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Analysis of institutional authors

Matera, CarloCorresponding AuthorRiefolo, FabioAuthor
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Novel analgesic agents obtained by molecular hybridization of orthosteric and allosteric ligands

Publicated to:European Journal Of Pharmacology. 876 173061- - 2020-06-05 876(), DOI: 10.1016/j.ejphar.2020.173061

Authors: Matera, C; Flammini, L; Riefolo, F; Domenichini, G; De Amici, M; Barocelli, E; Dallanoce, C; Bertoni, S

Affiliations

Barcelona Inst Sci & Technol, Inst Bioengn Catalonia IBEC, Carrer Baldiri Reixac 10-12, Barcelona 08028, Spain - Author
Nanoprobes and Nanoswitches. Institute for Bioengineering of Catalonia - Author
Univ Milan, Dipartimento Sci Farmaceut, Via L Mangiagalli 25, I-20133 Milan, Italy - Author
Univ Parma, Dipartimento Farm, Parco Area Sci 27A, I-43124 Parma, Italy - Author

Abstract

Despite the high incidence of acute and chronic pain in the general population, the efficacy of currently available medications is unsatisfactory. Insufficient management of pain has a profound impact on the quality of life and can have serious physical, psychological, social, and economic consequences. This unmet need reflects a failure to develop novel classes of analgesic drugs with superior clinical properties and lower risk of abuse. Nevertheless, recent advances in our understanding of the neurobiology of pain are offering new opportunities for developing different therapeutic approaches. Among those, the activation of M2 muscarinic acetylcholine receptors, which play a key role in the cholinergic regulation of the nociceptive transmission, constitutes one of the most promising strategies. We have recently developed a small library of novel pharmacological agents by merging the structures of known orthosteric and allosteric muscarinic ligands through their molecular hybridization, an emerging approach in medicinal chemistry based on the combination of pharmacophoric moieties of different bioactive substances to produce a new compound with improved pharmacological properties. Herein we report the functional characterization of the new ligands in vitro and the assessment of their efficacy as analgesic agents and tolerability in mice. This work provides new insights for the development and optimization of novel muscarinic hybrid compounds for the management of pain.

Keywords
allostericanalgesiahybrid ligandmolecular hybridizationmuscarinic acetylcholine receptorAgonistsAllostericAllosteric regulationAllosteric siteAnalgesiaAnalgesicsAnimalsAtrial function, leftBehavior, animalDesignDose-response relationship, drugDrug discoveryEfficaciesFunctional-characterizationGuinea pigsHeart atriaHybrid ligandIn vitro techniquesLigandsMaleMiceMolecular hybridizationMotor activityMuscarinic acetylcholine receptorMuscarinic acetylcholine-receptorsOrthostericOxotremorinePainReceptor, muscarinic m2Strategy

Quality index

Bibliometric impact. Analysis of the contribution and dissemination channel

The work has been published in the journal European Journal Of Pharmacology 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, 2020, it was in position , thus managing to position itself as a Q1 (Primer Cuartil), in the category Pharmacology.

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 2025-05-23:

  • WoS: 4
  • Scopus: 4
  • Europe PMC: 3
  • OpenCitations: 3
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 2025-05-23:

  • 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: 18 (PlumX).

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.
Leadership analysis of institutional authors

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

There is a significant leadership presence as some of the institution’s authors appear as the first or last signer, detailed as follows: First Author (Matera, Carlo) .

the author responsible for correspondence tasks has been Matera, Carlo.