Penetration of neurohypophyseal hormones from plasma into cerebrospinal fluid (CSF): Half-times of disappearance of these neuropeptides from CSF
Abstract
The penetration of neurohypophyseal peptides after peripheral administration into the cerebrospinal fluid (CSF) was studied in freely moving rats. In addition, the clearance of these peptides from CSF was investigated. Increased concentrations of vasopressin (AVP) in CSF were detectable 2 min after s.c. injection of 5.0 micrograms of this peptide. Peak concentration was reached at 5 min after administration and this level declined slowly over the next hour. Administration of 5.0 micrograms oxytocin (OXT) s.c. or i.v. resulted in increased OXT levels in CSF within 10 min after application. After 60 min a significant elevation of OXT in CSF was no longer present. These data reveal that approximately 0.002% of the peripherally applied amount of AVP or OXT reached the central nervous system at 10 min after injection. AVP (2.5 ng) and OXT (5.0 ng) applied into one of the lateral brain ventricles reached the cisternal cavity within 2 min after administration. Both neuropeptides were cleared from the CSF with terminal half-times of 26 and 19 min for AVP and OXT, respectively. The present data demonstrate that neurohypophyseal hormones do cross the blood-brain barrier in amounts obviously sufficient to induce central actions.
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After it enters the bloodstream, oxytocin does not cross the blood-brain barrier in significant quantities.
“After entering the blood, oxytocin rapidly penetrates extravascular fluid, but does not cross the blood-brain barrier in appreciable amounts.”
From Intranasal Oxytocin: Myths and Delusions (2016) · cites this paper as [10]
In rats given subcutaneous oxytocin, plasma levels rose about 500-fold while CSF levels rose only modestly, and only 0.002% of the dose reached the central nervous system by 10 minutes.
“The effectiveness of the blood-brain barrier for oxytocin was measured by Mens et al., who injected 5µg subcutaneously in rats, increasing plasma concentrations 500-fold to ~38,600pg/ml (10).Increases in CSF were modest; concentrations increased from ~40pg/ml to ~150pg/ml.The authors calculated that just 0.002% of the injected oxytocin had reached the CNS after 10min, when CSF concentrations were”
From Intranasal Oxytocin: Myths and Delusions (2016) · cites this paper as [10]
Evidence for CSF increases after intranasal oxytocin in humans is mixed.
“although mixed evidence has been observed in humans.80”
From Beyond the hype and hope: critical considerations for intranasal oxytocin research in autism spectrum disorder (2017) · cites this paper as [80]
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- Authors
- Mens, W. B. J., Witter, A., & Van Wimersma Greidanus, T. B.
- Affiliations
- Utrecht University (NL)
- Venue
- Brain Research
- Publisher
- Elsevier BV
- Published
- 1983-02
- Volume
- 262
- Issue
- 1
- Pages
- 143-149
- ISSN
- 0006-8993 (ISSN-L)
- OpenAlex
- W2062508009
- Cited by
- 360
- References
- 29
- Citations by year
- 2026: 6 · 2025: 11 · 2024: 14 · 2023: 14 · 2022: 20 · 2021: 28 · 2020: 24 · 2019: 11 · 2018: 28 · 2017: 16 · 2016: 16 · 2015: 21 · 2014: 18 · 2013: 14 · 2012: 5
- FWCI
- 12.43
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Brain Research (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Social Sciences › Psychology › Social Psychology › Neuroendocrine regulation and behavior
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Cerebrospinal fluid and hydrocephalus
- Life Sciences › Neuroscience › Neurology › Barrier Structure and Function Studies
- Keywords
- neurohypophyseal hormones, vasopressin, oxytocin, cerebrospinal fluid, blood-brain barrier penetration, peripheral administration, central nervous system action
- MeSH terms
- Animals, Arginine Vasopressin, Half-Life, Kinetics, Male, Oxytocin, Pituitary Hormones, Posterior, Rats, Inbred Strains, Rats
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