Bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics

Antipsychotics (APs) are widely used medications, however these are not without side effects such as disruption of blood brain barrier function (BBB). To investigate this further we have studied the chronic effects of the typical APs, chlorpromazine (CPZ) and haloperidol (HAL) and the atypical APs,...

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Main Authors: Elmorsy, Ekramy, Smith, Paul A.
Format: Article
Published: Elsevier 2015
Subjects:
Online Access:https://eprints.nottingham.ac.uk/43322/
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author Elmorsy, Ekramy
Smith, Paul A.
author_facet Elmorsy, Ekramy
Smith, Paul A.
author_sort Elmorsy, Ekramy
building Nottingham Research Data Repository
collection Online Access
description Antipsychotics (APs) are widely used medications, however these are not without side effects such as disruption of blood brain barrier function (BBB). To investigate this further we have studied the chronic effects of the typical APs, chlorpromazine (CPZ) and haloperidol (HAL) and the atypical APs, risperidone (RIS) and clozapine (CLZ), on the bioenergetics of human micro-vascular endothelial cells (HBVECs) of the BBB. Alamar blue (AB) and ATP assays showed that these APs impair bioenergenesis in HBVECs in a concentration and time dependent manner. However since these effects were incomplete they suggest a population of cell bioenergetically heterogeneous, an idea supported by the bistable nature by which APs affected the mitochondrial transmembrane potential. CPZ, HAL and CLZ inhibited the activity of mitochondrial complexes I and III. Our data demonstrates that at therapeutic concentrations, APs can impair the bioenergetic status of HBVECs, an action that help explains the adverse side effects of these drugs when used clinically.
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spelling nottingham-433222020-05-04T17:08:44Z https://eprints.nottingham.ac.uk/43322/ Bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics Elmorsy, Ekramy Smith, Paul A. Antipsychotics (APs) are widely used medications, however these are not without side effects such as disruption of blood brain barrier function (BBB). To investigate this further we have studied the chronic effects of the typical APs, chlorpromazine (CPZ) and haloperidol (HAL) and the atypical APs, risperidone (RIS) and clozapine (CLZ), on the bioenergetics of human micro-vascular endothelial cells (HBVECs) of the BBB. Alamar blue (AB) and ATP assays showed that these APs impair bioenergenesis in HBVECs in a concentration and time dependent manner. However since these effects were incomplete they suggest a population of cell bioenergetically heterogeneous, an idea supported by the bistable nature by which APs affected the mitochondrial transmembrane potential. CPZ, HAL and CLZ inhibited the activity of mitochondrial complexes I and III. Our data demonstrates that at therapeutic concentrations, APs can impair the bioenergetic status of HBVECs, an action that help explains the adverse side effects of these drugs when used clinically. Elsevier 2015-05-08 Article PeerReviewed Elmorsy, Ekramy and Smith, Paul A. (2015) Bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics. Biochemical and Biophysical Research Communications, 460 (3). pp. 857-862. ISSN 1090-2104 Antipsychotics Mitochondria Blood brain barrier Endothelia Heterogeneity Toxicology https://doi.org/10.1016/j.bbrc.2015.03.122 doi:10.1016/j.bbrc.2015.03.122 doi:10.1016/j.bbrc.2015.03.122
spellingShingle Antipsychotics
Mitochondria
Blood brain barrier
Endothelia
Heterogeneity
Toxicology
Elmorsy, Ekramy
Smith, Paul A.
Bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics
title Bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics
title_full Bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics
title_fullStr Bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics
title_full_unstemmed Bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics
title_short Bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics
title_sort bioenergetic disruption of human micro-vascular endothelial cells by antipsychotics
topic Antipsychotics
Mitochondria
Blood brain barrier
Endothelia
Heterogeneity
Toxicology
url https://eprints.nottingham.ac.uk/43322/
https://eprints.nottingham.ac.uk/43322/
https://eprints.nottingham.ac.uk/43322/