Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.
Publication
, Journal Article
Pinkerton, AB; Peddibhotla, S; Yamamoto, F; Slosky, LM; Bai, Y; Maloney, P; Hershberger, P; Hedrick, MP; Falter, B; Ardecky, RJ; Smith, LH ...
Published in: J Med Chem
September 12, 2019
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.
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Published In
J Med Chem
DOI
EISSN
1520-4804
Publication Date
September 12, 2019
Volume
62
Issue
17
Start / End Page
8357 / 8363
Location
United States
Related Subject Headings
- beta-Arrestins
- Structure-Activity Relationship
- Receptors, Neurotensin
- Rats
- Quinazolines
- Molecular Structure
- Mice, Knockout
- Mice, Inbred C57BL
- Mice
- Medicinal & Biomolecular Chemistry
Citation
APA
Chicago
ICMJE
MLA
NLM
Pinkerton, A. B., Peddibhotla, S., Yamamoto, F., Slosky, L. M., Bai, Y., Maloney, P., … Barak, L. S. (2019). Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators. J Med Chem, 62(17), 8357–8363. https://doi.org/10.1021/acs.jmedchem.9b00340
Pinkerton, Anthony B., Satyamaheshwar Peddibhotla, Fusayo Yamamoto, Lauren M. Slosky, Yushi Bai, Patrick Maloney, Paul Hershberger, et al. “Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.” J Med Chem 62, no. 17 (September 12, 2019): 8357–63. https://doi.org/10.1021/acs.jmedchem.9b00340.
Pinkerton AB, Peddibhotla S, Yamamoto F, Slosky LM, Bai Y, Maloney P, et al. Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators. J Med Chem. 2019 Sep 12;62(17):8357–63.
Pinkerton, Anthony B., et al. “Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.” J Med Chem, vol. 62, no. 17, Sept. 2019, pp. 8357–63. Pubmed, doi:10.1021/acs.jmedchem.9b00340.
Pinkerton AB, Peddibhotla S, Yamamoto F, Slosky LM, Bai Y, Maloney P, Hershberger P, Hedrick MP, Falter B, Ardecky RJ, Smith LH, Chung TDY, Jackson MR, Caron MG, Barak LS. Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators. J Med Chem. 2019 Sep 12;62(17):8357–8363.
Published In
J Med Chem
DOI
EISSN
1520-4804
Publication Date
September 12, 2019
Volume
62
Issue
17
Start / End Page
8357 / 8363
Location
United States
Related Subject Headings
- beta-Arrestins
- Structure-Activity Relationship
- Receptors, Neurotensin
- Rats
- Quinazolines
- Molecular Structure
- Mice, Knockout
- Mice, Inbred C57BL
- Mice
- Medicinal & Biomolecular Chemistry