O Salas C, Zarate AM, Kryštof V, Mella J, Faundez M, Brea J, Loza MI, Brito I, Hendrychová D, Jorda R, Cabrera AR, Tapia RA, Espinosa-Bustos C. Promising 2,6,9-Trisubstituted Purine Derivatives for Anticancer Compounds: Synthesis, 3D-QSAR, and Preliminary Biological Assays. Int J Mol Sci. 2019 Dec 25. DOI: 10.3390/ijms21010161.

Codony S, Valverde E, Leiva R, Brea J, Loza MI, Morisseau C, Hammock B, Vázquez S. Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors. Bioorg Med Chem. 2019 Oct 15; 27 (20), 115078. DOI: 10.1016/j.bmc.2019.115078. Indice de impacto: 2.802 (JCR 2018). Q2.

Mallo-Abreu A, Majellaro M, Jespers W, Azuaje J, Caamaño O, García-Mera X, Brea JM, Loza MI, Gutiérrez de Terán H, Sotelo E.. Trifluorinated Pyrimidine-Based A2B Antagonists: Optimization and Evidences of Stereospecific Recognition. J Med Chem. 2019 Oct 4. DOI: 10.1021/acs.jmedchem.9b01340. [Epub ahead of print]. Indice de impacto: 6.054 (JCR 2018). Q1.

Astolfi A, Kudolo M, Brea J, Manni G, Manfroni G, Palazzotti D, Sabatini S, Cecchetti F, Felicetti T, Cannalire R, Massari S, Tabarrini O, Loza MI, Fallarino F, Cecchetti V, Laufer SA, Barreca ML. Discovery of potent p38α MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation. Eur J Med Chem. 2019 Aug 16. DOI: 10.1016/j.ejmech.2019.111624. [Epub ahead of print]. Indice de impacto: 4.833 (JCR 2018). Q1.

Sampaio-Dias IE, Silva-Reis SC, García-Mera X, Brea JM, Loza MI, Alves C, Algarra M, Rodríguez-Borges JE. Synthesis, Pharmacological and Biological Evaluation of MIF-1 Picolinoyl Peptidomimetics as Positive Allosteric Modulators of D2R. ACS Chem Neurosci. 2019 Jul 26. DOI: 10.1021/acschemneuro.9b00259. [Epub ahead of print]. ]. Indice de impacto: 2.802 (JCR 2018). Q3.

Areias F, Correia C, Rocha A, Brea J, Castro M, Loza MI, Proença MF, Carvalho MA. 2-Aryladenine derivatives as a potent scaffold for A₁, A₃ and dual A₁ /A₃ adenosine receptor antagonists: Synthesis and structure-activity relationships. Bioorg Med Chem. 2019 Jun 20. DOI: 10.1016/j.bmc.2019.06.034. [Epub ahead of print]. Indice de impacto: 2.802 (JCR 2018). Q3.

Magli E, Severino B, Corvino A, Perissutti E, Frecentese F, Saccone I, Giordano F, Castro M, Brea J, Loza MI, Santagada V, Caliendo G, Fiorino F. New Serotoninergic Ligands Containing Indolic and Methyl Indolic Nuclei: Synthesis and in Vitro Pharmacological Evaluation. Med Chem. 2019 Jun 13. DOI: 10.2174/1573406415666190613153220. [Epub ahead of print]

Martínez AL., Brea J., Monroy X., Merlos M., Burgueño J., Loza MI. A New Model of Sensorial Neuron-Like Cells for HTS of Novel Analgesics for Neuropathic Pain. SLAS Discov. 2019 Feb;24(2):158-168. DOI: 10.1177/2472555218810323. Epub 2018 Nov 1. Indice de impacto: 2.355 (JCR 2017)

Toro-Sazo M., Brea J., Loza MI., Cimadevila M., Cassels BK. 5-HT2 receptor binding, functional activity and selectivity in N-benzyltryptamines. PLoS One. 2019 Jan 10;14(1):e0209804. DOI: 10.1371/journal.pone.0209804. eCollection 2019. Indice de impacto: 2.776 (JCR 2018). Q2.

Brennecke P, Rasina D, Aubi O, Herzog K, Landskron J, Cautain B, Vicente F, Quintana J, Mestres J, Stechmann B, Ellinger B, Brea J, Kolanowski JL, Pilarski R, Orzaez M, Pineda-Lucena A, Laraia L, Nami F, Zielenkiewicz P, Paruch K, Hansen E, von Kries JP, Neuenschwander M, Specker E, Bartunek P, Simova S, Leśnikowski Z, Krauss S, Lehtiö L, Bilitewski U, Brönstrup M, Taskén K, Jirgensons A, Lickert H, Clausen MH, Andersen JH, Vicent MJ, Genilloud O, Martinez A, Nazaré M, Fecke W, Gribbon P. EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology. SLAS Discov. 2019 Jan 7:2472555218816276. doi: 10.1177/2472555218816276. [Epub ahead of print]. Indice de impacto: 2.355 (JCR 2017).

Martínez AL, Brea J, Monroy X, Merlos M, Burgueño J, Loza MI. A New Model of Sensorial Neuron-Like Cells for HTS of Novel Analgesics for Neuropathic Pain. SLAS Discov. 2018 Nov 1:2472555218810323. doi: 10.1177/2472555218810323.

Ruiz-De Diego I, Fasano S, Solís O, Garcia-Montes JR, Brea J, Loza MI, Brambilla R, Moratalla R. Genetic enhancement of Ras-ERK pathway does not aggravate L-DOPA-induced dyskinesia in mice but prevents the decrease induced by lovastatin. Sci Rep.2018 Oct 18;8(1):15381. doi: 10.1038/s41598-018-33713-3.

Da Silva-Candal A, Pérez-Díaz A, Santamaría M, Correa-Paz C, Rodríguez-Yáñez M, Ardá A, Pérez-Mato M, Iglesias-Rey R, Brea J, Azuaje J, Sotelo E, Sobrino T, Loza MI, Castillo J, Campos F. Clinical validation of blood/brain glutamate grabbing in acute ischemic stroke. Ann Neurol.doi: 10.1002/ana.25286. [Epub ahead of print]

Jaiteh M, Zeifman A, Saarinen M, Svenningsson P, Brea JM, Loza MI, Carlsson J. Docking screens for dual inhibitors of disparate drug targets for Parkinson's disease. J Med Chem. 2018 May 24. doi: 10.1021/acs.jmedchem.8b00204.

Ferreira da Costa J, Silva D, Caamaño O, Brea JM, Loza MI, Munteanu CR, Pazos A, García-Mera X, González-Díaz H. Perturbation Theory/Machine Learning Model of ChEMBL Data for Dopamine Targets: Docking, Synthesis, and Assay of New l-Prolyl-l-leucyl-glycinamide Peptidomimetics. ACS Chem Neurosci. 2018 May 23. doi: 10.1021/acschemneuro.8b00083.

Rataj K, Kelemen ÁA, Brea J, Loza MI, Bojarski AJ, Keserű GM. Fingerprint-Based Machine Learning Approach to Identify Potent and Selective 5-HT2BR Ligands. Molecules. 2018 May 10;23(5). pii: E1137. doi: 10.3390/molecules23051137

Nkizinkiko Y, Desantis J, Koivunen J, Haikarainen T, Murthy S, Sancineto L, Massari S, Ianni F, Obaji E, Loza MI, Pihlajaniemi T, Brea J, Tabarrini O, Lehtiö L. 2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors. Sci Rep. 2018 Jan 26;8(1):1680. doi: 10.1038/s41598-018-19872-3.

Miret-Casals L, Sebastián D, Brea J, Rico-Leo EM, Palacín M, Fernández-Salguero PM, Loza MI, Albericio F, Zorzano A. Identification of New Activators of Mitochondrial Fusion Reveals a Link between Mitochondrial Morphology and Pyrimidine Metabolism. Cell Chem Biol. 2017 Dec 23. pii: S2451-9456(17)30428-2. doi: 10.1016/j.chembiol.2017.12.001.

Kalash L, Val C, Azuaje J, Loza MI, Svensson F, Zoufir A, Mervin L, Ladds G, Brea J, Glen R, Sotelo E, Bender A. Computer-aided design of multi-target ligands at A1R, A2AR and PDE10A, key proteins in neurodegenerative diseases. J Med Chem. 2017 Nov 8. doi: 10.1021/acs.jmedchem.7b00994.

García Cárceles J, Decara JM, Vázquez-Villa H, Rodríguez R, Codesido E, Cruces J, Brea JM, Loza MI, Alén F, Botta J, McCormick PJ, Ballesteros JA, Benhamú B, Rodriguez de Fonseca F, López-Rodrí Guez ML. A Positive Allosteric Modulator of the Serotonin 5-HT2C Receptor for Obesity. J Med Chem. 2017 Nov 8. doi: 10.1021/acs.jmedchem.7b00994.

Iglesias A, Cimadevila M, la Fuente RA, Martí-Solano M, Cadavid MI, Castro M, Selent J, Loza MI, Brea J. Serotonin 2A receptor disulfide bridge integrity is crucial for ligand binding to different signalling states but not for its homodimerization. Eur J Pharmacol. 2017 Sep 9. pii: S0014-2999(17)30594-0. doi: 10.1016/j.ejphar.2017.09.011. [Epub ahead of print]

Azuaje J, López P, Iglesias A, de la Fuente RA, Pérez-Rubio JM, García D, Stepniewski TM, García-Mera X, Brea JM, Selent J, Pérez D, Castro M, Loza MI, Sotelo E. Development of Fluorescent Probes that Target Serotonin 5-HT2B Receptors. Sci Rep. 2017 Sep 7;7(1):10765. doi: 10.1038/s41598-017-11370-2.

García AM, Brea J, González-García A, Pérez C, Cadavid MI, Loza MI, Martinez A, Gil C. Targeting PDE10A GAF Domain with Small Molecules: A Way for Allosteric Modulation with Anti-Inflammatory Effects. Molecules. 2017 Sep 4;22(9). doi: 10.3390/molecules22091472.

Azuaje J, Jespers W, Yaziji V, Mallo A, Majellaro M, Caamaño O, Loza MI, Cadavid MI, Brea J, Åqvist J, Sotelo E, Gutiérrez-de-Terán H. Effect of Nitrogen Atom Substitution in A3 Adenosine Receptor Binding: N-(4,6-Diarylpyridin-2-yl)acetamides as Potent and Selective Antagonists. J Med Chem. 2017 Aug 21. doi: 10.1021/acs.jmedchem.7b00860.

García AM, Salado IG, Perez DI, Brea J, Morales-García JA, González-García A, Cadavid MI, Loza MI, Luque FJ, Perez-Castillo A, Martinez A, Gil C. Pharmacological tools based on imidazole scaffold proved the utility of PDE10A inhibitors for Parkinson's disease. Future Med Chem. 2017 May 9. doi: 10.4155/fmc-2017-0005.

Rodríguez-Vázquez N, García-Fandiño R, Aldegunde MJ, Brea J, Loza MI, Amorín M, Granja JR. cis-Platinum Complex Encapsulated in Self-Assembling Cyclic Peptide Dimers. Org Lett. 2017 May 4. doi: 10.1021/acs.orglett.7b00871.

Kumar R, Yadav N, Lavilla R, Blasi D, Quintana J, Brea JM, Loza MI, Mestres J, Bhandari M, Arora R, Kakkar R, Prasad AK. Synthesis, pharmacological evaluation and molecular docking of pyranopyrazole-linked 1,4-dihydropyridines as potent positive inotropes. Mol Divers. 2017 Apr 25. doi: 10.1007/s11030-017-9738-7.

Carbajales C, Azuaje J, Oliveira A, Loza MI, Brea JM, Cadavid MI, Masaguer CF, García-Mera X, Gutiérrez-de-Terán H, Sotelo E. Enantiospecific Recognition at the A2B Adenosine Receptor by Alkyl 2-Cyanoimino-4-substituted-6-methyl-1,2,3,4-tetrahydropyrimidine-5-carboxylates. J Med Chem. 2017 Apr 3. doi: 10.1021/acs.jmedchem.7b00138. [Epub ahead of print]

Iria Salvadó, Ilaria Gamba, Javier Montenegro, José Martínez-Costas, Jose Manuel Brea, María Isabel Loza, Miguel Vázquez López and M. Eugenio Vázquez Membrane-disrupting iridium(III) oligocationic organometallopeptides Med. Chem. Commun. 2016 Sept 21;52(73): 11008-11011. doi: 10.1039/C6CC05537K

Digles D, Zdrazil B, Neefs JM, Van Vlijmen H, Herhaus C, Caracoti A, Brea J, Roibás B, Loza MI, Queralt Rosinach N, Furlong L, Gaulton A, Bartek L, Senger S, Chi chester C, Engkvist O, Evelo C, Franklin NI, Marren D, Ecker G, Jacoby E. Open PHACTS Computational Protocols for in silico Target Validation of Cellular Phenotypic Screens: Knowing the Knowns Med. Chem. Commun. 2016 First published online 11 May 2016. doi: 10.1039/C6MD00065G

Iglesias A, Lage S, Cadavid MI, Loza MI, Brea J. Development of a Multiplex Assay for Studying Functional Selectivity of Human Serotonin 5-HT2A Receptors and Identification of Active Compounds by High-Throughput Screening J Biomol Screen. 2016 Apr 19. pii: 1087057116644162. doi: 10.1177/1087057116644162.

Gamba I, Salvadó I, Brissos RF, Gamez P, Brea J, Loza MI, Vázquez ME, López MV. High-affinity sequence-selective DNA binding by iridium(III) polypyridyl organometallopeptides Chem Commun (Camb). 2016 Jan 7;52(6):1234-7. doi: 10.1039/c5cc07619f.

Anton-Torrecillas, Loza MI, Brea J, Gonzalez-Gomez JC. Concise asymmetric syntheses of novel phenanthroquinolizidines. Org Biomol Chem. 2016 Jan 21. doi: 10.1039/C5OB02624E.

Van Voorhis WC, Adams JH, Adelfio R, Ahyong V, Akabas MH, Alano P, Alday A, Alemán Resto Y, Alsibaee A, Alzualde A, Andrews KT, Avery SV, Avery VM, Ayong L, Baker M, Baker S, Ben Mamoun C, Bhatia S, Bickle Q, Bounaadja L, Bowling T, Bosch J, Boucher LE, Boyom FF, Brea J, Brennan M, Burton A, Caffrey CR, Camarda G, Carrasquilla M, Carter D, Belen Cassera M, Chih-Chien Cheng K, Chindaudomsate W, Chubb A, Colon BL, Colón-López DD, Corbett Y, Crowther GJ, Cowan N, D'Alessandro S, Le Dang N, Delves M, DeRisi JL, Du AY, Duffy S, Abd El-Salam El-Sayed S, Ferdig MT, Fernández Robledo JA, Fidock DA, Florent I, Fokou PV, Galstian A, Gamo FJ, Gokool S, Gold B, Golub T, Goldgof GM, Guha R, Guiguemde WA, Gural N, Guy RK, Hansen MA, Hanson KK, Hemphill A, Hooft van Huijsduijnen R, Horii T, Horrocks P, Hughes TB, Huston C, Igarashi I, Ingram-Sieber K, Itoe MA, Jadhav A, Naranuntarat Jensen A, Jensen LT, Jiang RH, Kaiser A, Keiser J, Ketas T, Kicka S, Kim S, Kirk K, Kumar VP, Kyle DE, Lafuente MJ, Landfear S, Lee N, Lee S, Lehane AM, Li F, Little D, Liu L, Llinás M, Loza MI, Lubar A, Lucantoni L, Lucet I, Maes L, Mancama D, Mansour NR, March S, McGowan S, Medina Vera I, Meister S, Mercer L, Mestres J, Mfopa AN, Misra RN, Moon S, Moore JP, Morais Rodrigues da Costa F, Müller J, Muriana A, Nakazawa Hewitt S, Nare B, Nathan C, Narraidoo N, Nawaratna S, Ojo KK, Ortiz D, Panic G, Papadatos G, Parapini S, Patra K, Pham N, Prats S, Plouffe DM, Poulsen SA, Pradhan A, Quevedo C, Quinn RJ, Rice CA, Abdo Rizk M, Ruecker A, St Onge R, Salgado Ferreira R, Samra J, Robinett NG, Schlecht U, Schmitt M, Silva Villela F, Silvestrini F, Sinden R, Smith DA, Soldati T, Spitzmüller A, Stamm SM, Sullivan DJ, Sullivan W, Suresh S, Suzuki BM, Suzuki Y, Swamidass SJ, Taramelli D, Tchokouaha LR, Theron A, Thomas D, Tonissen KF, Townson S, Tripathi AK, Trofimov V, Udenze KO, Ullah I, Vallieres C, Vigil E, Vinetz JM, Voong Vinh P, Vu H, Watanabe NA, Weatherby K, White PM, Wilks AF, Winzeler EA, Wojcik E, Wree M, Wu W, Yokoyama N, Zollo PH, Abla N, Blasco B, Burrows J, Laleu B, Leroy D, Spangenberg T, Wells T, Willis PA. Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond. PLoS Pathog. 2016 Jul 28;12(7):e1005763. doi: 10.1371/journal.ppat.1005763.

Pau A, Catto M, Pinna G, Frau S, Murineddu G, Asproni B, Curzu MM, Pisani L, Leonetti F, Loza MI, Brea J, Pinna GA, Carotti A Multitarget-Directed Tricyclic Pyridazinones as G Protein-Coupled Receptor Ligands and Cholinesterase Inhibitors. ChemMedChem. 2015 Jun;10(6):1054-70. doi: 10.1002/cmdc.201500124.

Rodriguez A, Guerrero A, Gutierrez de Terán H, Rodriguez D, Brea J, Loza MI, Rosell G, Bosh MP. New selective A2A agonists and A3 antagonists for human adenosine receptors: synthesis, biological activity and molecular docking studies. MedChemComm. 2015. Advance Article. First published online: 13 May 2015. doi: 10.1039/C5MD00086F.

Ferreira da Costa J, García-Mera X, Caamaño O, Brea JM, Loza MI. Synthesis by microwave-assisted 1,3-dipolar cycloaddition of 1,2,3-triazole 1'-homo-3'-isoazanucleosides and evaluation of their anticancer activity. Eur J Med Chem. 2015;98:212-220. doi: 10.1016/j.ejmech.2015.05.029.

Anton-Torrecillas C, Bosque I, Gonzalez-Gomez JC, Loza MI, Brea J. Syntheses and cytotoxicity of (R)- and (s)-7-methoxycryptopleurine. J Org Chem. 2015;80(2):1284-90. doi: 10.1021/jo502660r.

Sabatini S1, Manfroni G, Barreca ML, Bauer SM, Gargaro M, Cannalire R, Astolfi A, Brea J, Vacca C, Pirro M, Massari S, Tabarrini O, Loza MI, Fallarino F, Laufer SA, Cecchetti V. The Pyrazolobenzothiazine Core as a New Chemotype of p38 Alpha Mitogen-Activated Protein Kinase Inhibitors. Chem Biol Drug Des. 2015. doi: 10.1111/cbdd.12516.

Varela MJ, Lage S, Caruncho HJ, Cadavid MI, Loza MI, Brea J. Reelin influences the expression and function of dopamine D2 and serotonin 5-HT2A receptors: A comparative study. Neuroscience. 2015;290:165-74. doi: 10.1016/j.neuroscience.2015.01.031.

Domínguez J, Fernández-Nieto F, Castro M, Catto M, Paleo MR, Porto S, Sardina FJ, Brea J, Carotti A, Villaverde MC, Sussman F. Computer Aided Structure Based Design of Multitarget Leads for Alzheimers Disease J Chem Inf Model. 55(1):135-48 (2015)

Martí-Solano M, Iglesias A, de Fabritiis G, Sanz F, Brea J, Loza MI, Pastor M, Selent J. Detection of new biased agonists for the serotonin 5-HT2A receptor: modeling and experimental validation. Mol Pharmacol. 2015;87(4):740-6. doi: 10.1124/mol.114.097022.

Ratnam J, Zdrazil B, Digles D, Cuadrado-Rodriguez E, Neefs JM, Tipney H, Siebes R, Waagmeester A, Bradley G, Chau CH, Richter L, Brea J, Evelo CT, Jacoby E, Senger S, Loza MI, Ecker GF, Chichester C. The Application of the Open Pharmacological Concepts Triple Store (Open PHACTS) to Support Drug Discovery Research. PLoS One. PLoS One. 2014 Dec 18;9(12). 1-32. doi: 10.1371/journal.pone.0115460

Garcia AM, Brea JM, Morales JA, Perez DI, González A, Alonso-Gil S, Gracia-Rubio I, Ros-Simó C, Conde S, Cadavid MI, Loza MI, Perez-Castillo A, Valverde O, Martinez A, Gil C. Modulation of cAMP specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors. J Med Chem. 2014;57(20):8590-607. doi: 10.1021/jm501090m.

Rodríguez D, Brea J, Loza MI, Carlsson J. Structure-Based Discovery of Selective Serotonin 5-HT1B Receptor Ligands. Structure. 2014;22(8):1140-51. doi: 10.1016/j.str.2014.05.017.

Selent J, Marti-Solano M, Rodríguez J, Atanes P, Brea J, Castro M, Sanz F, Loza MI, Pastor M. Novel insights on the structural determinants of clozapine and olanzapine multi-target binding profiles. Eur J Med Chem 2014;77:91-5. doi: 10.1016/j.ejmech.2014.02.058.

Bosque I, Gonzalez-Gomez JC, Loza MI, Brea J. Natural Tetraponerines: A General Synthesis and Antiproliferative Activity. J Org Chem. 2014;79 (9):3982–3991. doi: 10.1021/jo500446f

Cambón A, Brea J, Loza MI, Alvarez-Lorenzo C, Concheiro A, Barbosa S, Taboada P, Mosquera V. Cytocompatibility and P-glycoprotein inhibition of block copolymers: structure-activity relationship. Mol Pharm. 2013;10(8):3232-41. doi: 10.1021/mp4002848.

Redondo M, Soteras I, Brea J, González-García A, Cadavid MI, Loza MI, Martinez A, Gil C, Campillo NE. Unraveling phosphodiesterase surfaces. Identification of phosphodiesterase 7 allosteric modulation cavities. Eur J Med Chem. 2013;70:781-8. doi: 10.1016/j.ejmech.2013.10.035

Crespo A, El Maatougui A, Biagini P, Azuaje J, Coelho A, Brea J, Loza MI, Cadavid MI, Garcia-Mera X, Gutierrez de Terán H, Sotelo E. Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Pontent and Selective A(2B) Adenosine Receptor Antagonists. ASC Med Chem Lett. 2013;4(11): 1031-1036. doi:10.1021/ml400185v.

Carro L, Torrado M, Raviña E, Masaguer CF, Lage S, Brea J, Loza MI. Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands. Eur J Med Chem. 2013;71C:237-249. doi: 10.1016/j.ejmech.2013.10.066.

Ferreira da Costa J, Caamaño O, Fernández F, García-Mera X, Sampaio-Dias IE, Brea JM, Cadavid MI. Synthesis and allosteric modulation of the dopamine receptor by peptide analogs of L-prolyl-L-leucyl-glycinamide (PLG) modified in the L-proline or L-proline and L-leucine scaffolds. Eur J Med Chem. 2013;69:146-58. doi: 10.1016/j.ejmech.2013.08.001

Insua I, Alvarado M, Masaguer CF, Iglesias A, Brea J, Loza MI, Carro L. Synthesis and binding affinity of new 1,4-disubstituted triazoles as potential dopamine D(3) receptor ligands. Bioorg Med Chem Lett. 2013;23(20):5586-91. doi: 10.1016/j.bmcl.2013.08.047

Atanes P, Lacivita , Rodríguez J, Brea J, Burgueño J, Vela JM, Cadavid MI, Loza MI, Leopoldo M, Castro M. The arylpiperazine derivatives N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide (LP-211) and N-benzyl-4-(2-diphenyl)-1-piperazinehexanamide (MEL-9) exert a long-lasting inhibition of human serotonin 5-HT7 receptor binding. Pharmacology Research & Perspectives. 2013. doi: 10.1002/prp2.13.

Lozano MV, Lollo G, Alonso-Nocelo M, Brea J, Vidal A, Torres D, Alonso MJ. Polyarginine nanocapsules: a new platform for intracellular drug delivery. Journal of Nanoparticle Research. Journal of Nanoparticle Research. 2013; 15:1515. doi: 10.1007/s11051-013-1515-7.

Cambón A, Rey-Rico A, Mistry D, Brea J, Loza MI, Attwood D, Barbosa S, Alvarez-Lorenzo C, Concheiro A, Taboada P, Mosquera V. Doxorubicin-loaded micelles of reverse poly(butylene oxide)-poly(ethylene oxide)-poly(butylene oxide) block copolymers as efficient "active" chemotherapeutic agents. Int J Pharm. 2013;445(1-2):47-57. doi: 10.1016/j.ijpharm.2013.01.056.

Cambón A, Rey-Rico A, Barbosa S, Soltero JF, Yeates SG, Brea J, Loza MI, Alvarez-Lorenzo C, Concheiro A, Taboada P, Mosquera V. Poly(styrene oxide)-poly(ethylene oxide) block copolymers: From "classical" chemotherapeutic nanocarriers to active cell-response inducers. J Control Release. 2013;167(1):68-75. doi: 10.1016/j.jconrel.2013.01.010.

Yaziji V, Rodriguez D, Coelho A, García-Mera X, El Maatougui A, Brea J, Loza MI, Gutiérrez-de-Terán H, Sotelo E. Selective and potent adenosine A (3) receptor antagonists by methoxyaryl substitution on the N-(2,6-diarylpyrimidin-4-yl) acetamide scaffold. Eur J Med Chem. 2013;59:235-42. doi: 10.1016/j.ejmech.2012.11.010.

Lozano MV, Esteban H, Brea J, Loza MI, Torres D, Alonso MJ. Intracellular delivery of docetaxel using freeze-dried polysaccharide nanocapsules. J Microencapsul. 2013;30(2):181-8. doi: 10.3109/02652048.2012.714411.

Areias F, Costa M, Castro M, Brea J, Gregori-Puigjané E, Proença MF, Mestres J, Loza MI. New chromene scaffolds for adenosine A(2A) receptors: Synthesis, pharmacology and structure-activity relationships. Eur J Med Chem. 2012;54:303-10. doi: 10.1016/j.ejmech.2012.05.009.

Redondo M, Palomo V, Brea J, Pérez DI, Martín-Álvarez R, Pérez C, Paúl-Fernández N, Conde S, Cadavid MI, Loza MI, Mengod G, Martínez A, Gil C, Campillo NE. Identification in silico and experimental validation of novel phosphodiesterase 7 inhibitors with efficacy in experimental autoimmune encephalomyelitis mice. ACS Chem Neurosci. 2012;3(10):793-803. doi: 10.1021/cn300105c.

Redondo M, Brea J, Perez DI, Soteras I, Val C, Perez C, Morales-García JA, Alonso-Gil S, Paul-Fernandez N, Martin-Alvarez R, Cadavid MI, Loza MI, Perez-Castillo A, Mengod G, Campillo NE, Martinez A, Gil C. Effect of phosphodiesterase 7 (PDE7) inhibitors in experimental autoimmune encephalomyelitis mice. Discovery of a new chemically diverse family of compounds. J Med Chem. 2012;55(7):3274-84. doi: 10.1021/jm201720d.

Oyarzun-Ampuero FA, Brea J, Loza MI, Alonso MJ, Torres D. A potential nanomedicine consisting of heparin-loaded polysaccharide nanocarriers for the treatment of asthma. Macromol Biosci. 2012;12(2):176-83. doi: 10.1002/mabi.201100102.

Redondo M, Zarruk JG, Ceballos P, Pérez DI, Pérez C, Perez-Castillo A, Moro MA, Brea J, Val C, Cadavid MI, Loza MI, Campillo NE, Martínez A, Gil C. Neuroprotective efficacy of quinazoline type phosphodiesterase 7 inhibitors in cellular cultures and experimental stroke model. Eur J Med Chem. 2012;47(1):175-85. doi: 10.1016/j.ejmech.2011.10.040.

Barcelo M, Raviña E, Varela MJ, Brea J, Loza MI, Massager CF. Potential atypical antipsychotics: synthesis, binding affinity and SAR of new heterocyclic bioisosteric butyrophenone analogues as multitarget ligands. Med. Chem. Commun. 2011; 2(12):1194-1200. doi: 10.1039/C1MD00202C.

Varela MJ, Brea J, Loza MI, Maldonado R, Robledo P. Sensitization to MDMA locomotor effects and changes in the functionality of 5-HT2A and D2 receptors in mice. Behavioural Pharmacology. August 2011 - Volume 22 - Issue 4 - p 362–369. doi: 10.1097/FBP.0b013e3283487346

Costa M, Areias F, Castro M, Brea J, Loza MI, Proença F. Synthesis of novel chromene scaffolds for adenosine receptors. Org Biomol Chem. 2011;9(11):4242-9. doi: 10.1039/c1ob05305a.

Yaziji V, Rodríguez D, Gutiérrez deTerán H, Coelho A, Caamaño O, García-Mera X, Brea J, Loza MI, Cadavid MI, Sotelo E. Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem 2011;54(2):457-71. doi: 10.1021/jm100843z.

Alvarez-Lorenzo C, Rey-Rico A, Brea J, Loza MI, Concheiro A, Sosnik A. Inhibition of P-glycoprotein pumps by PEO-PPO amphiphiles: branched versus linear derivatives. Nanomedicine (Lond)2010;5(9):1371-83. doi: 10.2217/nnm.10.53.

Lopez L, Selent J, Ortega R, Masaguer CF, Domínguez E, Areias F, Brea J, Loza MI, Sanz F, Pastor M. Synthesis, 3D-QSAR, and Structural Modeling of Benzolactam Derivatives with Binding Affinity for the D2 and D3 Receptors. ChemMedChem. 2010;5(8):1300-17. doi: 10.1002/cmdc.201000101.

Jenkins L, Brea J, Smith NJ, Hudson BD, Reilly G, Bryant NJ, Castro M, Loza MI, Milligan G. Identification of novel, species selective agonists of the G protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα 13. Biochem J. 2010; 432:51–459. doi:10.1042/BJ20101287.

Trifirò G, Gambassi G, Sen EF, Caputi AP, Bagnardi V, Brea J, Sturkenboom MC. Association of community-acquired pneumonia with antipsychotic drug use in elderly patients: a nested case-control study. Ann Intern Med. 2010;152(7):418-25. doi:10.7326/0003-4819-152-7-201004060-00006

Rodríguez-Borges JE, García-Mera X, Balo MC, Brea J, Caamaño O, Fernández F, López C, Loza MI, Nieto MI. Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists. Bioorg Med Chem. 2010;18(5):2001-9. doi: 10.1016/j.bmc.2010.01.028.

Varin T, Gutiérrez-de-Terán H, Castro M, Brea J, Fabis F, Dauphin F, Aqvist J, Lepailleur A, Perez P, Burgueño J, Vela JM, Loza MI, Rodrigo J. Phe369(7.38) at human 5-HT(7) receptors confers interspecies selectivity to antagonists and partial agonists. Br J Pharmacol. 2010;159(5):1069-81. doi: 10.1111/j.1476-5381.2009.00481.x.

Nieto MI, Balo MC, Brea J, Caamaño O, Fernández F, García-Mera X, López C, Loza MI, Rodríguez-Borges JE, Vidal B. Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists. Eur J Med Chem. 2010;45(7):2884-92. doi: 10.1016/j.ejmech.2010.03.011

Areias FM, Brea J, Gregori-Puigjané E, Zaki ME, Carvalho MA, Domínguez E, Gutiérrez-de-Terán H, Proença MF, Loza MI, Mestres J. In silico directed chemical probing of the adenosine receptor family. Bioorg Med Chem. 2010;18(9):3043-52. doi: 10.1016/j.bmc.2010.03.048.

Brea J, Castro-Palomino J, Yeste S, Cubero E, Párraga A, Domínguez E, Loza MI. Emerging opportunities and concerns for drug discovery at serotonin 5-HT2B receptors. Curr Top Med Chem. 2010;10(5):493-503. In Press.

Hierrezuelo J, Manuel López-Romero J, Rico R, Brea J, Isabel Loza M, Cai C, Algarra M. Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. Bioorg Med Chem. 2010;18(6):2081-8. doi: 10.1016/j.bmc.2010.02.014.

Yaziji V, Coelho A, El Maatougui A, Brea J, Loza MI, García-Mera X, Sotelo E. Divergent solution-phase síntesis of diarylpyrimidine libraries as selective A3 adenosine receptor antagonists. J. Com. Chem. 2009;11(4):519-22. doi: 10.1021/cc900044k.

Nieto MI, Balo MC, Brea J, Caamaño O, Cadavid MI, Fernández F, Mera XG, López C, Rodríguez-Borges JE. Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A(2B) receptor antagonists. Bioorg Med Chem. 2009;17(9):3426-32. doi: 10.1016/j.bmc.2009.03.029.

Fernández F, Caamaño O, Isabel Nieto M, López C, García-Mera X, Stefanachi A, Nicolotti O, Isabel Loza M, Brea J, Esteve C, Segarra V, Vidal B, Carotti A. 1,3-Dialkyl-8-N-substituted benzyloxycarbonylamino-9-deazaxanthines as potente adenosine receptor ligands: Design, synthesis, structure-affinity and structure-selectivity relationships. Bioorg Med Chem. 2009; 15;17(10):3618-29. doi: 10.1016/j.bmc.2009.03.062

Carro L, Raviña E, Dominguez E, Brea J, Loza MI, F. Masaguer C. Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif Bioorganic and Medicinal Chemistry Letters. 2009;19(21):6059-6062. doi: 10.1016/j.bmcl.2009.09.041.

Varin T1, Gutiérrez-de-Terán H, Castro M, Brea J, Fabis F, Dauphin F, Aqvist J, Lepailleur A, Perez P, Burgueño J, Vela JM, Loza MI, Rodrigo J. Phe369(7.38) at human 5-HT7 receptors confers interspecies selectivity to antagonists and partial agonists. Br J Pharmacol. 2010;159(5):1069-81. doi: 10.1111/j.1476-5381.2009.00481.x.

Balo MC, Brea J, Caamaño O, Fernández F, García-Mera X, López C, Loza MI, Nieto MI, Rodríguez-Borges JE. Synthesis and pharmacological evaluation of novel 1- and 8-substituted-3-furfurylxanthines as adenosine receptor antagonists. Bioorg Med Chem. 2009;17(18):6755-60. doi: 10.1016/j.bmc.2009.07.034.

Oyarzun-Ampuero FA, Brea J, Loza MI, Torres D, Alonso MJ. Chitosan-hyaluronic acid nanoparticles loaded with heparin for the treatment of asthma. Int J Pharm. 2009;381(2):122-9. doi: 10.1016/j.ijpharm.2009.04.009.

Gutierrez-de-Teran H, Correia C, Rodriguez D, Carvalho MA, Brea J, Cadavid MI, Loza MI, Proenca MF, Areias F. Identification of Novel Scaffolds from an Original Chemical Library as Potential Antipsychotics. QSAR Comb. Sci. 2009;28(8): 856 – 860. doi: 10.1002/qsar.200860198.

Brea J, Castro M, Giraldo J, Lopez-Gimenez JF, Padin JF, Quintian F, Cadavid MI, Vilaro T, Mengod G, Berg KA, Clarke WP, Vilardaga JP, Milligan G, Loza MI. Evidence for distinct antagonist-revealed functional states of 5-HT2A receptor homodimers. Mol Pharmacol. 2009;75(6):1380-91. doi: 10.1124/mol.108.054395.

Ortega R, Raviña E, Masaguer CF, Areias F, Brea J, Loza MI, López L, Selent J, Pastor M, Sanz F. Synthesis, Binding Affinity and SAR of New Benzolactam Derivatives as Dopamine D3 Receptor Ligands. Bioorg Med Chem Lett. 2009;15;19(6):1773-8. doi: 10.1016/j.bmcl.2009.01.067

Laguna R, Cadavid MI, Castro M, Brea JM, Loza MI. La experiencia de 10 años de docencia de la asignatura "Fuentes de Información Farmacológica de Medicamentos" impartida con el método de enseñanza basado en la resolución de problemas. Revista d'educació superior en Farmacia. 2008; nº 4. In Press

Stefanachi A, Nicolotti O, Leonetti F, Cellamare S, Campagna F, Loza MI, Brea JM, Mazza F, Gavuzzo E, Carotti A. 1,3-Dialkyl-8-(hetero)aryl-9-OH-9-deazaxanthines as potent A(2B) adenosine receptor antagonists: Design, synthesis, structure-affinity and structure-selectivity relationships. Bioorg Med Chem. 2008;16(22):9780-9. doi: 10.1016/j.bmc.2008.09.067.

Aranda R, Villalba K, Raviña E, Masaguer CF, Brea J, Areias F, Domínguez E, Selent J, López L, Sanz F, Pastor M, Loza MI. Synthesis, Binding Affinity, and Molecular Docking Analysis of New Benzofuranone Derivatives as Potential Antipsychotics. Journal of Medicinal Chemistry. 2008;51(19):6085-94. doi: 10.1021/jm800602w.

Buceta M, Dominguez E, Castro MA, Brea JM, Alvarez D, Barcala J, Valdés L, Alvarez-Calderón P, Domínguez F, Vidal B, Dí az JL, Miralpeix M, Beleta J, Cadavid MI, Loza MI. A new Chemicals tool (C0036E08) supports the role of adenosine A2B receptors in mediating human mast cell activation. Biochemical Pharmacology. 2008;76(7):912-21. doi: 10.1016/j.bcp.2008.07.011.

Rico-Gómez R, López-Romero JM, Hierrezuelo J, Brea J, Loza MI, Pérez-González M. Synthesis of new mannosyl, galactosyl and glucosyl theophylline nucleosides with potential activity as antagonists of adenosine receptors. DEMA-induced cyclization of glycosylideneiminouracils. Carbohydr Res. 2008;343:855-864. doi: 10.1016/j.carres.2008.01.011

Stefanachi A, Brea JM, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, Nieto R, Raviña E, Sanz F, Segarra V, Sotelo E, Vidal B, Carotti A. 1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A(2B) adenosine receptor. Bioorg Med Chem. 2008;16(6):2852-69. doi: 10.1016/j.bmc.2008.01.002

Martínez A, Gutiérrez-de-Terán H, Brea J, Raviña E, Loza MI, Cadavid MI, Sanz F, Vidal B, Segarra V, Sotelo E. Synthesis, adenosine receptor binding and 3D-QSAR of 4-substituted 2-(2'-furyl)-1,2,4-triazolo[1,5-a]quinoxalines. Bioorg Med Chem. 2008;16(4):2103-13. doi: 10.1016/j.bmc.2007.10.103.

Barceló M, Raviña E, Masaguer C, Dominguez E, Areias F, Brea JM, Loza MI. Synthesis and Binding Affinity of New Pyrazole and Isoxazole Derivatives as Potential Atypical Antipsychotics. Bioorg Med Chem Lett. 2007;1;17(17):4873-7. In Press.

Balo C, Lopez C, Brea JM, Fernande F, Caamano O. Synthesis and Evaluation of Adenosine Antagonist Activity of a Series of [1,2,4]Triazolo[1,5-c]quinazolines. Chem Pharm Bull (Tokyo). 2007;55(3):372-5. doi: 10.1248/cpb.55.372

Dezi C, Brea J, Alvarado M, Raviña E, Masaguer C, Loza MI, Sanz F, Pastor M. Multi-structure 3D-QSAR studies on a series of conformationally constrained butyrophenones docked into a new homology model of the 5-HT2A receptor. Journal of Medicinal Chemistry. 2007;12;50(14):3242-55. doi: 10.1021/jm070277a.

Padín JF, Rodríguez MA, Domínguez E, Dopeso-Reyes IG; Buceta M; Cano E; Sotelo E, Brea J, Caruncho HJ; Cadavid MI, Castro MA; Loza MI. Parallel regulation by olanzapine of the patterns of expression of 5-ht2a and d3 receptors in rat central nervous system and blood cells. Neuropharmacology. 2006;51(4):923-32. doi: 10.1016/j.neuropharm.2006.06.005.

Brea J, Castro M, Loza MI, Masaguer CF, Ravina E, Dezi C, Pastor M, Sanz F, Cabrero-Castel A, Galan-Rodriguez B, Fernandez-Espejo E, Maldonado R, Robledo P. QF2004B, a potential antipsychotic butyrophenone derivative with similar pharmacological properties to clozapine. Neuropharmacology. 2006;51(2):251-62. doi: 10.1016/j.neuropharm.2006.03.021.

Alvarado M, Coelho A, Masaguer CF, Raviña E, Brea J, Padín JF, Loza MI. Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics. Bioorganic & Medicinal Chemistry Letters. 2005;15(12):3063-6. doi: 10.1016/j.bmcl.2005.04.022

Bosch MP, Campos F, Niubó I, Rosell G, Díaz JL, Brea JM, Loza MI, Guerrero A. Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor. Journal of Medicinal Chemistry. 2004;47(16):4041-53. doi: 10.1021/jm031143.

Caro Y, Torrado M, Masaguer CG, Raviña E, Padín F, Brea J, Loza MI. Chemoenzymatic syntesis and binding affinity of novel (R)- and S)-3-aminomethyl-1-tetralones, potencial atypical antipsychotics. Bioorgaic & Medicinal Che mistry Letters. 2004;14:585-589. doi: 10.1016/j.bmcl.2003.11.064.

Villazón, M, Enguix MJ, Tristán H, Honrubia MA, Brea J, Maayani S, Cadavid MI, Loza MI. Different pharmacological properties of two equipotent antagonists (clozapine and rauwolscine) for 5-HT2B receptors in rat stomach fundus. Biochemical Pharmacology. 2003;66(6):927-937. doi: 10.1016/S0006-2952(03)00426-X.

Enguix MJ, Sánchez L, Villazón M, Brea J, Tristán H, Cadavid MI, Loza MI. Differential regulation of rat peripheral 5-HT2A and 5-HT receptors systems: influence of drug treatment. Naunyn-Schmiedeberg's archives of pharmacology. 2003;368(2):79-90. doi: 10.1007/s00210-003-0775-7.

Brea J, Masaguer F, Villazón M, Cadavid MI, Raviña E, Fontaine F, Dezi C, Pastor M, Sanz F, Loza MI. Conformationally constrained butyrophenones as new pharmacological tools to study 5-HT2A and 5-HT2C receptor behaviorus. European Journal of Medicinal Chemistry. 2003;38(4):433-440. doi: 10.1016/S0223-5234(03)00054-0.

González-Gómez JC, Santana L, Uriarte E, Brea J, Villazón, Loza MI, De Luca M, Rivas ME, Montenegro GY, Fontenla JA. New arylpiperazine derivatives with higt affinity for Alpha1A, D2 and 5-HT2A receptors. Bioorganic & Medicinal Chemistry Letters. 2003;13(2):175-178. doi: 10.1016/S0960-894X(02)00933-2.

Brea J, Rodrigo J, Carrieri A, Sanz F, Cadavid MI, Enguix M, Villazón M, Mengod G, Caro Y, Massaguer CF, Raviña E, Centeno NB, Carotti A, Loza MI. New serotonina 5-HT2A, 5-HT2B and 5-HT2C receptor antagonists: synthesis, pharmacology, 3D QSAR and molecular modelling of (aminoakyl) benzo and heterocycloalkanones. Journal of Medicinal Chemistry. 2002;45(1):54-71. doi: 10.1021/jm011014y

Sotelo E, Fraiz N, Yáñez M, Laguna R, Cano E, Brea J, Raviña E. 5-alkylidene-6-phenyl-3(2H)-pyridazinones a new family of platelet aggregation inhibitors. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1575-7. doi:10.1016/S0960-894X(02)00246-9

López-Jiménez JF, Villazón M, Brea J, Loza MI, Palacios JM, Mengod G, Vilaró MT Múltiple conformations of native and recombinant human 5-HT2A receptors are labeled agonists and discriminated by antagonists. Mol Pharmacol. 2001 Oct;60(4):690-9.

Masaguer CF, Raviña E, Fontenla JA, Brea JM, Tristán H, Loza MI. Butyrophenone analogues in the carbazole series as potential atypical antipsychotic. Synthesis and determination of affinities at D; 5-HT2A and 5-HT2c receptors Eur J Med Chem. 2000 Jan;35(1):83-95. doi:10.1016/S0223-5234(00)00109-4