SBI-553 is a potent, brain penetrant, and orally bioavailable allosteric modulator of neurotensin receptor 1 (NTSR1; EC 50 = 340 nM)). It acts as a ß-Arrestin-biased agonist and selectively antagonizes G protein signaling conferring profound ß-Arrestin bias towards the endogenous ligand. SBI-553...
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SBI-553 is a potent, brain penetrant, and orally bioavailable allosteric modulator of neurotensin receptor 1 (NTSR1; EC 50 = 340 nM)). It acts as a ß-Arrestin-biased agonist and selectively antagonizes G protein signaling conferring profound ß-Arrestin bias towards the endogenous ligand. 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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