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110 results

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Page 1
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.
Chopko TC, Han C, Gregro AR, Engers DW, Felts AS, Poslusney MS, Bollinger KA, Morrison RD, Bubser M, Lamsal A, Luscombe VB, Cho HP, Schnetz-Boutaud NC, Rodriguez AL, Chang S, Daniels JS, Stec DF, Niswender CM, Jones CK, Wood MR, Wood MW, Duggan ME, Brandon NJ, Conn PJ, Bridges TM, Lindsley CW, Melancon BJ. Chopko TC, et al. Among authors: morrison rd. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2224-2228. doi: 10.1016/j.bmcl.2019.06.032. Epub 2019 Jun 20. Bioorg Med Chem Lett. 2019. PMID: 31248774 Free PMC article.
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.
Melancon BJ, Lamers AP, Bridges TM, Sulikowski GA, Utley TJ, Sheffler DJ, Noetzel MJ, Morrison RD, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Among authors: morrison rd. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1044-8. doi: 10.1016/j.bmcl.2011.11.110. Epub 2011 Dec 6. Bioorg Med Chem Lett. 2012. PMID: 22197142 Free PMC article.
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.
Melancon BJ, Gogliotti RD, Tarr JC, Saleh SA, Chauder BA, Lebois EP, Cho HP, Utley TJ, Sheffler DJ, Bridges TM, Morrison RD, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Among authors: morrison rd. Bioorg Med Chem Lett. 2012 May 15;22(10):3467-72. doi: 10.1016/j.bmcl.2012.03.088. Epub 2012 Mar 29. Bioorg Med Chem Lett. 2012. PMID: 22507963 Free PMC article.
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
Sheffler DJ, Wenthur CJ, Bruner JA, Carrington SJ, Vinson PN, Gogi KK, Blobaum AL, Morrison RD, Vamos M, Cosford ND, Stauffer SR, Daniels JS, Niswender CM, Conn PJ, Lindsley CW. Sheffler DJ, et al. Among authors: morrison rd. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3921-5. doi: 10.1016/j.bmcl.2012.04.112. Epub 2012 Apr 30. Bioorg Med Chem Lett. 2012. PMID: 22607673 Free PMC article.
Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.
Melancon BJ, Utley TJ, Sevel C, Mattmann ME, Cheung YY, Bridges TM, Morrison RD, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Among authors: morrison rd. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5035-40. doi: 10.1016/j.bmcl.2012.06.018. Epub 2012 Jun 15. Bioorg Med Chem Lett. 2012. PMID: 22749871 Free PMC article.
Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.
Poslusney MS, Sevel C, Utley TJ, Bridges TM, Morrison RD, Kett NR, Sheffler DJ, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Poslusney MS, et al. Among authors: morrison rd. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6923-8. doi: 10.1016/j.bmcl.2012.09.011. Epub 2012 Sep 23. Bioorg Med Chem Lett. 2012. PMID: 23062550 Free PMC article.
N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.
Lovell KM, Felts AS, Rodriguez AL, Venable DF, Cho HP, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Lovell KM, et al. Among authors: morrison rd. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3713-8. doi: 10.1016/j.bmcl.2013.05.020. Epub 2013 May 17. Bioorg Med Chem Lett. 2013. PMID: 23727046 Free PMC article.
Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.
Manka JT, Rodriguez AL, Morrison RD, Venable DF, Cho HP, Blobaum AL, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Manka JT, et al. Among authors: morrison rd. Bioorg Med Chem Lett. 2013 Sep 15;23(18):5091-6. doi: 10.1016/j.bmcl.2013.07.029. Epub 2013 Jul 23. Bioorg Med Chem Lett. 2013. PMID: 23932792 Free PMC article.
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Felts AS, Rodriguez AL, Morrison RD, Venable DF, Manka JT, Bates BS, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Felts AS, et al. Among authors: morrison rd. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5779-85. doi: 10.1016/j.bmcl.2013.09.001. Epub 2013 Sep 10. Bioorg Med Chem Lett. 2013. PMID: 24074843 Free PMC article.
110 results