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TRV130
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TRV130图片
CAS NO:1401028-24-7
规格:98%
分子量:386.55
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
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%
存储:Store at -20°C

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.