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SBI-810 is a β-arrestin-2-biased positive allosteric modulator of neurotensin receptor 1 (NTS1).1,2 It increases neurotensin-1-induced β-arrestin-2 recruitment to human NTS1 receptors in HEK293T cells (EC50 = 98 nM).2 SBI-810 (12 mg/kg) increases the paw withdrawal threshold in mouse models of postoperative, neuropathic, and inflammatory pain.1 It reduces morphine-induced conditioned place preference (CPP) in mice without inducing CPP itself when administered at a dose of 30 mg/kg.
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1. Arrestin-
2. Discovery of β-
Arrestin-