Conflicts of interest: a matter of transparency

Citrome, Leslie

doi:10.1111/ijcp.12638

Cited by 3 publications

(2 citation statements)

References 6 publications

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“…The accuracy of the proposed voltammetric methods for the determination of BRX was studied. The results obtained were summarized in Tables (1) which confirmed that the proposed methods are accurate, as Log Ip (µA) = 0.698 log ν (Vs −1 ) + 1.455 r 2 = 0.990 ( 2)…”

supporting

confidence: 55%

Anodic Stripping Voltammetric Methods for Determination of Brexpiprazole and its Elec-Trochemical Oxidation Behavior in Pure Form and Pharmaceutical Preparations

Salama¹,

Attia²,

El-Shal³

et al. 2020

JNMES

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http://new-mat.org http://iieta.org/journals/jnmes Brexpiprazole The drug received FDA approval for the treatment of schizophrenia and for adjunctive use for the treatment of major depressive disorder (mental disorder with low mode for at least two weeks) due to its dopamine D2 receptor partial agonist effect based on a clinical trial development programme that included two pivotal Phase III trials of brexpiprazole monotherapy in acute schizophrenia (1). This drug has high affinity for 5-HT1A, 5-HT2A, D2 and α1B, 2C receptors. It displays partial agonism at 5-HT1A and D2 receptors and potent antagonism at 5-HT2Aand α1B, 2C adrenergic receptors. It also has some affinity (antagonism) for D3, 5-HT2B, 5-HT7 and α1A, 1D receptors, and moderate affinity for H1 and low affinity for M1 receptors. It has antipsychotic effect to improve the sleep patterns and cognitive performance; also, it has the potential to treat anhedonia (a loss of capacity to feel pleasure) and cognitive deficits as core symptoms in major depressive disorder and schizophrenia with a few side effects. Usually augmented with other typical and some atypical antipsychotics drugs to improve both positive and negative symptoms (2).Brexpiprazole is chemically designated as 7-{4-[4-(1benzothiophen-4-yl) piperazin-1-yl]butoxy}-1,2-dihydroquinolin-2one. Its molecular formula is C 25 H 27 N 3 O 2 S, and its molecular weight is 433.57. Brexpiprazole is a white-to-off white powder. It is practically insoluble in water and freely soluble in methanol [3]. A review of the literature revealed that a few analytical methods have been described for the determination of brexpiprazole in pharmaceutical by HPLC method [4], and in human urine sample with its metabolites using liquid chromatography-quadrupole time-of-flight mass spectrometry (LC-QTOF). [5] Up to date there is no study dealing with electrochemical behavior of BRX based on its oxidation or reduction, one aim of the present study was the investigation of electrochemical oxidation behavior of BRX using voltammetric methods. Development of new validated stripping voltammetric determination methods for the assay of BRX in

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supporting

confidence: 55%

Anodic Stripping Voltammetric Methods for Determination of Brexpiprazole and its Elec-Trochemical Oxidation Behavior in Pure Form and Pharmaceutical Preparations

Salama¹,

Attia²,

El-Shal³

et al. 2020

JNMES

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“…Brexpiprazole (ChEMBL2105760) is an antipsychotic approved for the treatment of schizophrenia and major depressive disorders (Citrome, 2015). Apart from theinteractions of the benzothiophene ring with Trp32, the carbonyl group engages in hydrogen bonding to Lys23, Glu24 and Pro28 (Supplementary Fig.…”

Section: Docking Results For Pharmacophore Modelmentioning

confidence: 99%

Structure-based discovery of an antipsychotic drug, paliperidone, as a modulator of human superoxide dismutase 1: a potential therapeutic target in amyotrophic lateral sclerosis

Aouti

Padavattan

Padmanabhan

2023

Acta Cryst Sect D Struct Biol

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Aggregates of the antioxidant superoxide dismutase 1 (SOD1) are one of the major contributors to the pathogenesis of amyotrophic lateral sclerosis (ALS). Mutations in SOD1 lead to an unstable structure and aggregation that perturbs the balance of reactive oxygen species in cells. Oxidation damage to the solvent-exposed Trp32 also causes aggregation of SOD1. Here, the FDA-approved antipsychotic drug paliperidone is identified to interact with Trp32 of SOD1 by structure-based pharmacophore mapping and crystallographic studies. Paliperidone is used for the treatment of schizophrenia. The crystal structure of the complex with SOD1, refined to 2.1 Å resolution, revealed that the ligand binds to the SOD1 β-barrel in the β-strand 2 and 3 regions, which are known to scaffold SOD1 fibrillation. The drug also makes substantial π–π interaction with Trp32. Microscale thermophoresis studies confirm significant binding affinity of the compound, suggesting that the ligand can inhibit or prevent tryptophan oxidation. Thus, the antipsychotic drug paliperidone or a derivative may avert SOD1 aggregation and can be used as a lead for ALS drug development.

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Perspectives on non-financial conflicts of interest in health-related journals: A scoping review

Wiersma,

Kerridge,

Lipworth

2024

Accountability in Research

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Conflicts of interest: a matter of transparency

Abstract: Linked Comment: Clark . 2015; 69: 270–2. Linked Comment: Mayes . 2015; 69: 384–5. Linked Comment: Stossel . 2015; 69: 385–6.

Cited by 3 publications

References 6 publications

Anodic Stripping Voltammetric Methods for Determination of Brexpiprazole and its Elec-Trochemical Oxidation Behavior in Pure Form and Pharmaceutical Preparations

Anodic Stripping Voltammetric Methods for Determination of Brexpiprazole and its Elec-Trochemical Oxidation Behavior in Pure Form and Pharmaceutical Preparations

Structure-based discovery of an antipsychotic drug, paliperidone, as a modulator of human superoxide dismutase 1: a potential therapeutic target in amyotrophic lateral sclerosis

Perspectives on non-financial conflicts of interest in health-related journals: A scoping review

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