SBI-553
ß-Arrestin-biased NTSR1 modulator / 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.
Biochemicals & reagents
1849603-72-0
1) Pinkerton et al. (2019), Discovery of ß-Arrestin Biased, Orally Bioavailable and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators; J. Med. Chem. 62 8357 2) Slosky et al. (2020), ß-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors; Cell 181 1364 3) Duan et al. (2023), GPCR activation and GRK2 assembly by a biased intracellular agonist; Nature 620 676
-20°C
TARGET: GPCR -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Addiction