Oliceridine hydrochloride (TRV130 hydrochloride) 是新颖的 MOR 激动剂，能够优先激活 G-protein 信号通路，而对 β-arrestin 的作用稍弱。
CAS：1401031-39-7
分子式：C22H31ClN2O2S
分子量：423.01
纯度：98%
存储：Store at -20°C

Background:

Oliceridine hydrochloride (TRV130 hydrochloride) is a G protein biased μ opioid receptor agonist with an pEC50 of 8.1.

Oliceridine (TRV130) elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin recruitment and receptor internalization[2].

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

[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