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SBI-810 hydrochloride is a functional selective allosteric modulator of the β-arrestin-biased neurotensin receptor 1 (NTSR1). It modulates NTSR1-G protein signaling in a G protein-specific manner in the presence of the endogenous ligand neurotensin (NT). SBI-810 hydrochloride fully antagonizes NT-induced Gq activation, partially antagonizes NT-induced Gi1 activation, while allowing activation of GoA and G12 by NTSR1.