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Page 1
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
Cid JM, Tresadern G, Vega JA, de Lucas AI, Del Cerro A, Matesanz E, Linares ML, García A, Iturrino L, Pérez-Benito L, Macdonald GJ, Oehlrich D, Lavreysen H, Peeters L, Ceusters M, Ahnaou A, Drinkenburg W, Mackie C, Somers M, Trabanco AA. Cid JM, et al. Among authors: iturrino l. J Med Chem. 2016 Sep 22;59(18):8495-507. doi: 10.1021/acs.jmedchem.6b00913. Epub 2016 Sep 9. J Med Chem. 2016. PMID: 27579727
Synthesis, evaluation, and radiolabeling of new potent positive allosteric modulators of the metabotropic glutamate receptor 2 as potential tracers for positron emission tomography imaging.
Andrés JI, Alcázar J, Cid JM, De Angelis M, Iturrino L, Langlois X, Lavreysen H, Trabanco AA, Celen S, Bormans G. Andrés JI, et al. Among authors: iturrino l. J Med Chem. 2012 Oct 25;55(20):8685-99. doi: 10.1021/jm300912k. Epub 2012 Oct 11. J Med Chem. 2012. PMID: 22992024
Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor.
Cid JM, Tresadern G, Vega JA, de Lucas AI, Matesanz E, Iturrino L, Linares ML, Garcia A, Andrés JI, Macdonald GJ, Oehlrich D, Lavreysen H, Megens A, Ahnaou A, Drinkenburg W, Mackie C, Pype S, Gallacher D, Trabanco AA. Cid JM, et al. Among authors: iturrino l. J Med Chem. 2012 Oct 25;55(20):8770-89. doi: 10.1021/jm3010724. Epub 2012 Oct 16. J Med Chem. 2012. PMID: 23072213
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.
Bartolomé-Nebreda JM, Conde-Ceide S, Delgado F, Iturrino L, Pastor J, Pena MÁ, Trabanco AA, Tresadern G, Wassvik CM, Stauffer SR, Jadhav S, Gogi K, Vinson PN, Noetzel MJ, Days E, Weaver CD, Lindsley CW, Niswender CM, Jones CK, Conn PJ, Rombouts F, Lavreysen H, Macdonald GJ, Mackie C, Steckler T. Bartolomé-Nebreda JM, et al. Among authors: iturrino l. J Med Chem. 2013 Sep 26;56(18):7243-59. doi: 10.1021/jm400650w. Epub 2013 Sep 4. J Med Chem. 2013. PMID: 23947773 Free PMC article.
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Andrés JI, Alcázar J, Alonso JM, Alvarez RM, Bakker MH, Biesmans I, Cid JM, De Lucas AI, Fernández J, Font LM, Hens KA, Iturrino L, Lenaerts I, Martínez S, Megens AA, Pastor J, Vermote PC, Steckler T. Andrés JI, et al. Among authors: iturrino l. J Med Chem. 2005 Mar 24;48(6):2054-71. doi: 10.1021/jm049619s. J Med Chem. 2005. PMID: 15771448
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Andrés JI, Alcázar J, Alonso JM, Alvarez RM, Bakker MH, Biesmans I, Cid JM, De Lucas AI, Drinkenburg W, Fernández J, Font LM, Iturrino L, Langlois X, Lenaerts I, Martínez S, Megens AA, Pastor J, Pullan S, Steckler T. Andrés JI, et al. Among authors: iturrino l. Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. doi: 10.1016/j.bmc.2007.03.053. Epub 2007 Mar 21. Bioorg Med Chem. 2007. PMID: 17407815
Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
Bartolomé-Nebreda JM, Delgado F, Martín-Martín ML, Martínez-Viturro CM, Pastor J, Tong HM, Iturrino L, Macdonald GJ, Sanderson W, Megens A, Langlois X, Somers M, Vanhoof G, Conde-Ceide S. Bartolomé-Nebreda JM, et al. Among authors: iturrino l. J Med Chem. 2014 May 22;57(10):4196-212. doi: 10.1021/jm500073h. Epub 2014 May 9. J Med Chem. 2014. PMID: 24758746
Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists.
Cid J, Alonso JM, Andrés JI, Fernández J, Gil P, Iturrino L, Matesanz E, Meert TF, Megens A, Sipido VK, Trabanco AA. Cid J, et al. Among authors: iturrino l. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2765-71. doi: 10.1016/j.bmcl.2004.03.069. Bioorg Med Chem Lett. 2004. PMID: 15125929
4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.
Trabanco AA, Pullan S, Alonso JM, Alvarez RM, Andrés JI, Boeckx I, Fernández J, Gómez A, Iturrino L, Janssens FE, Leenaerts JE, De Lucas AI, Matesanz E, Meert T, Steckler T. Trabanco AA, et al. Among authors: iturrino l. Bioorg Med Chem Lett. 2006 Jan 1;16(1):146-9. doi: 10.1016/j.bmcl.2005.09.025. Epub 2005 Oct 19. Bioorg Med Chem Lett. 2006. PMID: 16236510
24 results