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Page 1
Discovery of VU6016235: A Highly Selective, Orally Bioavailable, and Structurally Distinct Tricyclic M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM).
Engers JL, Baker LA, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Cho HP, Bubser M, Gray AT, Jones CK, Peng W, Rook JM, Bridges TM, Boutaud O, Conn PJ, Engers DW, Lindsley CW, Temple KJ. Engers JL, et al. Among authors: bubser m. ACS Chem Neurosci. 2024 Sep 24;15(20):3744-54. doi: 10.1021/acschemneuro.4c00465. Online ahead of print. ACS Chem Neurosci. 2024. PMID: 39316465 Free PMC article.
Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M5 Muscarinic Acetylcholine Receptor.
Li J, Orsi DL, Engers JL, Long MF, Capstick RA, Maurer MA, Presley CC, Vinson PN, Rodriguez AL, Han A, Cho HP, Chang S, Jackson M, Bubser M, Blobaum AL, Boutaud O, Nader MA, Niswender CM, Conn PJ, Jones CK, Lindsley CW, Han C. Li J, et al. Among authors: bubser m. J Med Chem. 2024 Aug 22;67(16):14394-14413. doi: 10.1021/acs.jmedchem.4c01193. Epub 2024 Aug 6. J Med Chem. 2024. PMID: 39105778 Free PMC article.
Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.
Garrison AT, Orsi DL, Capstick RA, Whomble D, Li J, Carter TR, Felts AS, Vinson PN, Rodriguez AL, Han A, Hajari K, Cho HP, Teal LB, Ragland MG, Ghamari-Langroudi M, Bubser M, Chang S, Schnetz-Boutaud NC, Boutaud O, Blobaum AL, Foster DJ, Niswender CM, Conn PJ, Lindsley CW, Jones CK, Han C. Garrison AT, et al. Among authors: bubser m. J Med Chem. 2022 Apr 28;65(8):6273-6286. doi: 10.1021/acs.jmedchem.2c00192. Epub 2022 Apr 13. J Med Chem. 2022. PMID: 35417155
Modulation of arousal and sleep/wake architecture by M1 PAM VU0453595 across young and aged rodents and nonhuman primates.
Gould RW, Russell JK, Nedelcovych MT, Bubser M, Blobaum AL, Bridges TM, Newhouse PA, Lindsley CW, Conn PJ, Nader MA, Jones CK. Gould RW, et al. Among authors: bubser m. Neuropsychopharmacology. 2020 Dec;45(13):2219-2228. doi: 10.1038/s41386-020-00812-7. Epub 2020 Aug 31. Neuropsychopharmacology. 2020. PMID: 32868847 Free PMC article.
Acute Negative Allosteric Modulation of M5 Muscarinic Acetylcholine Receptors Inhibits Oxycodone Self-Administration and Cue-Induced Reactivity with No Effect on Antinociception.
Gould RW, Gunter BW, Bubser M, Matthews RT, Teal LB, Ragland MG, Bridges TM, Garrison AT, Winder DG, Lindsley CW, Jones CK. Gould RW, et al. Among authors: bubser m. ACS Chem Neurosci. 2019 Aug 21;10(8):3740-3750. doi: 10.1021/acschemneuro.9b00274. Epub 2019 Jul 24. ACS Chem Neurosci. 2019. PMID: 31268669 Free PMC article.
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: bubser m. 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.
VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.
Engers DW, Melancon BJ, Gregro AR, Bertron JL, Bollinger SR, Felts AS, Konkol LC, Wood MR, Bollinger KA, Luscombe VB, Rodriguez AL, Jones CK, Bubser M, Yohn SE, Wood MW, Brandon NJ, Dugan ME, Niswender CM, Conn PJ, Bridges TM, Lindsley CW. Engers DW, et al. Among authors: bubser m. Bioorg Med Chem Lett. 2019 Jul 15;29(14):1714-1718. doi: 10.1016/j.bmcl.2019.05.026. Epub 2019 May 16. Bioorg Med Chem Lett. 2019. PMID: 31113706
Correction to Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models.
Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Lindsley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD. Abney KK, et al. Among authors: bubser m. ACS Chem Neurosci. 2019 May 15;10(5):2621. doi: 10.1021/acschemneuro.9b00165. Epub 2019 Mar 26. ACS Chem Neurosci. 2019. PMID: 30912639 No abstract available.
80 results