The DOI matches its Crossref record; 8 of the 8 references it cites were found in a registry or an index.
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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“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]
Citations
Cites
Pharmacological characterization in vivo of the novel opiate, beta-funaltrexamine.
Ward, S. J., Portoghese, P. S., & Takemori, A. E. (1982) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)32972-1 · Cited by 301
A kappa opioid effect: increased urination in the rat.
Leander, J. D. (1983) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)33435-x · Cited by 225
Further study of kappa opioids on increased urination.
Leander, J. D. (1983) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)22031-6 · Cited by 97
Evidence that nalorphine, butorphanol and oxilorphan are partial agonists at a κ-opioid receptor
Leander, J. D. (1983) · European Journal of Pharmacology · doi:10.1016/0014-2999(83)90198-x · Cited by 69
Further demonstration of kappa opioid binding sites in the brain: evidence for heterogeneity.
Su, T. (1985) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)20058-1 · Cited by 63
Animal and molecular pharmacology of mixed agonist‐antagonist analgesic drugs.
Rance, M. J. (1979) · British Journal of Clinical Pharmacology · doi:10.1111/j.1365-2125.1979.tb04701.x · Cited by 58
Opioid agonist and antagonist behavioural effects of buprenorphine
Leander, J. D. (1983) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1983.tb09410.x · Cited by 39
Compounds of novel structure having kappa-agonist behavioral effects in Rhesus monkeys
Katz, J. L., Woods, J. H., Winger, G. D., & Jacobson, A. E. (1982) · Life Sciences · doi:10.1016/0024-3205(82)90160-6 · Cited by 26
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Mu Opioids and Their Receptors: Evolution of a Concept
Pasternak, G. W., & Pan, Y. (2013) · Pharmacological Reviews · doi:10.1124/pr.112.007138 · Cited by 582
Fudala, P. J., Bridge, T. P., Herbert, S., Williford, W. O., Chiang, C. N., Jones, K., Collins, J., Raisch, D., Casadonte, P., Goldsmith, R. J., et al. (2003) · New England Journal of Medicine · doi:10.1056/nejmoa022164 · Cited by 577
Attenuation of Antidepressant Effects of Ketamine by Opioid Receptor Antagonism
Williams, N. R., Heifets, B. D., Blasey, C., Sudheimer, K., Pannu, J., Pankow, H., Hawkins, J., Birnbaum, J., Lyons, D. M., Rodriguez, C. I., et al. (2018) · American Journal of Psychiatry · doi:10.1176/appi.ajp.2018.18020138 · Cited by 519
Huang, P., Kehner, G. B., Cowan, A., & Liu‐Chen, L. (2001) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)29586-0 · Cited by 340
Buprenorphine vs Methadone Maintenance Treatment for Concurrent Opioid Dependence and Cocaine Abuse
Schottenfeld, R. S. (1997) · Archives of General Psychiatry · doi:10.1001/archpsyc.1997.01830200041006 · Cited by 300
Metadata
- 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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