Peptides readily penetrate the blood-brain barrier: Uptake of peptides by synaptosomes is passive

R. Greenberg, C. E. Whalley, F. Jourdikian, I. S. Mendelson, R. Walter, K. Nikolics, D. H. Coy, Andrew V Schally, A. J. Kastin

Research output: Contribution to journalArticle

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Abstract

The intracarotid artery quick injection technique of Oldendorf was utilized to determine the Brain Uptake Index (BUI) of radio-labeled peptides in comparison with 3H2 O or 14C-antipyrine as counterlabels. The normalized BUI values for 3H-MIF-I, 3H-α-MSH and 14C-AVP were 13.7, 9.6 and 13.0, respectively at 15 sec after injection consistent with their having readily penetrated the blood-brain barrier. The BUI values were similar, though somewhat increased, at 10 min postinjection consistent with their ready exit across the blood-brain barrier. At 15 sec after injection 0.5 ± 0.1%/g brain of the originally injected peptide label was recovered; and 0.1 ± 0.2%/g brain was recovered after 10 min. The label was distributed uniformly in the major brain regions at both times. However, the percentage of the originally injected label/g of pineal and pituitary gland tissue was 10-20 × increased as compared with the major brain regions as would be expected by their location outside the blood-brain barrier. The in vitro uptake of the radio-labeled peptides by synaptosomes prepared from the whole brain and the major brain regions was passive; it was not temperature dependent, nor was it Na+ dependent. However, the binding of the three peptides by the synaptosomes varied considerably: AVP>MSH>MIF : 50>5>1. The penetration of the blood-brain barrier by the three peptides is consistent with their having CNS effects.

Original languageEnglish
Pages (from-to)151-158
Number of pages8
JournalPharmacology, Biochemistry and Behavior
Volume5
Issue numberSUPPL. 1
DOIs
StatePublished - Jan 1 1976
Externally publishedYes

Fingerprint

Synaptosomes
Blood-Brain Barrier
Brain
Peptides
Melanocyte-Stimulating Hormones
Labels
Radio
Injections
MSH Release-Inhibiting Hormone
Antipyrine
Pineal Gland
Pituitary Gland
Arteries
Tissue
Temperature

Keywords

  • AVP
  • Blood-brain barrier
  • Brain uptake index
  • MIF-I
  • Passive uptake
  • Peptide binding
  • Peptides
  • Synaptosome uptake
  • α-MSH

ASJC Scopus subject areas

  • Biochemistry
  • Behavioral Neuroscience
  • Pharmacology

Cite this

Greenberg, R., Whalley, C. E., Jourdikian, F., Mendelson, I. S., Walter, R., Nikolics, K., ... Kastin, A. J. (1976). Peptides readily penetrate the blood-brain barrier: Uptake of peptides by synaptosomes is passive. Pharmacology, Biochemistry and Behavior, 5(SUPPL. 1), 151-158. https://doi.org/10.1016/0091-3057(76)90345-2

Peptides readily penetrate the blood-brain barrier : Uptake of peptides by synaptosomes is passive. / Greenberg, R.; Whalley, C. E.; Jourdikian, F.; Mendelson, I. S.; Walter, R.; Nikolics, K.; Coy, D. H.; Schally, Andrew V; Kastin, A. J.

In: Pharmacology, Biochemistry and Behavior, Vol. 5, No. SUPPL. 1, 01.01.1976, p. 151-158.

Research output: Contribution to journalArticle

Greenberg, R, Whalley, CE, Jourdikian, F, Mendelson, IS, Walter, R, Nikolics, K, Coy, DH, Schally, AV & Kastin, AJ 1976, 'Peptides readily penetrate the blood-brain barrier: Uptake of peptides by synaptosomes is passive', Pharmacology, Biochemistry and Behavior, vol. 5, no. SUPPL. 1, pp. 151-158. https://doi.org/10.1016/0091-3057(76)90345-2
Greenberg, R. ; Whalley, C. E. ; Jourdikian, F. ; Mendelson, I. S. ; Walter, R. ; Nikolics, K. ; Coy, D. H. ; Schally, Andrew V ; Kastin, A. J. / Peptides readily penetrate the blood-brain barrier : Uptake of peptides by synaptosomes is passive. In: Pharmacology, Biochemistry and Behavior. 1976 ; Vol. 5, No. SUPPL. 1. pp. 151-158.
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