Oliceridine hydrochloride 是 G 蛋白偏向 μ 阿片受体 (pEC50: 8.1) 的激动剂。

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

Oliceridine elicits robust G protein signaling, with potency and efficacy similar to morphine [2].

In mice, Robust antinociception, complete inhibition of gastrointestinal function produced by Oliceridine treatment, and weak abuse-related effects [1]. In an analgesic assay, Oliceridine displays an ED50 of 0.9 mg/kg. 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 (1.2 mg/kg, s.c.) significantly depresses the respiration of mice [3].

1401031-39-7

C22H31ClN2O2S

423.01

TRV130 (hydrochloride)

DMSO:38 mg/mL (89.83 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years