Clobenpropit, a histamine H 3 receptor antagonist/inverse agonist, inhibits [ 3 H]-dopamine uptake by human neuroblastoma SH-SY5Y cells and rat brain synaptosomes

Mena-Avila, Elvia; Márquez-Gómez, Ricardo; Aquino-Miranda, Guillermo; Nieto-Alamilla, Gustavo; Arias‐Montaño, José‐Antonio

doi:10.1016/j.pharep.2017.08.007

Cited by 6 publications

(1 citation statement)

References 38 publications

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“…Nonetheless, 6-OHDA and rotenone are mitochondrial toxicants known to have different mechanisms of action. Firstly, while rotenone is a highly lipophilic and hydrophobic molecule that can easily cross cell membranes without the need for specific membrane transport mechanisms [ 31 ], 6-OHDA cellular uptake needs specific transporters such as the dopamine or norepinephrine transporters [ 32 , 33 ]. Regarding mitochondrial-induced toxic effects, these compounds also display different mechanisms of action.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of 6-Hydroxydopamine and Rotenone In Vitro Neurotoxicity on Differentiated SH-SY5Y Cells Using Applied Computational Statistics

Simões

Oliveira

Cunha‐Oliveira

et al. 2022

IJMS

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With the increase in life expectancy and consequent aging of the world’s population, the prevalence of many neurodegenerative diseases is increasing, without concomitant improvement in diagnostics and therapeutics. These diseases share neuropathological hallmarks, including mitochondrial dysfunction. In fact, as mitochondrial alterations appear prior to neuronal cell death at an early phase of a disease’s onset, the study and modulation of mitochondrial alterations have emerged as promising strategies to predict and prevent neurotoxicity and neuronal cell death before the onset of cell viability alterations. In this work, differentiated SH-SY5Y cells were treated with the mitochondrial-targeted neurotoxicants 6-hydroxydopamine and rotenone. These compounds were used at different concentrations and for different time points to understand the similarities and differences in their mechanisms of action. To accomplish this, data on mitochondrial parameters were acquired and analyzed using unsupervised (hierarchical clustering) and supervised (decision tree) machine learning methods. Both biochemical and computational analyses resulted in an evident distinction between the neurotoxic effects of 6-hydroxydopamine and rotenone, specifically for the highest concentrations of both compounds.

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Section: Discussionmentioning

confidence: 99%

Evaluation of 6-Hydroxydopamine and Rotenone In Vitro Neurotoxicity on Differentiated SH-SY5Y Cells Using Applied Computational Statistics

Simões

Oliveira

Cunha‐Oliveira

et al. 2022

IJMS

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Milligram scale enantioresolution of promethazine and its main metabolites, determination of their absolute configuration and assessment of enantioselective effects on human SY-SY5Y cells

Coelho,

Costa,

de Albuquerque

et al. 2024

Journal of Pharmaceutical and Biomedical Analysis

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Histamine H3 receptor activation reduces the impairment in prepulse inhibition (PPI) of the acoustic startle response and Akt phosphorylation induced by MK-801 (dizocilpine), antagonist at N-Methyl-d-Aspartate (NMDA) receptors

Aquino-Miranda

Rivera-Ramírez

Márquez-Gómez

et al. 2019

Progress in Neuro-Psychopharmacology and Biological Psychiatry

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Clobenpropit, a histamine H 3 receptor antagonist/inverse agonist, inhibits [ 3 H]-dopamine uptake by human neuroblastoma SH-SY5Y cells and rat brain synaptosomes

Abstract: These data indicate a direct inhibitory effect of clobenpropit on catecholamine transport.

Cited by 6 publications

References 38 publications

Evaluation of 6-Hydroxydopamine and Rotenone In Vitro Neurotoxicity on Differentiated SH-SY5Y Cells Using Applied Computational Statistics

Evaluation of 6-Hydroxydopamine and Rotenone In Vitro Neurotoxicity on Differentiated SH-SY5Y Cells Using Applied Computational Statistics

Milligram scale enantioresolution of promethazine and its main metabolites, determination of their absolute configuration and assessment of enantioselective effects on human SY-SY5Y cells

Histamine H3 receptor activation reduces the impairment in prepulse inhibition (PPI) of the acoustic startle response and Akt phosphorylation induced by MK-801 (dizocilpine), antagonist at N-Methyl-d-Aspartate (NMDA) receptors

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