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Discovery of a potent M5 antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists.
Bioorg Med Chem Lett. 2022 Nov 15;76:128988. doi: 10.1016/j.bmcl.2022.128988. Epub 2022 Sep 14.
Bioorg Med Chem Lett. 2022.
PMID: 36113671
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: whomble d.
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
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