Cited by 40Lipid Membrane Structure and BehaviorPharmacological Receptor Mechanisms and EffectsProtein Interaction Studies and Fluorescence Analysis

The Interaction of Antipsychotic Drugs with Lipids and Subsequent Lipid Reorganization Investigated Using Biophysical Methods

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Alves, Isabel, Staneva, Galya, Tessier, Cedric, Salgado, Gilmar F., Nuss, Philippe·2011·Biochimica et Biophysica Acta (BBA) - Biomembranes

Abstract

The interaction of antipsychotic drugs (AP) with lipids and the subsequent lipid reorganization on model membranes was assessed using a combination of several complementary biophysical approaches (calorimetry, plasmon resonance, fluorescence microscopy, X-ray diffraction and molecular modeling). The effect of haloperidol (HAL), risperidone (RIS), and 9-OH-risperidone (9-OH-RIS) was examined on single lipid and mixtures comprising lipids of biological origin. All APs interact with lipids and induced membrane reorganization. APs showed higher affinity for sphingomyelin than for phosphatidylcholine. Cholesterol increased AP affinity for the lipid bilayer and led to the following AP ranking regarding affinity and structural changes: RIS >9-OH-RIS >HAL. Liquid-ordered domain formation and bilayer thickness were differentially altered by AP addition. Docking calculations helped understanding the observed differences between the APs and offer a representation of their conformation in the lipid bilayer. Present results indicate that AP drugs may change membrane compartmentalization which could differentially modulate the signaling cascade of the dopamine D2 receptor for which APs are ligands.

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Crossref · 10.1016/j.bbamem.2011.02.021

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References 53 · Cited by 40

Authors
Alves, I., Staneva, G., Tessier, C., Salgado, G. F., & Nuss, P.
Affiliations
  • Centre National de la Recherche Scientifique (FR)
  • Bulgarian Academy of Sciences (BG)
  • Inserm (FR)
Corresponding author
Nuss, Philippe
Venue
Biochimica et Biophysica Acta (BBA) - Biomembranes
Publisher
Elsevier BV
Published
2011-08
Volume
1808
Issue
8
Pages
2009-2018
ISSN
0005-2736 (ISSN-L)
OpenAlex
W1987792440
Cited by
40
References
53
Citations by year
2026: 1 · 2025: 4 · 2024: 2 · 2023: 6 · 2022: 5 · 2021: 2 · 2020: 3 · 2019: 5 · 2018: 3 · 2017: 1 · 2016: 2 · 2015: 1 · 2014: 2 · 2012: 3
FWCI
0.65
Type
journal article
Language
en
Open access
Locations
  • Biochimica et Biophysica Acta (BBA) - Biomembranes (publishedVersion)
  • PubMed (publishedVersion)
  • HAL (submittedVersion)
Funders
European Social Fund
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Lipid Membrane Structure and Behavior
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Pharmacological Receptor Mechanisms and Effects
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Interaction Studies and Fluorescence Analysis
Keywords
antipsychotic drugs, drug-lipid interactions, lipid reorganization, model membranes, haloperidol, risperidone, sphingomyelin, phosphatidylcholine, cholesterol, liquid-ordered domains, bilayer thickness, membrane compartmentalization, molecular docking
MeSH terms
Paliperidone Palmitate, Calorimetry, Differential Scanning, Cell Membrane, Cholesterol, Haloperidol, Isoxazoles, Membrane Lipids, Membranes, Artificial, Microscopy, Fluorescence, Models, Molecular, Molecular Conformation, Phosphatidylcholines, Pyrimidines, Sphingomyelins, Structure-Activity Relationship, Antipsychotic Agents, X-Ray Diffraction, 1,2-Dipalmitoylphosphatidylcholine, Molecular Structure, Receptors, Dopamine D2, Dopamine Antagonists, Risperidone, Surface Plasmon Resonance, Dopamine D2 Receptor Antagonists

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