| Literature DB >> 31390201 |
Anthony B Pinkerton1, Satyamaheshwar Peddibhotla1, Fusayo Yamamoto1, Lauren M Slosky2, Yushi Bai2, Patrick Maloney1, Paul Hershberger1, Michael P Hedrick1, Bekhi Falter1, Robert J Ardecky1, Layton H Smith1, Thomas D Y Chung1, Michael R Jackson1, Marc G Caron2, Lawrence S Barak2.
Abstract
Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator. Neurotensin receptors have been implicated in a wide variety of CNS disorders, but despite extensive efforts to develop small molecule ligands there are few reports of such compounds. Herein we describe the optimization of a quinazoline based lead to give 18 (SBI-553), a potent and brain penetrant NTR1 allosteric modulator.Entities:
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Year: 2019 PMID： 31390201 PMCID： PMC7003992 DOI： 10.1021/acs.jmedchem.9b00340
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446