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567 results

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Page 1
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: alcazar j. 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: alcazar j. 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 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
Cid JM, Tresadern G, Duvey G, Lütjens R, Finn T, Rocher JP, Poli S, Vega JA, de Lucas AI, Matesanz E, Linares ML, Andrés JI, Alcazar J, Alonso JM, Macdonald GJ, Oehlrich D, Lavreysen H, Ahnaou A, Drinkenburg W, Mackie C, Pype S, Gallacher D, Trabanco AA. Cid JM, et al. Among authors: alcazar j. J Med Chem. 2014 Aug 14;57(15):6495-512. doi: 10.1021/jm500496m. Epub 2014 Jul 28. J Med Chem. 2014. PMID: 25032784
Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents.
Rook JM, Xiang Z, Lv X, Ghoshal A, Dickerson JW, Bridges TM, Johnson KA, Foster DJ, Gregory KJ, Vinson PN, Thompson AD, Byun N, Collier RL, Bubser M, Nedelcovych MT, Gould RW, Stauffer SR, Daniels JS, Niswender CM, Lavreysen H, Mackie C, Conde-Ceide S, Alcazar J, Bartolomé-Nebreda JM, Macdonald GJ, Talpos JC, Steckler T, Jones CK, Lindsley CW, Conn PJ. Rook JM, et al. Among authors: alcazar j. Neuron. 2015 May 20;86(4):1029-1040. doi: 10.1016/j.neuron.2015.03.063. Epub 2015 Apr 30. Neuron. 2015. PMID: 25937172 Free PMC article.
Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.
Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Garcia-Barrantes PM, Lavreysen H, Mackie C, Vinson PN, Rook JM, Bridges TM, Daniels JS, Megens A, Langlois X, Drinkenburg WH, Ahnaou A, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Conde-Ceide S, et al. Among authors: alcazar j. ACS Med Chem Lett. 2015 May 20;6(6):716-20. doi: 10.1021/acsmedchemlett.5b00181. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26157544 Free PMC article.
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.
Zhou Y, Malosh C, Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW. Zhou Y, et al. Among authors: alcazar j. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3515-9. doi: 10.1016/j.bmcl.2015.06.096. Epub 2015 Jul 4. Bioorg Med Chem Lett. 2015. PMID: 26183084 Free PMC article.
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.
Conde-Ceide S, Alcázar J, Alonso de Diego SA, López S, Martín-Martín ML, Martínez-Viturro CM, Pena MA, Tong HM, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Lindsley CW, Bartolomé-Nebreda JM. Conde-Ceide S, et al. Among authors: alcazar j. Bioorg Med Chem Lett. 2016 Jan 15;26(2):429-434. doi: 10.1016/j.bmcl.2015.11.098. Epub 2015 Nov 28. Bioorg Med Chem Lett. 2016. PMID: 26684851 Free PMC article.
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.
Andrés JI, Alcázar J, Alonso JM, Díaz A, Fernández J, Gil P, Iturrino L, Matesanz E, Meert TF, Megens A, Sipido VK. Andrés JI, et al. Among authors: alcazar j. Bioorg Med Chem Lett. 2002 Jan 21;12(2):243-8. doi: 10.1016/s0960-894x(01)00721-1. Bioorg Med Chem Lett. 2002. PMID: 11755364
567 results