SBI-810 is a potent, selective arrestin-biased allosteric modulator of neurotensin receptor 1 (NTSR1, NTR1).
SBI-810 inhibits acute pain in naive mice through NTSR1 and βarr2.
SBI-810 stimulated βarr2 recruitment to the human NTSR1, failed to stimulate NTSR1-mediated activation of Gq.
SBI-810 (12 mg/kg, i.p.) effectively alleviated mechanical, spontaneous, and cold pain in mouse model of plantar incision-induced postoperative pain.
SBI-810 blocks peripheral and central sensitization in DRG and spinal cord neurons.
SBI-810 mitigates opioid abuse and does not impair motor and cognitive function
