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Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.
Abe M, Seto M, Gogliotti RG, Loch MT, Bollinger KA, Chang S, Engelberg EM, Luscombe VB, Harp JM, Bubser M, Engers DW, Jones CK, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Abe M, et al. ACS Med Chem Lett. 2017 Sep 1;8(10):1110-1115. doi: 10.1021/acsmedchemlett.7b00317. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057060 Free PMC article.
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. 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.