TRV0109101

TRV0109101 is a μ-opioid peptide receptor (MOPR) selective agonist (K_D = 70 nM) with blood-brain barrier permeability. TRV0109101 selectively promotes G protein signaling pathway coupling while reducing the recruitment of β-arrestin. TRV0109101 inhibits opioid-induced mechanical hyperalgesia and induces antinociceptive tolerance. TRV0109101 is applicable for pain-related research^[1]. In Vitro:TRV0109101 acts as a potent, G protein-biased, MOPR-selective agonist in HEK-293 cells, with an EC₅₀ of 10 nM for cAMP inhibition^[1].
TRV0109101 (41 nM-10 μM; 5 min) interacts with the orthosteric ligand binding site of human MOPR in HEK-293 cells, with an apparent K_D of 70 nM in competition with DAMGO for β-arrestin2 recruitment^[1]. In Vivo:TRV0109101 (20 mg/kg/day; s.c.; continuous infusion; 7 days) does not promote opioid-induced mechanical allodynia in male C57BL/6 mice but does induce antinociceptive tolerance^[1].
TRV0109101 (20-40 mg/kg; s.c.; twice daily (days 1-3), single double dose (day 4); 5 days) does not induce opioid-induced mechanical allodynia in male C57BL/6 mice but does induce antinociceptive tolerance^[1].
TRV0109101 (20 mg/kg; s.c.; twice daily; 7 days) rapidly reverses mechanical allodynia in male C57BL/6 mice, though antinociceptive tolerance still develops^[1].
TRV0109101 (1-3 mg/kg; s.c.; twice daily) rapidly and fully reverses induced mechanical allodynia in male C57BL/6 mice, though antinociceptive tolerance still develops^[1].
TRV0109101 (0.1-10 mg/kg; s.c.; single dose) produces dose-dependent antinociception in the mouse 56°C hot plate assay, with an ED₅₀ of 1.1 mg/kg^[1].
TRV0109101 (1-20 mg/kg; s.c.; single dose) produces dose-dependent inhibition of fecal boli accumulation in male C57BL/6 mice, with an ED₅₀ of 6.3 mg/kg^[1].
TRV0109101 (1-20 mg/kg; s.c.; single dose) produces dose-dependent inhibition of colonic motility in male C57BL/6 mice, with an ED₅₀ of 9.4 mg/kg^[1].