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Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782.
Lavreysen H, Langlois X, Ahnaou A, Drinkenburg W, te Riele P, Biesmans I, Van der Linden I, Peeters L, Megens A, Wintmolders C, Cid JM, Trabanco AA, Andrés JI, Dautzenberg FM, Lütjens R, Macdonald G, Atack JR. Lavreysen H, et al. Among authors: macdonald g. J Pharmacol Exp Ther. 2013 Sep;346(3):514-27. doi: 10.1124/jpet.113.204990. Epub 2013 Jun 13. J Pharmacol Exp Ther. 2013. PMID: 23766542
N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.
Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, Macdonald GJ, Bartolomé JM, Mackie C, Hrupka BJ, Caron MG, Daigle TL, Lindsley CW, Conn PJ, Jones CK. Gregory KJ, et al. Among authors: macdonald gj. J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. doi: 10.1124/jpet.113.206623. Epub 2013 Aug 21. J Pharmacol Exp Ther. 2013. PMID: 23965381 Free PMC article.
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: macdonald gj. J Med Chem. 2012 Oct 25;55(20):8770-89. doi: 10.1021/jm3010724. Epub 2012 Oct 16. J Med Chem. 2012. PMID: 23072213
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. 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.
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: macdonald gj. 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
Translational neurophysiological markers for activity of the metabotropic glutamate receptor (mGluR2) modulator JNJ-40411813: Sleep EEG correlates in rodents and healthy men.
Ahnaou A, de Boer P, Lavreysen H, Huysmans H, Sinha V, Raeymaekers L, Van De Casteele T, Cid JM, Van Nueten L, Macdonald GJ, Kemp JA, Drinkenburg WH. Ahnaou A, et al. Among authors: macdonald gj. Neuropharmacology. 2016 Apr;103:290-305. doi: 10.1016/j.neuropharm.2015.11.031. Epub 2015 Dec 12. Neuropharmacology. 2016. PMID: 26686390
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: macdonald gj. J Med Chem. 2014 May 22;57(10):4196-212. doi: 10.1021/jm500073h. Epub 2014 May 9. J Med Chem. 2014. PMID: 24758746
Identification of a novel orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor with efficacy in animal models of schizophrenia.
Bartolomé-Nebreda JM, Alonso de Diego SA, Artola M, Delgado F, Delgado Ó, Martín-Martín ML, Martínez-Viturro CM, Pena MÁ, Tong HM, Van Gool M, Alonso JM, Fontana A, Macdonald GJ, Megens A, Langlois X, Somers M, Vanhoof G, Conde-Ceide S. Bartolomé-Nebreda JM, et al. Among authors: macdonald gj. J Med Chem. 2015 Jan 22;58(2):978-93. doi: 10.1021/jm501651a. Epub 2015 Jan 12. J Med Chem. 2015. PMID: 25495129
997 results