TRV130 is a novel mu opioid receptor (MOR) agonist that preferentially activates G-protein versus β-arrestin signaling pathways coupled to MORs.
CAS：1401028-24-7
分子式：C22H30N2O2S
分子量：386.55
纯度：98%
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Background:

TRV130 is a novel mu opioid receptor (MOR) agonist that preferentially activates G-protein versus β-arrestin signaling pathways coupled to MORs.

In cell-based assays, TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin recruitment and receptor internalization[2].

TRV130 treatment produces robust antinociception, complete inhibition of gastrointestinal function, and weak abuse-related effects in mice[1]. TRV130 displays an ED50 of 0.9 mg/kg in an analgesic assay. TRV130 analgesia is reversible in mice by administration of 3 mg/kg naloxone s.c. 15 minutes after TRV130 dosing. In the rat 52°C hot plate, TRV130 is 10-fold more potent than morphine with ED50 of 0.32 and 3.2 mg/kg, respectively. TRV130 (0.3 mg/kg, s.c.) possesses an improved therapeutic index of analgesia to constipation relative to morphine in mice[2]. TRV130 (1.2 mg/kg, s.c.) significantly depresses respiration of mice[3].

参考文献:
[1]. Altarifi AA, et al. Effects of acute and repeated treatment with the biased mu opioid receptor agonist TRV130 (oliceridine) on measures of antinociception, gastrointestinal function, and abuse liability in rodents. J Psychopharmacol. 2017 Jan 1:2698811166
[2]. DeWire SM, et al. A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17.
[3]. Manglik A, et al. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 8;537(7619):185-190.