Brain uptake and the analgesic effect of oxytocin—its usefulness as an analgesic agent
Abstract
To establish the usefulness of oxytocin (OT) as an analgesic for women in delivery, the pharmacokinetic parameters and blood-brain barrier (BBB) permeability of [3H]OT were obtained using an intravenous injection technique or the internal carotid artery perfusion/capillary depletion (ICAP/CDM) method. Brain uptake of OT was similar to that of sucrose, plasma space marker, indicating that OT has a poor BBB permeability. Moreover, the analgesic effects of OT injected through the jugular vein on nociception were evaluated by the tail-flick method. The antinociceptive effects of OT injected at a dose of 0.2 mg/kg or 2 mg/kg were dose-dependent. In addition, the analgesic effects of OT on the CNS were unaffected by naloxone, a m-receptor antagonist. In a similar manner to the opioid system, OT may play a modulatory role in antinociception.
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The assessment of intravenous oxytocin effects is hampered because peripheral oxytocin is not readily transported across the blood-brain barrier.
“The assessment of respective effects of intravenous oxytocin (17) is hampered because peripheral oxytocin is not readily transported across the blood–brain barrier (18).”
From Oxytocin Reduces Reward-Driven Food Intake in Humans (2013) · cites this paper as [18]
Cites
Delivery of peptides and proteins through the blood–brain barrier
Bickel, U., Yoshikawa, T., & Pardridge, W. M. (2001) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(00)00139-3 · Cited by 482 · see citing works
Triguero, D., Buciak, J., & Pardridge, W. M. (1990) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.1990.tb04886.x · Cited by 463 · see citing works
Peptide Drug Delivery to the Brain
(1992) · Annals of Internal Medicine · doi:10.7326/0003-4819-116-9-783_2 · Cited by 311 · see citing works
Blood-Brain Barrier Restriction of Peptides and the Low Uptake of Enkephalins*
Cornford, E. M., Braun, L. D., Crane, P. D., & Oldendorf, W. H. (1978) · Endocrinology · doi:10.1210/endo-103-4-1297 · Cited by 220 · see citing works
Yang, J. (1994) · Spine · doi:10.1097/00007632-199404150-00001 · Cited by 157 · see citing works
A new extraction of arginine vasopressin from blood: The use of octadecasilyl-silica
Larochelle, F. T., North, W. G., & Stern, P. (1980) · Pflügers Archiv - European Journal of Physiology · doi:10.1007/bf00580849 · Cited by 145 · see citing works
Anti-nociceptive effects of oxytocin in rats and mice
Lundeberg, T., Uvnäs‐Moberg, K., Ågren, G., & BRUZELIUS, G. (1994) · Neuroscience Letters · doi:10.1016/0304-3940(94)90262-3 · Cited by 139 · see citing works
Houghten, R. A., Swann, R. W., & Li, C. H. (1980) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.77.8.4588 · Cited by 98 · see citing works
Terasaki, T., Hirai, K., Sato, H., et al. (1989) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)20727-3 · Cited by 87 · see citing works
Oxytocin reduces intravenous heroin self-administration in heroin-tolerant rats
Kovács, G. L., Borthaiser, Z., & Telegdy, G. (1985) · Life Sciences · doi:10.1016/0024-3205(85)90620-4 · Cited by 84 · see citing works
Yoshikawa, T., & Pardridge, W. M. (1992) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)10429-1 · Cited by 78 · see citing works
Kovács, G. L., Horváth, Z., Sarnyai, Z., FALUDI, M., & Telegdy, G. (1985) · Neuropharmacology · doi:10.1016/0028-3908(85)90026-7 · Cited by 76 · see citing works
Samii, A., Bickel, U., Stroth, U., & Pardridge, W. M. (1994) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.1994.267.1.e124 · Cited by 67 · see citing works
Transport of nutrients and hormones through the blood-brain barrier.
Pardridge, W. M. (1984) · PubMed · Cited by 55 · see citing works
Delivering Peptides to the Central Nervous System: Dilemmas and Strategies
Banks, W. A., Kastin, A. J., & Barrera, C. M. (1991) · Pharmaceutical Research · doi:10.1023/a:1015884603456 · Cited by 54 · see citing works
Delivery of peptides and proteins through the blood-brain barrier
Bickel, U., Yoshikawa, T., & Pardridge, W. M. (1993) · Advanced Drug Delivery Reviews · doi:10.1016/0169-409x(93)90048-9 · Cited by 47 · see citing works
Rabenstein, D. L., & Yeo, P. L. (1994) · The Journal of Organic Chemistry · doi:10.1021/jo00094a039 · Cited by 39 · see citing works
β-endorphin tolerance is inhibited by oxytocin
Kovács, G. L., & Telegdy, G. (1987) · Pharmacology Biochemistry and Behavior · doi:10.1016/0091-3057(87)90533-8 · Cited by 33 · see citing works
van de Heijning, B. J. M., den Herik, I. K.-V., Maigret, C., & Greidanus, T. B. V. W. (1991) · European Journal of Pharmacology · doi:10.1016/0014-2999(91)90518-u · Cited by 12 · see citing works
Bickel, U., Yamada, S., & Pardridge, W. M. (1994) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)39012-9 · Cited by 11 · see citing works
Kang, Y., & Kim, J.-M. (1999) · Archives of Pharmacal Research · doi:10.1007/bf02976541 · Cited by 7 · see citing works
Self-citationPeri‐Arterial Innervation within the Neurohypophysis
Saito, S., Hanley, D. F., Kidd, G. J., et al. (1993) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.1993.tb55589.x · Cited by 1 · see citing works
North, W. G. (1993) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.1993.tb55531.x · Cited by 1 · see citing works
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Oxytocin and vasopressin in the human brain: social neuropeptides for translational medicine
Meyer-Lindenberg, A., Domes, G., Kirsch, P., & Heinrichs, M. (2011) · Nature Reviews Neuroscience · doi:10.1038/nrn3044 · Cited by 1,688 · see citing works
Oxytocin, vasopressin, and human social behavior
Heinrichs, M., von Dawans, B., & Domes, G. (2009) · Frontiers in Neuroendocrinology · doi:10.1016/j.yfrne.2009.05.005 · Cited by 799 · see citing works
Oxytocin Reduces Reward-Driven Food Intake in Humans
Ott, V., Finlayson, G., Lehnert, H., Heitmann, B., Heinrichs, M., Born, J., & Hallschmid, M. (2013) · Diabetes · doi:10.2337/db13-0663 · Cited by 226 · see citing works
Juif, P.-E., & Poisbeau, P. (2013) · Pain · doi:10.1016/j.pain.2013.05.003 · Cited by 101 · see citing works
Prosocial effects of oxytocin in two mouse models of autism spectrum disorders
Teng, B. L., Nonneman, R. J., Agster, K. L., Nikolova, V. D., Davis, T. T., Riddick, N. V., Baker, L. K., Pedersen, C. A., Jarstfer, M. B., & Moy, S. S. (2013) · Neuropharmacology · doi:10.1016/j.neuropharm.2013.04.038 · Cited by 98 · see citing works
Ge, Y., Lundeberg, T., & Yu, L.-C. (2002) · Brain Research · doi:10.1016/s0006-8993(01)03346-7 · Cited by 79 · see citing works
Hobo, S., Hayashida, K.-I., & Eisenach, J. C. (2012) · Anesthesia & Analgesia · doi:10.1213/ane.0b013e31823b1bc8 · Cited by 52 · see citing works
Glucocorticoid-mediated effects of systemic oxytocin upon memory retrieval
de Oliveira, L. F., Camboim, C., Diehl, F., Consiglio, A. R., & Quillfeldt, J. A. (2007) · Neurobiology of Learning and Memory · doi:10.1016/j.nlm.2006.05.006 · Cited by 34 · see citing works
Lambert, B., Declerck, C. H., Boone, C., & Parizel, P. M. (2017) · Hormones and Behavior · doi:10.1016/j.yhbeh.2017.06.011 · Cited by 30 · see citing works
- Authors
- Kang, Y.-S., & Park, J.-H.
- Affiliations
- Sookmyung Women's University (KR)
- Corresponding author
- Kang, Young-Sook
- ORCID
- Kang, Young-Sook
- Venue
- Archives of Pharmacal Research
- Published
- 2000-08
- Volume
- 23
- Issue
- 4
- Pages
- 391-395
- ISSN
- 0253-6269 (ISSN-L)
- 1976-3786
- OpenAlex
- W1995510818
- Cited by
- 63
- References
- 23
- Citations by year
- 2026: 1 · 2025: 1 · 2024: 2 · 2023: 1 · 2022: 3 · 2021: 4 · 2020: 6 · 2019: 3 · 2018: 8 · 2017: 4 · 2016: 2 · 2015: 3 · 2014: 3 · 2013: 5 · 2012: 4
- FWCI
- 0.41
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Archives of Pharmacal Research (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Social Sciences › Psychology › Social Psychology › Neuroendocrine regulation and behavior
- Keywords
- oxytocin, analgesia, antinociception, blood-brain barrier permeability, brain uptake, labor pain, pharmacokinetics, intravenous administration, naloxone, mu-opioid receptor, nociception, tail-flick test
- MeSH terms
- Animals, Blood-Brain Barrier, Brain, Male, Oxytocin, Rats, Sprague-Dawley, Analgesics, Non-Narcotic, Rats
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