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Page 1
mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome.
Gogliotti RG, Senter RK, Rook JM, Ghoshal A, Zamorano R, Malosh C, Stauffer SR, Bridges TM, Bartolome JM, Daniels JS, Jones CK, Lindsley CW, Conn PJ, Niswender CM. Gogliotti RG, et al. Among authors: bartolome jm. Hum Mol Genet. 2016 May 15;25(10):1990-2004. doi: 10.1093/hmg/ddw074. Epub 2016 Mar 2. Hum Mol Genet. 2016. PMID: 26936821 Free PMC article.
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.
Manka JT, Vinson PN, Gregory KJ, Zhou Y, Williams R, Gogi K, Days E, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Manka JT, et al. Among authors: bartolome jm. Bioorg Med Chem Lett. 2012 Oct 15;22(20):6481-5. doi: 10.1016/j.bmcl.2012.08.043. Epub 2012 Aug 24. Bioorg Med Chem Lett. 2012. PMID: 22981332 Free PMC article.
Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.
Rodriguez AL, Zhou Y, Williams R, Weaver CD, Vinson PN, Dawson ES, Steckler T, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Rodriguez AL, et al. Among authors: bartolome jm. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7388-92. doi: 10.1016/j.bmcl.2012.10.068. Epub 2012 Oct 23. Bioorg Med Chem Lett. 2012. PMID: 23142615 Free PMC article.
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: bartolome jm. 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.
Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: in vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions.
Blobaum AL, Bridges TM, Byers FW, Turlington ML, Mattmann ME, Morrison RD, Mackie C, Lavreysen H, Bartolomé JM, Macdonald GJ, Steckler T, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR, Daniels JS. Blobaum AL, et al. Among authors: bartolome jm. Drug Metab Dispos. 2013 Dec;41(12):2066-75. doi: 10.1124/dmd.113.052662. Epub 2013 Sep 3. Drug Metab Dispos. 2013. PMID: 24003250 Free PMC article.
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