Preclinical and clinical characterization of the selective 5‐HT1Areceptor antagonist DU‐125530 for antidepressant treatment

Scorza, MC; Lladó‐Pelfort, L; Oller, S; Cortés, R; Puigdemont, D; Portella, MJ; Pérez‐Egea, R; Alvarez, E; Celada, P; Pérez, V; Artigas, F

doi:10.1111/j.1476-5381.2011.01770.x

Cited by 46Treatment of Major DepressionNeurotransmitter Receptor Influence on BehaviorNeuroscience and Neuropharmacology Research

Preclinical and clinical characterization of the selective 5‐HT1Areceptor antagonist DU‐125530 for antidepressant treatment

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Scorza, MC, Lladó‐Pelfort, L, Oller, S, Cortés, R, Puigdemont, D, Portella, MJ, Pérez‐Egea, R, Alvarez, E +3 more·2012·British Journal of Pharmacology

DOI 10.1111/j.1476-5381.2011.01770.xPMC PMC3492984

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Abstract

BACKGROUND AND PURPOSE The antidepressant efficacy of selective 5‐HT reuptake inhibitors (SSRI) and other 5‐HT‐enhancing drugs is compromised by a negative feedback mechanism involving 5‐HT 1A autoreceptor activation by the excess 5‐HT produced by these drugs in the somatodendritic region of 5‐HT neurones. 5‐HT 1A receptor antagonists augment antidepressant‐like effects in rodents by preventing this negative feedback, and the mixed β‐adrenoceptor/5‐HT 1A receptor antagonist pindolol improves clinical antidepressant effects by preferentially interacting with 5‐HT 1A autoreceptors. However, it is unclear whether 5‐HT 1A receptor antagonists not discriminating between pre‐ and post‐synaptic 5‐HT 1A receptors would be clinically effective. EXPERIMENTAL APPROACH We characterized the pharmacological properties of the 5‐HT 1A receptor antagonist DU‐125530 using receptor autoradiography, intracerebral microdialysis and electrophysiological recordings. Its capacity to accelerate/enhance the clinical effects of fluoxetine was assessed in a double‐blind, randomized, 6 week placebo‐controlled trial in 50 patients with major depression (clinicaltrials.gov identifier NCT01119430). KEY RESULTS DU‐125530 showed equal (low nM) potency to displace agonist and antagonist binding to pre‐ and post‐synaptic 5‐HT 1A receptors in rat and human brain. It antagonized suppression of 5‐hydroxytryptaminergic activity evoked by 8‐OH‐DPAT and SSRIs in vivo. DU‐125530 augmented SSRI‐induced increases in extracellular 5‐HT as effectively as in mice lacking 5‐HT 1A receptors, indicating a silent, maximal occupancy of pre‐synaptic 5‐HT 1A receptors at the dose used. However, DU‐125530 addition to fluoxetine did not accelerate nor augment its antidepressant effects. CONCLUSIONS AND IMPLICATIONS DU‐125530 is an excellent pre‐ and post‐synaptic 5‐HT 1A receptor antagonist. However, blockade of post‐synaptic 5‐ HT 1A receptors by DU‐125530 cancels benefits obtained by enhancing pre‐synaptic 5‐hydroxytryptaminergic function.

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SSRIs can impact the 5-HT signaling pathway, activating 5-HT1A.
“Second, SSRIs can impact the 5-HT signaling pathway, activating 5-HT 1A. 358 , 359”
From Major depressive disorder: hypothesis, mechanism, prevention and treatment (2024) · cites this paper as [359]

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“357 Second, SSRIs can impact the 5-HT signaling pathway, activating 5-HT 1A.358,359 In addition, studies have shown that antagonism of 5-HT 2A/2C receptors can enhance the effects of SSRIs such as ﬂ uoxetine.”
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Authors: Scorza, M., Lladó‐Pelfort, L., Oller, S., Cortés, R., Puigdemont, D., Portella, M., Pérez‐Egea, R., Alvarez, E., Celada, P., Pérez, V, & Artigas, F.
Affiliations: Universitat Autònoma de Barcelona (ES)
Consejo Superior de Investigaciones Científicas (ES)
Corresponding author: Artigas, F
ORCID: Cortés, R
Puigdemont, D
Celada, P
Pérez, V
Artigas, F
Venue: British Journal of Pharmacology
Publisher: Wiley
Published: 2012-10-08
Volume: 167
Issue: 5
Pages: 1021-1034
ISSN: 0007-1188 (ISSN-L)
1476-5381
DOI: 10.1111/j.1476-5381.2011.01770.x
PMC: PMC3492984
OpenAlex: W2078004955
Cited by: 46
References: 56
Citations by year: 2025: 3 · 2024: 2 · 2023: 2 · 2022: 1 · 2021: 2 · 2020: 2 · 2019: 2 · 2018: 3 · 2017: 4 · 2016: 6 · 2015: 6 · 2014: 4 · 2013: 6 · 2012: 3
FWCI: 3.04
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor)
Locations: British Journal of Pharmacology (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
DIGITAL.CSIC (Spanish National Research Council (CSIC)) (submittedVersion)
Funders: Generalitat de Catalunya (2009-SGR220)
Centro de Investigación Biomédica en Red de Salud Mental
Fundación Carolina
Instituto de Salud Carlos III
Topics: Health Sciences › Medicine › Pharmacology › Treatment of Major Depression
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords: 5-HT1A receptor antagonist, 5-HT1A autoreceptors, selective serotonin reuptake inhibitors, fluoxetine, major depressive disorder, antidepressant augmentation, negative feedback, serotonin release, 8-OH-DPAT
MeSH terms: Adult, Animals, Antidepressive Agents, Brain, Major Depressive Disorder, Drug Therapy, Combination, Female, Fluoxetine, Humans, Male, Mice, Inbred C57BL, Middle Aged, Piperazines, Pyridines, Serotonin Antagonists, Thiazoles, Rats, Wistar, Serotonin Receptor Agonists, 8-Hydroxy-2-(di-n-propylamino)tetralin, Mice, Knockout, Receptor, Serotonin, 5-HT1A, Mice, Rats

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Preclinical and clinical characterization of the selective 5‐HT1Areceptor antagonist DU‐125530 for antidepressant treatment

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