Interactions of selective serotonin reuptake inhibitors with subtypes of σ receptors in rat brain
Abstract
The interactions of selective serotonin reuptake inhibitors and tricyclic antidepressants with subtypes of sigma receptors were investigated. The rank order of affinity (Ki values) from competition experiments of [3H](+)-pentazocine binding to sigma 1 sites was: fluvoxamine > sertraline > S(+)-fluoxetine > (+/-)-fluoxetine > citalopram > imipramine > paroxetine > desipramine > R(-)-fluoxetine > (+/-)-norfluoxetine. The Ki values of all drugs for sigma 2 sites were more than 1000 nM. Furthermore, all drugs were more potent at sigma 1 sites than at sigma 2 sites. These findings suggest that sigma receptors (sigma 1 site) may play, in some way, a role in the actions of selective serotonin reuptake inhibitors.
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Activation of S1R by SSRIs enhances BDNF expression.
“In like manner, activation of S1R by SSRIs enhances BDNF expression (105, 106).”
From Psychedelics and Neuroplasticity: A Systematic Review Unraveling the Biological Underpinnings of Psychedelics. (2021) · cites this paper as [106]
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References 12 · Cited by 254
- Authors
- Narita, N., Hashimoto, K., Tomitaka, S.-I., & Minabe, Y.
- Affiliations
- National Center of Neurology and Psychiatry (JP)
- Corresponding author
- Hashimoto, Kenji
- ORCID
- Hashimoto, Kenji
- Venue
- European Journal of Pharmacology
- Publisher
- Elsevier BV
- Published
- 1996-06
- Volume
- 307
- Issue
- 1
- Pages
- 117-119
- ISSN
- 0014-2999 (ISSN-L)
- OpenAlex
- W1970897378
- Cited by
- 254
- References
- 12
- Citations by year
- 2026: 4 · 2025: 10 · 2024: 5 · 2023: 5 · 2022: 16 · 2021: 15 · 2020: 8 · 2019: 7 · 2018: 7 · 2017: 13 · 2016: 6 · 2015: 9 · 2014: 13 · 2013: 18 · 2012: 17
- FWCI
- 1.27
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Pharmacological Receptor Mechanisms and Effects
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Health Sciences › Medicine › Pharmacology › Treatment of Major Depression
- Keywords
- selective serotonin reuptake inhibitors, sigma receptors, sigma-1 receptor, sigma-2 receptor, tricyclic antidepressants, fluoxetine, fluvoxamine, sertraline, citalopram, paroxetine, imipramine, desipramine, receptor binding affinity, drug interactions
- MeSH terms
- Animals, Antidepressive Agents, Tricyclic, Brain, Desipramine, Fluoxetine, Imipramine, Male, Stereoisomerism, Rats, Sprague-Dawley, Selective Serotonin Reuptake Inhibitors, Receptors, Opioid, delta, Antidepressive Agents, Second-Generation, Rats
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