SBI-553 is a potent, brain penetrant, and orally bioavailable allosteric modulator of neurotensin receptor 1 (NTSR1, EC50 = 340 nM)).1 It acts as a ß-Arrestin-biased agonist and selectively antagonizes G protein signaling conferring profound ß-Arrestin bias towards the endogenous ligand.2,3 SBI-553 displayed efficacy in mouse models of psychostimulant abuse without the characteristic undesirable side effects of unbiased NTSR1 agonism. This functionally selective modulation of NTSR1 may be a new therapeutic approach to treating psychostimulant abuse and other chemical and behavioral addictions.
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