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Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous sys-tem where it acts as a neuromodulator. Neurotensin receptors have been implicated… Click to show full abstract
Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous sys-tem 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.
Keywords:
neurotensin receptor;
receptor ntr1;
cns;
ntr1 allosteric;
receptor
Journal Title: Journal of medicinal chemistry
Year Published: 2019
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Journal Title: Journal of medicinal chemistry
Year Published: 2019
Link to full text (if available)
Share on Social Media: Sign Up to like & get
recommendations!