Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • 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

Published Date

  • September 12, 2019

Published In

Volume / Issue

  • 62 / 17

Start / End Page

  • 8357 - 8363

PubMed ID

  • 31390201

Pubmed Central ID

  • PMC7003992

Electronic International Standard Serial Number (EISSN)

  • 1520-4804

Digital Object Identifier (DOI)

  • 10.1021/acs.jmedchem.9b00340


  • eng

Conference Location

  • United States