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ACS Chemical Neuroscience|January 25, 2026
Discovery of VU6025733 (AG06827): A Highly Selective, Orally Bioavailable, and Structurally Distinct M<sub>4</sub> Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM) with Robust <i>In Vivo</i> EfficacyAlison R Gregro, Charlotte Park, Madeline F Long, et al.Journal of Medicinal Chemistry|April 13, 2022
Development of <b>VU6019650</b>: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M<sub>5</sub> Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use DisorderAaron T Garrison, Douglas L Orsi, Rory A Capstick, et al.The Journal of Neuroscience : the Official Journal of the Society for Neuroscience|June 23, 2012
Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal modelsGregory J Digby, Meredith J Noetzel, Michael Bubser, et al.ACS Chemical Neuroscience|December 11, 2024
Discovery of VU0467319: an M<sub>1</sub> Positive Allosteric Modulator Candidate That Advanced into Clinical TrialsMichael S Poslunsey, Michael R Wood, Changho Han, et al.ACS Chemical Neuroscience|June 6, 2026
Discovery of VU6053371/BI03738809: A First-in-Class Selective and CNS-Penetrant mGlu<sub>3</sub> Positive Allosteric Modulator (PAM) with Efficacy in a Preclinical Cognition ModelCaleb A Jones, Renn A Duncan, Kristen M Gilliland, et al.Bioorganic & Medicinal Chemistry Letters|June 29, 2019
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M<sub>4</sub> PAMsTrevor C Chopko, Changho Han, Alison R Gregro, et al.Neuron|May 5, 2015
Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR CurrentsJerri M Rook, Zixiu Xiang, Xiaohui Lv, et al.Journal of Medicinal Chemistry|June 11, 2008
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonistWilliam D Shipe, James C Barrow, Zhi-Qiang Yang, et al.Journal of Medicinal Chemistry|September 27, 2008
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channelsZhi-Qiang Yang, James C Barrow, William D Shipe, et al.Cell|June 6, 2015
Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule ProbesStuart L Schreiber, Joanne D Kotz, Min Li, et al.Pageof 57