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Analysis of institutional authors

López Arribas, RaquelAuthorDe Los Ríos, CristóbalCorresponding Author

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January 23, 2023
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Article

Synthesis and Biological Assessment of 4,1-Benzothiazepines with Neuroprotective Activity on the Ca2+ Overload for the Treatment of Neurodegenerative Diseases and Stroke

Publicated to: Molecules. 26 (15): 4473- - 2021-08-01 26(15), DOI: 10.3390/molecules26154473

Authors:

Viejo, Lucia; Rubio-Alarcon, Marcos; Arribas, Raquel L; Moreno-Castro, Manuel; Perez-Marin, Raquel; Braun-Cornejo, Maria; Estrada-Valencia, Martin; de los Rios, Cristobal
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Affiliations

Hosp Univ La Princesa, Inst Invest Sanitaria, Serv Farmacol Clin, Madrid 28006, Spain - Author
Univ Autonoma Madrid, Dept Farmacol & Terapeut, C Arzobispo Morcillo 4, Madrid 28029, Spain - Author
Univ Autonoma Madrid, Inst Fdn Teofilo Hernando, C Arzobispo Morcillo 4, Madrid 28029, Spain - Author
Univ Leeds, Sch Med, Leeds Inst Cardiovasc & Metab Med, Leeds LS2 9JT, W Yorkshire, England - Author
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Abstract

In excitable cells, mitochondria play a key role in the regulation of the cytosolic Ca2+ levels. A dysregulation of the mitochondrial Ca2+ buffering machinery derives in serious pathologies, where neurodegenerative diseases highlight. Since the mitochondrial Na+/Ca2+ exchanger (NCLX) is the principal efflux pathway of Ca2+ to the cytosol, drugs capable of blocking NCLX have been proposed to act as neuroprotectants in neuronal damage scenarios exacerbated by Ca2+ overload. In our search of optimized NCLX blockers with augmented drug-likeness, we herein describe the synthesis and pharmacological characterization of new benzothiazepines analogues to the first-in-class NCLX blocker CGP37157 and its further derivative ITH12575, synthesized by our research group. As a result, we found two new compounds with an increased neuroprotective activity, neuronal Ca2+ regulatory activity and improved drug-likeness and pharmacokinetic properties, such as clog p or brain permeability, measured by PAMPA experiments.
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Keywords

7-chloro-5-(2-isopropylphenyl)-3,5-dihydro-4,1-benzothiazepin-2-(1h)-oneAlpha-synucleinAmpa receptorsAnimalsBenzothiazepine cgp37157BenzothiazepinesCa overload 2+Ca2+ overloadCalciumCalcium channel blockersCalcium signalingCell line, tumorCellsCgp37157FemaleGated calcium-channelsHumansMitochondriaMouse modelNeurodegenerative diseasesNeuronal vulnerabilityNeuronsNeuroprotectionNeuroprotective agentsNmda-receptorsOxidative stressRatsSensitivityStrokeThiazepines

Quality index

Bibliometric impact. Analysis of the contribution and dissemination channel

The work has been published in the journal Molecules due to its progression and the good impact it has achieved in recent years, according to the agency Scopus (SJR), it has become a reference in its field. In the year of publication of the work, 2021, it was in position , thus managing to position itself as a Q1 (Primer Cuartil), in the category Pharmaceutical Science.

Independientemente del impacto esperado determinado por el canal de difusión, es importante destacar el impacto real observado de la propia aportación.

Según las diferentes agencias de indexación, el número de citas acumuladas por esta publicación hasta la fecha 2025-12-17:

  • WoS: 9
  • Scopus: 11
  • Europe PMC: 4
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Impact and social visibility

From the perspective of influence or social adoption, and based on metrics associated with mentions and interactions provided by agencies specializing in calculating the so-called "Alternative or Social Metrics," we can highlight as of 2025-12-17:

  • The use, from an academic perspective evidenced by the Altmetric agency indicator referring to aggregations made by the personal bibliographic manager Mendeley, gives us a total of: 19.
  • The use of this contribution in bookmarks, code forks, additions to favorite lists for recurrent reading, as well as general views, indicates that someone is using the publication as a basis for their current work. This may be a notable indicator of future more formal and academic citations. This claim is supported by the result of the "Capture" indicator, which yields a total of: 19 (PlumX).

With a more dissemination-oriented intent and targeting more general audiences, we can observe other more global scores such as:

  • The Total Score from Altmetric: 3.
  • The number of mentions on the social network X (formerly Twitter): 4 (Altmetric).

It is essential to present evidence supporting full alignment with institutional principles and guidelines on Open Science and the Conservation and Dissemination of Intellectual Heritage. A clear example of this is:

  • The work has been submitted to a journal whose editorial policy allows open Open Access publication.
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Leadership analysis of institutional authors

This work has been carried out with international collaboration, specifically with researchers from: United Kingdom.

There is a significant leadership presence as some of the institution’s authors appear as the first or last signer, detailed as follows: Last Author (Ríos Salgado, Cristóbal de los).

the author responsible for correspondence tasks has been Ríos Salgado, Cristóbal de los.

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Awards linked to the item

This research was funded by Acciones Estrategicas en Salud, Proyectos de Investigacion en Salud (ISCIII/FEDER, PI16/01041, PI19/01724).
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