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