Bremazocine: A κ‐Opioid Agonist with Potent Analgesic and Other Pharmacologic Properties

Dortch‐Carnes, Juanita; Potter, David E.

doi:10.1111/j.1527-3458.2005.tb00270.x

Cited by 47Neuropeptides and Animal PhysiologyPain Management and Opioid UseAlkaloids: synthesis and pharmacology

Bremazocine: A κ‐Opioid Agonist with Potent Analgesic and Other Pharmacologic Properties

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Dortch‐Carnes, Juanita, Potter, David E.·2005·CNS Drug Reviews

DOI 10.1111/j.1527-3458.2005.tb00270.xPMC PMC6741727

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Abstract

Bremazocine is a κ‐opioid receptor agonist with potent analgesic and diuretic activities. As an analgesic it is three‐ to four‐times more potent than morphine, as determined in both hot plate and tail flick tests. Bremazocine and other benzomorphan analogs were synthesized in an effort to produce opiates with greater κ‐opioid receptor selectivity and with minimal morphine‐like side effects. Unlike morphine bremazocine is devoid of physical and psychological dependence liability in animal models and produces little or no respiratory depression. While bremazocine does not produce the characteristic euphoria associated with morphine and its abuse, it has been shown to induce dysphoria, a property that limits its clinical usefulness. Similarly to morphine, repeated administration of bremazocine leads to tolerance to its analgesic effect. It has been demonstrated that the marked diuretic effect of bremazocine is mediated primarily by the central nervous system. Because of its psychotomimetic side effects (disturbance in the perception of space and time, abnormal visual experience, disturbance in body image perception, de‐personalization, de‐realization and loss of self control) bremazocine has limited potential as a clinical analgesic. However, its possible utility for the therapy of alcohol and drug addiction warrants further consideration because of its ability to decrease ethanol and cocaine self‐administration in non‐human primates. In addition, the ability of bremazocine‐like drugs to lower intraocular pressure and to minimize ischemic damage in animal models suggests their possible use in the therapy of glaucoma and cardiovascular disease.

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Authors: Dortch‐Carnes, J., & Potter, D. E.
Affiliations: Morehouse School of Medicine (US)
Medical University of South Carolina (US)
Corresponding author: Dortch‐Carnes, Juanita
ORCID: Potter, David E.
Venue: CNS Drug Reviews
Publisher: Wiley
Published: 2005-03
Volume: 11
Issue: 2
Pages: 195-212
ISSN: 1080-563X (ISSN-L)
1527-3458
DOI: 10.1111/j.1527-3458.2005.tb00270.x
PMC: PMC6741727
OpenAlex: W1993659014
Cited by: 47
References: 131
Citations by year: 2026: 1 · 2023: 1 · 2022: 2 · 2021: 4 · 2020: 2 · 2019: 4 · 2018: 2 · 2017: 2 · 2016: 3 · 2015: 6 · 2014: 1 · 2013: 4 · 2012: 1
FWCI: 0.20
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor, 463 d)
Locations: CNS Drug Reviews (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Funders: National Institutes of Health (7r01ey012807-04, 5r01ey011977-08)
National Eye Institute (EY 011977, EY-014793, R24EY014793, EY-012807)
Topics: Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
Health Sciences › Medicine › Anesthesiology and Pain Medicine › Pain Management and Opioid Use
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Alkaloids: synthesis and pharmacology
Keywords: bremazocine, kappa opioid receptor agonists, analgesia, diuretic effect, morphine dependence, respiratory depression, dysphoria, analgesic tolerance, psychotomimetic effects, alcohol and drug addiction, ethanol self-administration, cocaine self-administration, intraocular pressure, glaucoma, cardiovascular disease, opioid side effects
MeSH terms: Analgesics, Animals, Benzomorphans, Cardiovascular System, Disease Models, Animal, Diuresis, Humans, Motor Activity, Synaptic Transmission, Pain, Respiration, Signal Transduction, Receptors, Opioid, kappa

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Bremazocine: A κ‐Opioid Agonist with Potent Analgesic and Other Pharmacologic Properties

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