Examinando por Autor "Callado Hernando, Luis Felipe"

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    Discovery of (3-Phenylcarbamoyl-3,4-dihydro-2H-pyrrol-2-yl)phosphonates as Imidazoline I2 Receptor Ligands with Anti-Alzheimer and Analgesic Properties
    (American Chemical Society, 2025) Bagán, Andrea; López Ruiz, Alba; Abás Prades, Sònia; Ruiz Cantero, María del Carmen; Vasilopoulou, Foteini; Taboada Jara, Teresa; Griñán Ferré, Christian; Pallàs, Mercè; Muguruza, Carolina; Diez Alarcia, Rebeca; Callado Hernando, Luis Felipe; Entrena Fernández, José Manuel; Cobos del Moral, Enrique José; Pérez, Belén; Morales García, José Ángel; Molins Grau, Elies; De Jonghe, Steven; Daelemans, Dirk; Brea Floriani, José Manuel; Val, Cristina; Loza García, M. Isabel; Hernández Hernández, Elena; García Sevilla, Jesús Andrés; García Fuster, María Julia; Díaz, Caridad; Fernández Godino, Rosario; Genilloud Rodríguez, Olga; Beljkaš, Milan; Oljačić, Slavika; Nikolic, Katarina; Escolano Mirón, Carmen
    Imidazoline I2 receptors (I2-IRs) are altered in Alzheimer’s disease (AD) patients and are associated with analgesia. I2-IRs are not structurally described, and their pharmacological characterization relies on their modulation by highly affine ligands. Herein, we describe the synthesis of (3-phenylcarbamoyl-3,4-dihydro-2H-pyrrol-2-yl)phosphonates endowed with relevant affinities for I2-IRs in human brain tissues. The optimal ADME and pharmacokinetic profile of a selected compound, 12d, secured its in vivo exploration in a senescence accelerated prone 8 mice revealing improvement in the cognitive impairment and unveiling the mechanism of action by analyzing specific AD biomarkers. The treatment of a capsaicin-induced mechanical hypersensitivity murine model with 12d revealed analgesic properties devoid of motor coordination issues. The target engagement of 12d was demonstrated by suppression of the analgesic effect by pretreatment with idazoxan. Overall, 12d is a putative candidate for advancing preclinical phases and supports the modulation of I2-IRs as an innovative approach for therapeutics.
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    Quality indicators for penitentiary medical reports supporting the adoption of alternative measures to imprisonment on health grounds
    (Elsevier España, 2026) Aia Goikoetxea, Nahia; Bengoetxea Martínez, Itxaso; Morentín, Benito; Arostegui Madariaga, Inmaculada; Callado Hernando, Luis Felipe ; Garro Carrera, Enara
    Introduction/objectives. Humanitarian release from prison on health grounds is a measure to preserve human dignity, recommended by international human rights bodies and enshrined in the legislation of many countries. A medical report is required for such a judicial decision. The objective of this study was to analyse the quality, content and variability of medical reports used for early release from prison on health grounds. Methods: a retrospective observational descriptive study was conducted on 164 medical reports for the early release of persons deprived of liberty obtained in the Basque Autonomous Community (BAC) and Catalonia. Structural aspects, clinical content, compliance with the standards of clinical reports in the health system, and relevant medico-legal aspects were evaluated. Results.The study revealed that there was a high degree of variability, that the importance of the temporary life prognosis for the granting of this type of measure was significant in Spain, and that the health baseline situation of the subjects studied was advanced. Analysis of the quality of the reports revealed significant technical deficiencies and the frequent absence of basic clinical elements. Barriers to accessing information sources limit research. Conclusions. The absence of standardised guidelines or protocols at the national and international levels for the drafting of this type of report leads us to propose further advancement in this important area of human rights.