLINE    
Peptides have been shown in both in vivo and in vitro systems to cross the blood-brain barrier (BBB) and so affect function on the side contralateral to their origin. Some peptides cross primarily by transmembrane diffusion, a nonsaturable mechanism largely dependent on the lipid solubility of the peptide. Other peptides are transported by saturable systems across the BBB. These transport systems can be in the CNS to blood direction, as in the cases of Tyr-MIF-1 and methionine enkephalin, in the blood to CNS direction, as in the case of peptide T, or bidirectional, as in the case of LHRH. Other factors that also affect the amount of peptide crossing the BBB include binding in blood, volume of distribution, enzymatic resistance, and half-time disappearance from the blood. An in vitro model of the BBB has been characterized and used to confirm that peptides can cross the BBB. Results with the model agree with those obtained in vivo and have been used to study the permeability of the BBB to peptides, the effect of peptides on BBB integrity, the cellular pathway peptides and proteins use to cross the BBB, and the ability of the BBB to degrade peptides. The in vivo and in vitro methods have been used together to develop halogenated enkephalin analogs that are enzymatically resistant, cross the BBB readily to accumulate in areas of the brain rich in opiate receptors, and are powerful analgesics.(ABSTRACT TRUNCATED AT 250 WORDS)
W A Banks; K L Audus; T P Davis
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.; Review    
Journal Detail:
Title:  Peptides     Volume:  13     ISSN:  0196-9781     ISO Abbreviation:  Peptides     Publication Date:    1992 Nov-Dec
Date Detail:
Created Date:  1993-03-09     Completed Date:  1993-03-09     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  8008690     Medline TA:  Peptides     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1289-94     Citation Subset:  IM    
Veterans Affairs Medical Center, New Orleans, LA 70146.
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MeSH Terms
Amino Acid Sequence
Blood-Brain Barrier / physiology*
Capillary Permeability / physiology*
Cells, Cultured
Molecular Sequence Data
Peptides / metabolism,  pharmacokinetics*
Grant Support
Reg. No./Substance:

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