Buprenorphine has potent kappa opioid receptor antagonist activity
Abstract
Buprenorphine was studied for its effects on urinary output to determine if it was an agonist, partial agonist, or antagonist at the kappa receptor. Buprenorphine was a potent antagonist of bremazocine-induced urination and had no kappa agonist activity. Thus, the high affinity that buprenorphine has for the kappa receptor results in potent kappa receptor antagonist activity in vivo.
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Buprenorphine blocks the action of kappa agonists, and functional kappa antagonism has been proposed from animal models to function therapeutically as an antidepressant compound in humans.
“In addition, BUP has also been shown to block the action of k agonists [56] and a functional k antagonism has been proposed on the basis of the results derived by animal models to function therapeutically as an antidepressant compound in humans [24]”
From The Efficacy of Buprenorphine in Major Depression, Treatment-Resistant Depression and Suicidal Behavior: A Systematic Review (2018) · cites this paper as [56]
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- Authors
- LEANDER, J.
- Affiliations
- Eli Lilly (United States) (US)
- Corresponding author
- LEANDER, J
- ORCID
- LEANDER, J
- Venue
- Neuropharmacology
- Publisher
- Elsevier BV
- Published
- 1987-09
- Volume
- 26
- Issue
- 9
- Pages
- 1445-1447
- ISSN
- 0028-3908 (ISSN-L)
- OpenAlex
- W2146835843
- Cited by
- 140
- References
- 8
- Citations by year
- 2025: 3 · 2024: 3 · 2023: 2 · 2022: 6 · 2021: 2 · 2020: 3 · 2019: 2 · 2018: 13 · 2017: 1 · 2016: 3 · 2015: 1 · 2014: 9 · 2013: 2 · 2012: 5
- FWCI
- 0.69
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Neuropharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Keywords
- buprenorphine, kappa opioid receptor, receptor antagonism, partial agonist activity, bremazocine, urine output, opioid receptor affinity
- MeSH terms
- Animals, Benzomorphans, Buprenorphine, Diuresis, Drug Combinations, Male, Naltrexone, Rats, Inbred Strains, Receptors, Opioid, Rats
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