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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

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MLA
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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.
Journal cover image

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